Endocrinology & Hormones

Effect of follicular wave synchronization using a progesterone-releasing intravaginal device-based protocol on in vitro embryo production in Bos taurus cows subjected to 14-day intervals ovum pick-up

80 | Feb 11 2024

The study highlighted that follicular wave synchronization in Angus cows before ovum pick-up enhanced embryo quality while revealing sustained carryover effects on follicle numbers and cumulus-oocyte complex morphology. [Read the Full Post]

Ecological benefits of artificial light at night (ALAN): Accelerating the development and metamorphosis of marine shellfish larvae

221 | Feb 10 2024

The comprehensive study on artificial light at night (ALAN) reveals a surprising positive impact of short-wavelength blue light on Pacific abalone embryonic development, offering crucial insights into the differential effects of light spectrums and their implications for marine benthic ecosystems. [Read the Full Post]

Sibutramine-Induced Nonischemic Cardiomyopathy

236 | Feb 09 2024

The case report of sibutramine-induced nonischemic cardiomyopathy in a young individual underscores the critical need for safer anti-obesity medications and vigilant patient monitoring to mitigate severe cardiovascular risks associated with pharmacotherapy. [Read the Full Post]

[99mTc]Tc-HYNIC-RM2: A potential SPECT probe targeting GRPR expression in prostate cancers

106 | Jan 12 2024

The study successfully synthesized and evaluated the 99mTc-labeled HYNIC-RM2 probe, demonstrating high affinity, metabolic stability, enhanced tumor uptake, and clear visualization of GRPR-positive prostate cancer tumors via SPECT imaging, affirming its potential as a promising agent for further exploration in targeting GRPR. [Read the Full Post]

AURKA inhibitor-induced PD-L1 upregulation impairs antitumor immune responses

97 | Jan 09 2024

"Our study reveals that the AURKA inhibitor MLN8237 enhances the effectiveness of immunotherapy in tumor cells by upregulating PD-L1 expression, presenting a promising approach to augmenting anti-tumor responses and potentially overcoming drug resistance in targeted therapy." [Read the Full Post]

A tool for nuclear imaging of the SARS-CoV-2 entry receptor: molecular model and preclinical development of ACE2-selective radiopeptides

180 | Dec 30 2023

This study developed gallium-labeled radiopeptides, notably [67Ga]Ga-HBED-CC-DX600, showing selective ACE2 targeting and promising tissue distribution, offering a potential noninvasive imaging tool to assess (patho)physiological ACE2 expression levels post-SARS-CoV-2 infection. [Read the Full Post]

Age- and sex-adjusted reference intervals for steroid hormones measured by liquid chromatography‑tandem mass spectrometry (LC-MS/MS) using a widely available kit

118 | Dec 18 2023

This study established reference intervals for nine endogenous steroids using a commercially available liquid chromatography-tandem-mass-spectrometry (LC MS/MS) kit, revealing age and sex as major determinants of steroid levels while highlighting limitations in sensitivity for certain compounds, thereby providing valuable insights for interpreting steroid profiles in routine laboratory analyses. [Read the Full Post]

Theophylline-induced endothelium-dependent vasodilation is mediated by increased nitric oxide release and phosphodiesterase inhibition in rat aorta

212 | Dec 06 2023

Theophylline-induced endothelium-dependent vasodilation in isolated rat thoracic aortas is mediated by increased endothelial nitric oxide release, guanylate cyclase activation, elevated cGMP levels, and enhanced endothelial nitric oxide synthase phosphorylation. [Read the Full Post]

The anticonvulsant effect of saiga horn on febrile seizures by regulating brain serotonin content and inhibiting neuroinflammation

154 | Nov 30 2023

Saiga antelope horn (SAH) demonstrates significant anticonvulsant effects in a febrile seizures rat model by modulating neurotransmitter levels, exerting anti-inflammatory actions, and activating the ER-β/TPH2/5-HT signaling pathway, offering potential insights for the development of SAH-based treatments and substitutes. [Read the Full Post]

High-intensity interval training improves fatty infiltration in the rotator cuff through the β3 adrenergic receptor in mice

201 | Nov 25 2023

High-Intensity Interval Training (HIIT) improved muscle quality in a rotator cuff tear model by activating the β3 adrenergic receptor pathway, enhancing supraspinatus muscle function, and reducing atrophy and fatty infiltration. [Read the Full Post]

Proxalutamide reduces SARS-CoV-2 infection and associated inflammatory response

42 | Nov 25 2023

The study suggests that proxalutamide, an androgen receptor antagonist, has the potential to prevent SARS-CoV-2 infection, inhibit multiple variants, protect against cytokine-induced lung damage, and may yield promising clinical outcomes pending ongoing phase 3 trials. [Read the Full Post]

ACSS2-mediated NF-κB activation promotes alkaliptosis in human pancreatic cancer cells

351 | Nov 11 2023

In this hypothetical scenario, researchers have identified ACSS2 as a key regulator of alkaliptosis, a pH-dependent cell death process, and its manipulation holds promise as a potential therapeutic strategy for pancreatic ductal adenocarcinoma (PDAC) treatment. [Read the Full Post]

Novel vesicular and particulate drug delivery systems for topical treatment of acne

83 | Oct 27 2023

The utilization of vesicular and particulate drug delivery systems in topical antiacne treatment shows promise in minimizing side effects while maintaining efficacy, offering a novel approach to improve patient outcomes. [Read the Full Post]

The protective effects of NE 52-QQ57 against interleukin-33-induced inflammatory response in activated synovial mast cells

535 | Oct 09 2023

The study suggests that inhibiting GPR4 signaling with the antagonist NE 52-QQ57 may have therapeutic benefits in rheumatoid arthritis by reducing inflammatory responses and oxidative stress in synovial mast cells. [Read the Full Post]

Tamoxifen pharmacokinetics and pharmacodynamics in older patients with non-metastatic breast cancer

76 | Oct 06 2023

In older women with non-metastatic breast cancer, higher concentrations of tamoxifen and its metabolites were observed, independent of CYP2D6 and CYP3A4 gene polymorphisms, but these differences did not have a significant impact on clinical outcomes. [Read the Full Post]

An overview of PROTACs: a promising drug discovery paradigm

0 | Sep 25 2023

This review provides a comprehensive analysis of the features of PROTAC technology, principles for designing efficient PROTACs, their applications across different protein categories, progress in clinical trials, and the challenges and limitations they may face, serving as a valuable reference for further advancements in PROTAC research and application. [Read the Full Post]

Recent understandings about hypertension management in type 2 diabetes: What are the roles of SGLT2 inhibitor, GLP-1 receptor agonist, and finerenone?

90 | Sep 20 2023

Managing blood pressure in patients with diabetes is crucial for preventing cardiovascular complications, and emerging drugs like GLP-1RA, SGLT2i, and finerenone have shown potential in both lowering blood pressure and providing cardio-renal protection. [Read the Full Post]

Phospholipase D2 targeted by miR-5132-5p alleviates cerulein-induced acute pancreatitis via the Nrf2/NFκB pathway

299 | Sep 19 2023

The study revealed that phospholipase D2 (PLD2), targeted by microRNA-5132-5p (miR-5132-5p), can attenuate cerulein-induced acute pancreatitis in AR42J cells by modulating the Nrf2/NFκB pathway, highlighting its potential as a therapeutic target for AP. [Read the Full Post]

Acetylation regulates the nucleocytoplasmic distribution and oncogenic function of karyopherin alpha 2 in lung adenocarcinoma

372 | Sep 18 2023

The acetylation of KPNA2 by CBP/p300 promotes cytosolic localization and suppresses its oncogenic activity in lung cancer cells. [Read the Full Post]

Phase 1 study of oral selective estrogen receptor degrader (SERD) amcenestrant (SAR439859), in Japanese women with ER-positive and HER2-negative advanced breast cancer (AMEERA-2)

74 | Sep 16 2023

The AMEERA-2 study found that amcenestrant 400 mg QD demonstrated favorable safety and efficacy, leading to its selection as the recommended Phase II dose for monotherapy in a larger clinical trial for metastatic breast cancer. [Read the Full Post]

Design of SERENA-6, a phase III switching trial of camizestrant in ESR1-mutant breast cancer during first-line treatment

180 | Sep 12 2023

The SERENA-6 study is a phase III trial evaluating the efficacy and safety of switching from an aromatase inhibitor to camizestrant, while maintaining the same CDK4/6 inhibitor treatment, in HR+/HER2- advanced breast cancer patients with ESR1 mutations, with the primary endpoint being progression-free survival. [Read the Full Post]

Evaluation of mitochondrial oxidative toxicity in mammalian cardiomyocytes by determining the highly reproducible and reliable increase in mitochondrial superoxides after exposure to therapeutic drugs

0 | Sep 11 2023

The study demonstrated that increased MitoSOX™ red fluorescence following drug exposure is a reliable biomarker for evaluating mitochondrial-specific oxidative toxicity in cardiomyocytes, offering potential applications in new drug development. [Read the Full Post]

Divergent splanchnic sympathetic efferent nerve pathways regulate interleukin-10 and tumour necrosis factor-α responses to endotoxaemia

325 | Jul 19 2023

This study demonstrates that the splanchnic sympathetic nerves mediate an endogenous neural reflex that enhances interleukin-10 levels and suppresses tumor necrosis factor-α levels in response to systemic immune challenge, with distinct pathways regulating these cytokine responses. [Read the Full Post]

Generation of a Live Attenuated Influenza A Vaccine Using Chemical-Triggered Intein

157 | Jul 01 2023

A novel method using 4-hydroxytamoxifen (4-HT)-dependent intein insertion into the polymerase acidic (PA) protein of influenza A virus generates recombinant viruses that demonstrate excellent replication characteristics and induce robust immunity, offering potential for the development of a more effective live attenuated influenza vaccine and possibly vaccines against other pathogens as well. [Read the Full Post]

5-Oxoproline Enhances 4-Hydroxytamoxifen-induced Cytotoxicity by Increasing Oxidative Stress in MCF-7 Breast Cancer Cells

0 | Jul 01 2023

In conclusion, the study demonstrates that 5-oxoproline enhances the cytotoxic effects of 4-hydroxytamoxifen in estrogen receptor-positive breast cancer cells under normal glucose conditions, suggesting the potential utility of monocarboxylate transporter inhibitors as adjunctive therapeutic agents. [Read the Full Post]

Triplet Therapy in Metastatic Castrate Sensitive Prostate Cancer (mCSPC)-A Potential New Standard of Care

110 | Jun 15 2023

This article reviews the phase-three data on triplet therapy for metastatic castrate-sensitive prostate cancer (mCSPC), addresses knowledge gaps, discusses implementation challenges, and proposes a treatment selection algorithm for clinicians. [Read the Full Post]

Personalizing approaches to the management of metastatic hormone sensitive prostate cancer: role of advanced imaging, genetics and therapeutics

111 | Jun 15 2023

Advancements in the diagnosis and management of metastatic hormone-sensitive prostate cancer (mHSPC), including improved imaging techniques, germline multigene testing, and the integration of multiple agents, have significantly enhanced patient care and outcomes in the last decade. [Read the Full Post]

An overview of PROTACs: a promising drug discovery paradigm

175 | May 16 2023

PROTAC technology has emerged as a promising therapeutic approach due to its ability to target "undruggable" proteins and induce complete protein degradation, but further research and development are needed to optimize its efficacy and overcome its limitations. [Read the Full Post]

Targeting androgen receptor degradation with PROTACs from bench to bedside

110 | May 16 2023

Recent advances in the development of small-molecule PROTAC AR degraders have shown promising clinical efficacy in the treatment of prostate cancer, overcoming resistance mechanisms and improving current therapies. [Read the Full Post]

Quality by Design (QbD)-Steered Development and Validation of Analytical and Bioanalytical Methods for Raloxifene: Application of Monte Carlo Simulations and Variance Inflation Factor

196 | May 05 2023

The study developed and validated a sensitive, rapid, reproducible, and economical HPLC method for quantifying raloxifene hydrochloride using QbD principles, and demonstrated its applicability for drug quantification in biological fluids, as well as in bulk and marketed dosage forms. [Read the Full Post]

Randomised, prospective, blinded, clinical trial of opioid-free injectable anaesthesia with or without multimodal analgesia in kittens undergoing ovariohysterectomy

232 | Apr 27 2023

This study found that an opioid-free injectable anaesthetic protocol with multimodal analgesia provided effective pain relief and reduced the need for rescue analgesia in kittens undergoing ovariohysterectomy, while also observing a decrease in food intake due to pain. [Read the Full Post]

The effect of rifampin on serum etonogestrel concentrations and biomarkers of ovulation among contraceptive implant users: a pharmacokinetic and pharmacodynamic study

86 | Apr 27 2023

Short-term exposure to rifampin, a strong CYP3A inducer, can lead to clinically significant decreases in serum ENG concentrations and changes in biomarkers indicative of waning suppression of ovulation in ENG implant users. [Read the Full Post]

A 2023 update on the advancements in the treatment of agitation in Alzheimer's disease

271 | Apr 16 2023

Recent advances in the understanding of neurobiological mechanisms of agitation in Alzheimer's Disease have led to the identification of several agents with promise for treating agitation, and clinical trials are underway to develop safe and efficacious treatment options. [Read the Full Post]

Papain Exerts an Anti-atherosclerosis Effect with Suppressed MPA-mediated Foam Cell Formation by Regulating the MAPK and PI3K/Akt-NF-κB Pathways

405 | Apr 13 2023

The study found that papain inhibits MPA-induced foam cell formation by inactivating the MAPK and PI3K/Akt-NF-κB pathways, thereby exerting an anti-AS effect. [Read the Full Post]

HOW TO OPTIMALLY SEQUENCE AVAILABLE THERAPY LINES IN ADVANCED PROSTATE CANCER

105 | Apr 08 2023

The optimal sequencing of available therapy lines for advanced prostate cancer should be individualized based on several factors and decided in collaboration with the patient and their healthcare team. [Read the Full Post]

Modeling drug-induced liver injury and screening for anti-hepatofibrotic compounds using human PSC-derived organoids

303 | Mar 27 2023

Human liver organoids derived from pluripotent stem cells have the potential to serve as a preclinical model for drug safety testing and anti-fibrotic drug screening. [Read the Full Post]

Investigation of the Pharmacokinetics and Metabolic Fate of Fasiglifam (TAK-875) in Male and Female Rats Following Oral and Intravenous Administration

273 | Mar 27 2023

Fasiglifam has good oral bioavailability and is extensively metabolized in rats, with a novel biotransformation observed and sex-related differences in drug elimination. [Read the Full Post]

Effect of 11-Deoxycorticosterone in the Transcriptomic Response to Stress in Rainbow Trout Skeletal Muscle

201 | Mar 26 2023

The study demonstrates the role of 11-deoxycorticosterone (DOC) in modulating the stress response of skeletal muscles in rainbow trout and highlights its differential modulation by glucocorticoid receptor (GR) and mineralocorticoid receptor (MR), complementing the action of cortisol. [Read the Full Post]

Evaluation of Pain and Use of Analgesics during Medical Termination of Pregnancy in Real-Life Settings

307 | Mar 25 2023

This study evaluated pain related to medical termination of pregnancy (MToP) and its management in 23 centers in France, finding that higher doses of misoprostol were strongly associated with both pain and curative analgesic intake, while analgesic prophylaxis prescription was associated with a decreased risk of curative analgesic intake. [Read the Full Post]

Update on current contraceptive options: A case-based discussion of efficacy, eligibility, and use

86 | Mar 24 2023

It is important for clinicians to be informed about the full spectrum of contraceptive options, including new and established methods, to improve patient reproductive autonomy and remove unnecessary barriers to contraception. [Read the Full Post]

Response to medroxyprogesterone acetate (NSC-26386) as secondary hormone therapy for metastatic breast cancer in postmenopausal women

96 | Mar 24 2023

This study evaluated the use of medroxyprogesterone acetate in treating metastatic breast cancer in postmenopausal women and found it to be of minimal usefulness as secondary therapy. [Read the Full Post]

Abigene, a Prospective, Multicentric Study of Abiraterone Acetate Pharmacogenetics in Metastatic Castration-Resistant Prostate Cancer

179 | Mar 21 2023

This study suggests that genetic variations in CYP17A1 and other androgen-related genes may help predict the efficacy and toxicity of abiraterone acetate treatment in advanced prostate cancer patients. [Read the Full Post]

Prospective role of 3βHSD1 in prostate cancer precision medicine

151 | Mar 20 2023

3βHSD1 is both a promising therapeutic target and a predictive biomarker for prostate cancer, with the development of novel inhibitors and a better understanding of its regulatory mechanisms providing new opportunities for disease management. [Read the Full Post]

Prophylactic Agents for Preventing Cardiotoxicity Induced Following Anticancer Agents: A Systematic Review and Meta-Analysis of Clinical Trials

153 | Mar 14 2023

This meta-analysis showed that prophylactic treatment with cardio-protective drugs can protect the left ventricular ejection fraction (LVEF) and prevent EF drop in patients undergoing chemotherapy with anthracyclines. [Read the Full Post]

Pharmacokinetic and Pharmacodynamic Comparison of Fluticasone Propionate/Formoterol Fumarate Administered via a Pressurized Metered-Dose Inhaler and a Novel Breath-Actuated Inhaler in Healthy Volunteers

182 | Mar 13 2023

The passage describes the results of two studies comparing the exposure of fluticasone/formoterol following administration via BAI with pMDI with/without a spacer in healthy volunteers, which showed that BAI performance was comparable to pMDI and systemic safety with BAI was no worse than the primary comparator. [Read the Full Post]

Effect of double-dose levonorgestrel subdermal implant in women taking efavirenz-based antiretroviral therapy: The DoubLNG pharmacokinetic study

65 | Mar 06 2023

The study found that double-dose LNG implants did not fully overcome drug-drug interactions with efavirenz-based ART in women with HIV, and alternative ART without drug-drug interactions should be used with contraceptive implants. [Read the Full Post]

IgG4 related pericardium and lung disease in pediatric patient complicated with fatal massive hemoptysis: a case report and review of literature

143 | Mar 06 2023

This case highlights the rarity and severity of pericardio-pulmonary involvement in pediatric IgG4-RD and the potential risks associated with the use of rituximab as a rescue therapy. [Read the Full Post]

A case of systemic lupus erythematosus having concurrent Evans syndrome and acquired thrombotic thrombocytopenic purpura

112 | Mar 06 2023

TTP in patients with refractory immune-mediated thrombocytopenia and atypical symptoms. [Read the Full Post]

Bioactive compounds from four Indian medicinal plants have different potency to induce sex reversal in Nile tilapia: A chromatographic, molecular docking and in silico analysis

120 | Mar 05 2023

The study evaluated the anti-aromatase activity of four plant extracts, identified androgenic bioactive compounds, and determined their potential for masculinization in Nile tilapia, with Tribulus terrestris and Asparagus racemosus extracts showing the greatest potency and 2,4-bis(1,1-dimethylethyl) phenol being identified as a potential compound for masculinization through dietary administration. [Read the Full Post]

Transport of hydrocortisone in targeted layers of the skin by multi-lamellar liposomes

81 | Mar 04 2023

Encapsulation of hydrocortisone in multi-lamellar liposomes enabled targeted delivery to different skin layers with non-Fickian diffusion observed for formulations targeting the stratum corneum and living epidermis. [Read the Full Post]

A Novel Mutation in Melanocortin Receptor 2 and a Reported Mutation in Melanocortin Receptor 2 Accessory Protein: Three Chinese Cases with Familial Glucocorticoid Deficiency

81 | Mar 04 2023

This report describes three Chinese patients with familial glucocorticoid deficiency, their different clinical presentations, and the importance of genetic testing for accurate diagnosis and appropriate treatment. [Read the Full Post]

Traditional and disease-related cardiovascular risk factors in ANCA-associated vasculitis: a prospective, two-centre cohort study

143 | Feb 28 2023

The study found that age, Framingham risk score, HbA1c level, Diabetes Mellitus (DM), and previous cardiovascular event were significantly associated with cardiovascular events in patients with ANCA-associated vasculitis, highlighting the importance of treating risk factors for optimal long-term outcomes. [Read the Full Post]

Combination chemotherapy with vincristine (NSC-67574), procarbazine (NSC-77213), prednisone (NSC-10023) with or without nitrogen mustard (NSC-762)(MOPP vs OPP) in children with recurrent brain tumors

109 | Feb 28 2023

The study compared two chemotherapy regimens in treating recurrent central nervous system tumors in 73 pediatric patients, with the more toxic MOPP producing more responses but not statistically significant differences in duration of response or survival, and with two patients in the MOPP group experiencing fatal myelosuppression. [Read the Full Post]

Inclusion complex of ketoconazole and p-sulfonic acid calix[6]arene improves antileishmanial activity and selectivity against Leishmania amazonensis and Leishmania infantum

129 | Feb 18 2023

An inclusion complex (IC6HKTZ) of ketoconazole and p-sulfonic acid calix[6]arene (CX6SO3H) was prepared to improve solubility and efficacy of ketoconazole against Leishmania amazonensis and Leishmania infantum, and results showed a 95-fold solubility enhancement and improved antileishmanial activities. [Read the Full Post]

Phytochemical Analysis, Antifungal, and Antioxidant Properties of Two Herbs ( Tristemma mauritianum and Crassocephalum bougheyanum) and One Tree ( Lavigeria macrocarpa) Species

222 | Feb 17 2023

Tristemma mauritianum, Crassocephalum bougheyanum, and Lavigeria macrocarpa showed promising antifungal and antioxidant properties due to high phenolic, tannin, and flavonoid content, with T. mauritianum displaying the highest antifungal and antioxidant activities and a synergistic effect with ketoconazole against clinical resistant Candida isolates. [Read the Full Post]

Allolobophora caliginosa coelomic fluid and extract alleviate glucocorticoid-induced osteoporosis in mice by suppressing oxidative stress and regulating osteoblastic/osteoclastic-related markers

321 | Feb 16 2023

This study investigated the chemo-preventive activity of A.calignosa coelomic fluid and extract on glucocorticoid-induced osteoporosis in mice, revealing that both showed chemo-preventive activity by inhibiting oxidative stress and regulating expression and activity of osteoblast/osteoclast-related markers, resulting in increased bone mineral density and decreased activity of alkaline phosphatase and parathyroid hormone. [Read the Full Post]

16a-Methyl corticosteroids; a new series of anti-inflammatory compounds; clinical appraisal of their antirheumatic potencies

256 | Feb 16 2023

Four new derivatives of hydrocortisone with a methyl grouping at the 16a-carbon position were synthesized and studied in human subjects for anti-inflammatory activity, with 16a-methyl 9a-fluoroprednisolone showing the highest potency per milligram and potential for long-term therapeutic use. [Read the Full Post]

A systematic review and meta-analysis on overall survival, failure-free survival and safety outcomes in patients with metastatic hormone-sensitive prostate cancer treated with new anti-androgens

181 | Feb 13 2023

The use of antiandrogens (abiraterone, apalutamide, darolutamide, or enzalutamide) in combination with androgen-deprivation therapy (ADT) improves overall survival and failure-free survival in hormone-sensitive metastatic prostate cancer, but causes an increase in treatment-related adverse events. [Read the Full Post]

Effect of Gubenyiliu formula II and its disassembled prescriptions on cell autophagy in breast cancer through PI3K/AKT/mTOR pathway

519 | Feb 12 2023

This study confirmed that GYII can effectively treat breast cancer by inhibiting the PI3K/AKT/mTOR signaling pathway-mediated autophagy, while QX and FZ have different effects on tumor growth and metastasis. [Read the Full Post]

Specific gene module pair-based target identification and drug discovery

700 | Feb 12 2023

A novel method called "gene module pair-based target identification (GMPTI)" was developed to predict the targets of new compounds using consensus gene modules extracted from transcriptional profiles induced by perturbagens of known targets, resulting in the discovery of novel inhibitors for three PI3K pathway proteins. [Read the Full Post]

Variations in Incidence of Trigger Finger and Response to Corticosteroid Injection after Aromatase Inhibitor Therapy for Breast Cancer

134 | Feb 11 2023

Patients receiving aromatase inhibitors for breast cancer have a higher incidence of trigger finger, with those switching regimens due to musculoskeletal symptoms and poorly controlled diabetics being more likely to fail steroid treatment. [Read the Full Post]

Evaluation of The Effect of Letrozole in the Ovarian Hyperstimulation Syndrome Prevention in Participants at Risk of Treatment with Ovulation-Stimulating Drugs:A Randomized Controlled Trial

166 | Feb 11 2023

The results of this study showed that administering Letrozole with a GnRH antagonist protocol in PCOS cases undergoing IVF reduced the incidence of ovarian hyperstimulation syndrome, but had no significant effect on oocyte retrieval, implantation, or pregnancy rates. [Read the Full Post]

[Androgens and Parkinson's disease: the role in humans and in experiment]

132 | Feb 05 2023

Parkinson's disease is more common in men than women and studies suggest a role of sex hormones in its pathogenesis, but current drug therapy with androgens, androgen precursors, antiandrogens and drugs that modify androgen metabolism have not shown sufficient effectiveness and 5α-reductase inhibitors show promise for neuroprotection and anti-dyskinetic properties, but more research is needed. [Read the Full Post]

Anti-Androgenic Therapies Targeting the Luminal Androgen Receptor of a Typical Triple-Negative Breast Cancer

205 | Feb 04 2023

A review of literature shows a need for anti-androgenic strategies against luminal androgen receptor (LAR) triple-negative breast cancer (TNBC) to improve the treatment and prognosis of TNBC by targeting the androgen receptor, with bicalutamide and enzalutamide being currently assessed as potential treatments. [Read the Full Post]

A trio of tumor suppressor miRNA downregulates CREB5 dependent transcription to modulate neoadjuvant hormonal therapy sensitivity

80 | Feb 04 2023

MicroRNAs 142-3p, 150-5p, and 342-3p can contribute to neoadjuvant hormonal therapy resistance in prostate cancer by targeting CREB5 and inhibit cell proliferation in vitro, according to a study. [Read the Full Post]

On-treatment derived neutrophil-to-lymphocyte ratio and survival with palbociclib and endocrine treatment: analysis of a multicenter retrospective cohort and the PALOMA-2/3 study with immune correlates

104 | Feb 04 2023

On-treatment derived neutrophil-to-lymphocyte ratio (dNLR) is a significant predictor of progression-free survival (PFS) in postmenopausal women with HR-positive, HER2-negative advanced breast cancer (ABC) receiving palbociclib and endocrine treatment, with reduction in dNLR after treatment predictive of a survival benefit and evidence of systemic immune responses elicited by palbociclib. [Read the Full Post]

Ostarine-Induced Myogenic Differentiation in C2C12, L6, and Rat Muscles

41 | Feb 03 2023

Ostarine stimulates muscle tissue proliferation and differentiation via the androgen receptor, as shown in studies of C2C12 and L6 cells, and 30-day administration of ostarine increased myogenin, MyoD, and MyH expression and muscle mass in rats. [Read the Full Post]

Risk of cognitive impairment in men with advanced prostate cancer treated with novel hormonal agents: a systematic review and network meta-analysis

76 | Nov 13 2022

Shi-Wei Huang et al. found that NHAs, especially enzalutamide, might increase the risk of cognitive impairment compared with placebo/standard care. [Read the Full Post]

Baseline Plasma Tumor DNA (ctDNA) Correlates with PSA Kinetics in Metastatic Castration-Resistant Prostate Cancer (mCRPC) Treated with Abiraterone or Enzalutamide

171 | May 16 2022

Vincenza Conteduca et al. thought that elevated ctDNA levels and AR gain were negatively and independently correlated with PSA kinetics in mCRPC men treated with abiraterone or enzalutamide. [Read the Full Post]

Long-Term Outcomes of Targeted Therapy after First-Line Immunotherapy in BRAF-Mutated Advanced Cutaneous Melanoma Patients-Real-World Evidence

233 | Apr 28 2022

Paweł Rogala et al. found that BRAFi/MEKi therapy was effective in the second-line in advanced and metastatic melanoma patients. [Read the Full Post]

Long-term Outcomes for Ibrutinib-Rituximab and Chemoimmunotherapy in CLL: Updated Results of the E1912 Trial

311 | Apr 17 2022

Tait D Shanafelt et al. found that Ibrutinib-rituximab therapy offered superior PFS relative to FCR in both IGHV mutated and unmutated CLL patients as well as superior OS. [Read the Full Post]

Hyperactivation of MAPK Induces Tamoxifen Resistance in SPRED2-Deficient ERα-Positive Breast Cancer

280 | Feb 27 2022

Vasiliki Vafeiadou et al. indicated that SPRED2 might also be a tumor suppressor for breast cancer and that it was a key regulator of cellular sensitivity to 4-OHT. [Read the Full Post]

Impact of New Systemic Therapies in Overall Survival in Non-Metastatic Castration Resistant Prostate Cancer: Systematic Review and Meta-Analysis

307 | Dec 20 2021

Alejo Rodriguez-Vida et al. found that first-line treatment of nmCRPC patients with anti-androgens increased OS with an acceptable safety profile. [Read the Full Post]

Prostate Cancer Detected by Choroidal Tumor and Complete Response to Hormonal Therapy: Case Report and Literature Review of 24 Patients With Choroidal Metastasis From Prostate Cancer

395 | Jun 25 2021

Toshihiko Matsuo et al. found that metastatic choroidal tumors of prostate cancer would show good response to hormonal therapy when the therapy had not been initiated. [Read the Full Post]

[Molecular background of BRAF inhibitor induced resistance in BRAFV600E mutant melanoma cell lines]

493 | Jun 04 2021

István Szász et al. found that withdrawal of the inhibitor reduced cell proliferation in the resistant cells. [Read the Full Post]

Prognostic value of [ 18 F]FDG PET/CT in patients with CNS lymphoma receiving ibrutinib-based therapies

436 | May 14 2021

Simone Krebs et al. found that higher lesional metabolic parameters were inversely related to outcome in patients undergoing ibrutinib-based therapies, and sumSUVmax emerged as a strong independent prognostic factor. [Read the Full Post]

4-hydroxytamoxifen does not deteriorate cardiac function in cardiomyocyte-specific MerCreMer transgenic mice

624 | Mar 09 2021

Andre Heinen et al. investigated potential adverse effects of DNA editing by the αMHC-MerCreMer/loxP system in combination with a low-dose treatment protocol with the tamoxifen metabolite 4-hydroxytamoxifen (OH-Txf). [Read the Full Post]

Physcion, a novel inhibitor of 5α-reductase that promotes hair growth in vitro and in vivo

397 | Mar 02 2021

Zizhao Lao et al. suggested that Physcion was a potent 5α-reductase inhibitor, as well as a new natural medicine for treating AGA. [Read the Full Post]

Prostate Cancer Foundation Hormone-Sensitive Prostate Cancer Biomarker Working Group Meeting Summary

280 | Dec 30 2020

Martin R Hofmann wt al. proposed that there was no high level clinical evidence for treatment selection among these choices based on biological drivers of clinical disease. [Read the Full Post]

Low-Dose Enzalutamide in Late-Elderly Patients (≥ 75 Years Old) Presenting With Metastatic Castration-Resistant Prostate Cancer.

588 | May 19 2020

Vinh-Hung V et al. found that Low-dose enzalutamide in very old, symptomatic, poor-performance patients with metastatic disease was associated with high response rate and survival comparable to standard dose. [Read the Full Post]

Inhibition of the erythropoietin-producing receptor EPHB4 antagonizes androgen receptor overexpression and reduces enzalutamide resistance

0 | May 13 2020

Li C et al. provided critical insight into the mechanism of enzalutamide resistance in PCa, potentially offering a therapeutic avenue for enhancing the efficacy of enzalutamide to better manage this common malignancy. [Read the Full Post]

Investigation of lncRNA H19 in prostate cancer cells and secreted exosomes upon androgen stimulation or androgen receptor blockage

427 | May 06 2020

Ozgur E et al. provided evidence that H19 might be involved in androgen receptor pathway. [Read the Full Post]

Safety and Antitumor Activity of Apalutamide (ARN-509) in Metastatic Castration-Resistant Prostate Cancer With and Without Prior Abiraterone Acetate and Prednisone

355 | Apr 23 2020

Dana E Rathkopf et al. indicated that apalutamide was safe, well tolerated, and demonstrated clinical activity in mCRPC, with 80% of AAP-naïve and 43% of post-AAP patients, remaining on treatment for 6 months or longer. [Read the Full Post]

Blocking c-Met and EGFR reverses acquired resistance of PARP inhibitors in triple-negative breast cancer

377 | Mar 20 2020

Chu YY et al. suggested that combined inhibition of c-MET and EGFR could potentially re-sensitize TNBC to the cytotoxic effects of PARPi. [Read the Full Post]

Inhibition of the erythropoietin-producing receptor EPHB4 antagonizes androgen receptor overexpression and reduces enzalutamide resistance

429 | Mar 20 2020

Li C et al. provided critical insight into the mechanism of enzalutamide resistance in PCa, potentially offering a therapeutic avenue for enhancing the efficacy of enzalutamide to better manage this common malignancy. [Read the Full Post]

Transcriptomics-Guided Personalized Prescription of Targeted Therapeutics for Metastatic ALK-Positive Lung Cancer Case Following Recurrence on ALK Inhibitors

334 | Nov 03 2019

Poddubskaya E et al. showed that transcriptomic-guided sequential personalized prescription of targeted therapies can be effective in terms of survival and quality of life in ALK-mutated NSCLC. [Read the Full Post]

Abiraterone Acetate and Enzalutamide: Similar Efficacy in Treating Post Docetaxel Metastatic Castration-resistant Prostate Cancer: Single Center Experience

389 | Oct 07 2019

Chang LW et al. found that AA and ENZ had a similar efficacy in treating post-docetaxel mCRPC patients. Metastatic volume and nadir PSA were independent risk factors of these patients in predicting their disease-specific survival and overall survival. [Read the Full Post]

Elevating SOX2 in prostate tumor cells upregulates expression of neuroendocrine genes, but does not reduce the inhibitory effects of enzalutamide

363 | Oct 06 2019

Metz EP et al. indicated that NE marker expression can increase independently of the sensitivity to enzalutamide. [Read the Full Post]

A novel antiandrogen, Compound 30, suppresses castration-resistant and MDV3100-resistant prostate cancer growth in vitro and in vivo

466 | Jul 15 2019

Kuruma H et al. provided a preclinical proof-of-principle that Compound 30 could be a promising next generation anti-AR agent, especially in the context of antiandrogen-resistant tumors. [Read the Full Post]

Tamoxifen a pioneering drug: An update on the therapeutic potential of tamoxifen derivatives

768 | May 21 2019

Shagufta et al. anticipated that it will assist medicinal chemists in the synthesis of novel and pharmacologically potent agents for various therapeutic targets. [Read the Full Post]

Functional and Mechanistic Interrogation of BET Bromodomain Degraders for the Treatment of Metastatic Castration Resistant Prostate Cancer

551 | Mar 30 2019

Kregel S et al. identified increases in polyunsaturated fatty acids (PUFAs) and Thioredoxin-interacting protein (TXNIP) as potential pharmacodynamics biomarkers for targeting BET proteins. [Read the Full Post]

Effects of Combination of Estradiol with Selective Progesterone Receptor Modulators (SPRMs) on Human Breast Cancer Cells In Vitro and In Vivo

634 | Mar 27 2019

Nair HB et al. hypothesized that a combination of estradiol (E2) with selective progesterone receptor modulator (SPRM) to exert a safer profile on endometrium will also reduce mammary gland proliferation and could be used to prevent breast cancer when used in MHT. [Read the Full Post]

Ultraviolet A eye irradiation ameliorates colon carcinoma induced by azoxymethane and dextran sodium sulfate through β-endorphin and methionine-enkephalin

0 | Mar 16 2019

Hiramoto K et al. suggested that UVA eye irradiation exerts major effects on AOM + DSS-induced colon carcinoma. [Read the Full Post]

ΔNp63 drives metastasis in breast cancer cells via PI3K/CD44v6 axis

678 | Feb 28 2019

Di Franco S et al. found that tumor microenvironmental cytokines significantly contribute to the establishment of breast cancer cell phenotype by positively regulating ΔNp63 and CD44v6 expression. [Read the Full Post]

Role of connexin 43 in cadmium-induced proliferation of human prostate epithelial cells

491 | Jan 26 2019

Liu Q et al. found that Cx43 might be a target for prostatic diseases associated with Cd exposure. [Read the Full Post]

Ultraviolet A eye irradiation ameliorates colon carcinoma induced by azoxymethane and dextran sodium sulfate through β-endorphin and methionine-enkephalin

1257 | Jan 25 2019

Hiramoto K et al. suggested that UVA eye irradiation exerts major effects on AOM + DSS-induced colon carcinoma. [Read the Full Post]

Long-term treatment of spontaneously hypertensive rats with PD123319 and electrophysiological remodeling of left ventricular myocardium

594 | Jan 20 2019

Ying X et al. showed that long-term treatment with PD123319 worsened the development of myocyte hypertrophy and associated electrophysiological alterations in spontaneously hypertensive rat. [Read the Full Post]

Impacts of ABCB1 (G1199A) polymorphism on resistance, uptake, and efflux to steroid drugs

0 | Jan 13 2019

Peng R et al. showed the ABCB1 (G1199A) polymorphism may affect effective steroids concentration in target cells by regulating the drug transport and distribution. [Read the Full Post]

Cell-based assay system for high-throughput screening of anti-photo-aging agents in fibroblast transfectants

0 | Jan 03 2019

Lee S et al. indicated sclareol attenuated UVB-induced photo-aging by an increase in collagen synthesis and decrease in MMP-1 activity. [Read the Full Post]

Tracking gastrointestinal transit of solids in aged rats as pharmacological models of chronic dysmotility

0 | Dec 28 2018

Dalziel JE et al. demonstrated that loperamide slowed overall transit in aged rats, while prucalopride increased stomach emptying and accelerates colonic transit. [Read the Full Post]

Experimental observation of human bone marrow mesenchymal stem cell transplantation into rabbit intervertebral discs

1373 | Sep 30 2018

Tao H et al. indicated that in the sections of specimens removed at 1, 2, 4, 6 and 8 weeks post-transplantation, no GFP-positive cells were observed in the control groups, whereas GFP-positive cells were apparent in the nucleus pulposus at all periods in the GFP-labeled human BMSCs group, and the cell density at 6 and 8 weeks was significantly less than that at 1, 2 and 4 weeks post-transplantation (P<0.001). [Read the Full Post]

Kaempferol suppresses lipid accumulation by inhibiting early adipogenesis in 3T3-L1 cells and zebrafish

1261 | Sep 16 2018

Lee YJ et al. indicated that kaempferol might have an anti-obesity effect by regulating lipid metabolism. [Read the Full Post]

The Effects of Ultraviolet Eye Irradiation on Dextran Sodium Sulfate-Induced Ulcerative Colitis in Mice

1562 | Sep 15 2018

Hiramoto K et al. suggested that UV eye irradiation plays an important role in DSS-induced ulcerative colitis. [Read the Full Post]

Robust and stimuli-responsive POSS hybrid PDMAEMA hydrogels for controlled drug release

760 | Aug 30 2018

Chen Y, et al. showed that the increased Oa-POSS could improve the drug loading ability, and OP-PD gels showed well controlled-release effect in simulated human stomachic condition. [Read the Full Post]

A simple, fast, label-free colorimetric method for detection of telomerase activity in urine by using hemin-graphene conjugates

1079 | Aug 29 2018

Xu X, et al. found a colorimetric approach affords simplicity, sensitivity and reliability in telomerase activity detection. [Read the Full Post]

Central Agonism of GPR120 Acutely Inhibits Food Intake and Food Reward and Chronically Suppresses Anxiety-Like Behavior in Mice

1006 | Aug 23 2018

Auguste S et al. suggested that GPR120 could mediate the effects of central ω-3 polyunsaturated fatty acids to inhibit appetite. The anxiolytic effect elicited by GPR120 agonist infusions favors the testing of compounds that can enter the brain to activate GPR120 for the mitigation of anxiety. [Read the Full Post]

Acquired CDK6 amplification promotes breast cancer resistance to CDK4/6 inhibitors and loss of ER signaling and dependence

0 | Aug 14 2018

Yang C et al. suggested that the clinical paradigm of sequential endocrine-based therapy may be ineffective in some settings of acquired CDK4/6 resistance. [Read the Full Post]

Inhibition of local estrogen synthesis in the hippocampus impairs hippocampal memory consolidation in ovariectomized female mice

0 | Jun 25 2018

Tuscher JJ et al. examined the role of hippocampal E2 synthesis in hippocampal memory consolidation. Using bilateral dorsal hippocampal infusions of the aromatase inhibitor letrozole, we first found that blockade of dorsal hippocampal E2 synthesis impaired hippocampal memory consolidation. We next found that elevated levels of E2 in the dorsal hippocampus observed 30min after object training were blocked by dorsal hippocampal infusion of letrozole, suggesting that behavioral experience increases acute and local E2 synthesis. Finally, aromatase inhibition did not prevent exogenous E2 from enhancing hippocampal memory consolidation, indicating that hippocampal E2 synthesis is not necessary for exogenous E2 to enhance hippocampal memory. Combined, these data are consistent with the hypothesis that hippocampally-synthesized E2 is necessary for hippocampus-dependent memory consolidation in rodents. [Read the Full Post]

Estrogen promotes the brain metastatic colonization of triple negative breast cancer cells via an astrocyte-mediated paracrine mechanism

969 | Jun 24 2018

Sartorius CA et al. provided a novel mechanism by which estrogens, acting through ER+ astrocytes in the brain microenvironment, can promote BM of TN breast cancers, and suggests existing endocrine agents may provide some clinical benefit towards reducing and managing BM. [Read the Full Post]

Letrozole-induced functional changes in carcinoma-associated fibroblasts and their influence on breast cancer cell biology

1104 | Jun 24 2018

Li K et al. revealed that down-regulation of several secreted factors (CCL2, CCL5, CXCL1 etc.) in CAFs might be partially responsible for the efficacy of letrozole. [Read the Full Post]

Evaluation of cardioprotective effect of aqueous extract of Garcinia indica Linn. fruit rinds on isoprenaline-induced myocardial injury in Wistar albino rats

1545 | Apr 18 2018

Patel KJ et al. found that the aqueous extract of G. indica was not found to be cardioprotective against myocardial injury. [Read the Full Post]

A Novel TGR5 Activator WB403 Promotes GLP-1 Secretion and Preserves Pancreatic β-Cells in Type 2 Diabetic Mice

1278 | Mar 30 2018

Zheng C et al. demonstrated that TGR5 activator WB403 effectively promoted GLP-1 release, improved hyperglycemia and preserved the mass and function of pancreatic β-cells, whereas it did not show a significant side effect on gallbladder. [Read the Full Post]

Relative cytotoxic potencies and cell death mechanisms of α1 -adrenoceptor antagonists in prostate cancer cell lines

0 | Mar 17 2018

Forbes A et al. demonstrated cytotoxic actions on both castration-resistant PC-3 and androgen-sensitive LNCap prostate cancer cells. [Read the Full Post]

The Correlation Between PARP1 and BRCA1 in AR Positive Triple-negative Breast Cancer

738 | Feb 26 2018

Luo J et al. suggested that the combination of bicalutamide and PARP inhibitor may be a potential strategy for TNBC patients and merits further evaluation. [Read the Full Post]

The Correlation Between PARP1 and BRCA1 in AR Positive Triple-negative Breast Cancer

0 | Feb 26 2018

Luo J et al. suggested that the combination of bicalutamide and PARP inhibitor may be a potential strategy for TNBC patients and merits further evaluation. [Read the Full Post]

Role of protein S in castration-resistant prostate cancer-like cells

748 | Feb 25 2018

Ning P et al. suggested that PROS may facilitate cell proliferation and promote castration resistance in human castration-resistant PCa-like cells via its apoptosis-regulating property. Future study emphasizing on delineating how PROS regulate cellular processes controlling transformation during the development of castration resistance should open new doors for the development of novel therapeutic targets for CRPC. [Read the Full Post]

CX4945 suppresses the growth of castration-resistant prostate cancer cells by reducing AR-V7 expression

822 | Feb 25 2018

Deng C et al. presented a potential option for the treatment of prostate cancer, especially CRPC. [Read the Full Post]

Triggering of Suicidal Erythrocyte Death by Exemestane

885 | Feb 20 2018

Exemestane triggers phospholipid scrambling of the erythrocyte cell membrane, an effect paralleled by enhanced [Ca2+]i, oxidative stress, and increased ceramide abundance. [Read the Full Post]

Androgen-Sensitized Apoptosis of HPr-1AR Human Prostate Epithelial Cells

0 | Jan 31 2018

Chen C et al. proposed that the net effect of these AR-mediated expression changes shifts the balance of BCL2-family proteins, such that androgen signaling sensitizes mitochondria to apoptotic signaling, thus rendering HPr-1AR more vulnerable to cell death signals. [Read the Full Post]

Tumor suppressor SPOP mediates the proteasomal degradation of progesterone receptors (PRs) in breast cancer cells

1170 | Sep 20 2017

Gao K et al. revealed novel molecular mechanisms underlying the regulation of PR protein homeostasis in breast cancer cells, and provided insights in understanding the relationship between SPOP inactivation and the development of breast cancer. [Read the Full Post]

New insights into estrogenic regulation of O6-methylguanine DNA-methyltransferase (MGMT) in human breast cancer cells: Co-degradation of ER-α and MGMT proteins by fulvestrant or O6-benzylguanine indicates fresh avenues for therapy

0 | Sep 19 2017

Paranjpe A et al. offered a clear rationale for combining alkylating agents with endocrine therapy. [Read the Full Post]

Koumine enhances spinal cord 3α-hydroxysteroid oxidoreductase expression and activity in a rat model of neuropathic pain

2587 | Sep 19 2017

Qiu HQ et al. demonstrated that 3α-HSOR is an important molecular target of koumine for alleviating neuropathic pain. Koumine may prove a promising compound for the development of novel analgesic agents effective against intractable neuropathic pain. [Read the Full Post]

Acquired CDK6 amplification promotes breast cancer resistance to CDK4/6 inhibitors and loss of ER signaling and dependence

1808 | Aug 02 2017

Yang C et al. suggested that the clinical paradigm of sequential endocrine-based therapy may be ineffective in some settings of acquired CDK4/6 resistance [Read the Full Post]

Src Is a Potential Therapeutic Target in Endocrine-Resistant Breast Cancer Exhibiting Low Estrogen Receptor-Mediated Transactivation

0 | Jul 21 2017

Guest SK et al. suggested that src has differential effects in endocrine-resistant cell lines, particularly in tamoxifen resistant models, with low ER genomic activity, providing further evidence of the importance of patient selection for clinical trials testing dasatinib utility in ER+ breast cancer. [Read the Full Post]

New insights into estrogenic regulation of O6-methylguanine DNA-methyltransferase (MGMT) in human breast cancer cells: Co-degradation of ER-α and MGMT proteins by fulvestrant or O6-benzylguanine indicates fresh avenues for therapy

1125 | Jun 29 2017

Paranjpe A et al. concluded that MGMT and ER-α proteins exist as a complex and are co-targeted for ubiquitin-conjugation and subsequent proteasomal degradation. The findings offer a clear rationale for combining alkylating agents with endocrine therapy. [Read the Full Post]

The gender differences in the inhibitory action of UVB-induced melanocyte activation by the administration of tranexamic acid

0 | Jun 04 2017

Hiramoto K et al. suggested that the suppression by tranexamic acid of the UVB-induced melanocyte activation (UVB sensitivity) is stronger in female mice than in male mice and that female hormones and β-endorphin play an important role in this sex difference. [Read the Full Post]

Regulated expression of the prostacyclin receptor (IP) gene by androgens within the vasculature: Combined role for androgens and serum cholesterol.

1316 | May 26 2017

Eivers SB et al. found that the human IP gene is under the transcriptional regulation of DHT, where this regulation is further influenced by serum-cholesterol levels. [Read the Full Post]

Inhibition of local estrogen synthesis in the hippocampus impairs hippocampal memory consolidation in ovariectomized female mice

1358 | May 20 2017

Tuscher JJ et al. found that hippocampally-synthesized E2 is necessary for hippocampus-dependent memory consolidation in rodents. [Read the Full Post]

The gender differences in the inhibitory action of UVB-induced melanocyte activation by the administration of tranexamic acid

0 | Mar 28 2017

Hiramoto K et al suggested that the suppression by tranexamic acid of the UVB-induced melanocyte activation (UVB sensitivity) is stronger in female mice than in male mice and that female hormones and β-endorphin play an important role in this sex difference. [Read the Full Post]

GRP78 confers the resistance to 5-FU by activating the c-Src/LSF/TS Axis in hepatocellular carcinoma

0 | Mar 10 2017

Gu YJ et al found that GRP78 confers the resistance to 5-FU by up-regulating the c-Src/LSF/TS axis via its ATPase domain [Read the Full Post]

Relative cytotoxic potencies and cell death mechanisms of α1 -adrenoceptor antagonists in prostate cancer cell lines

2570 | Feb 24 2017

Prazosin and doxazosin demonstrated cytotoxic actions on both castration-resistant PC-3 and androgen-sensitive LNCap prostate cancer cells. The mechanisms involved included changes in a number of proliferation and apoptosis regulatory proteins. The role of autophagy depended on the cell type, but contributed to cell death in PC3 cells. [Read the Full Post]

The gender differences in the inhibitory action of UVB-induced melanocyte activation by the administration of tranexamic acid.

3329 | Feb 01 2017

Hiramoto K et al. suggested that the suppression by tranexamic acid of the UVB-induced melanocyte activation (UVB sensitivity) is stronger in female mice than in male mice and that female hormones and β-endorphin play an important role in this sex difference. [Read the Full Post]

Src Is a Potential Therapeutic Target in Endocrine-Resistant Breast Cancer Exhibiting Low Estrogen Receptor-Mediated Transactivation

2694 | Dec 16 2016

Guest SK, et al. suggested that src has differential effects in endocrine-resistant cell lines, particularly in tamoxifen resistant models, with low ER genomic activity, providing further evidence of the importance of patient selection for clinical trials testing dasatinib utility in ER+ breast cancer. [Read the Full Post]

Androgen-Sensitized Apoptosis of HPr-1AR Human Prostate Epithelial Cells

1747 | Nov 13 2016

The study of Chen C et al. offers insight into AR-mediated regulation of prostate epithelial cell death signaling. [Read the Full Post]

Inhibition of local estrogen synthesis in the hippocampus impairs hippocampal memory consolidation in ovariectomized female mice

1848 | Oct 18 2016

Tuscher JJ et al. found that hippocampally-synthesized E2 is necessary for hippocampus-dependent memory consolidation in rodents. [Read the Full Post]

TAK 875 was dissolved in dimethyl sulfoxide

3184 | Feb 12 2014

AK-875 is a selective GPR40 agonist with EC50 of 14 nM, 400-fold more potent than oleic acid. [Read the Full Post]

EPZ005687 is the catalytic subunit of the polycomb repressive complex 2

2837 | Dec 06 2013

EPZ005687 is a potent and selective inhibitor of EZH2 with Ki of 24 nM, 50-fold selectivity against EZH1 and 500-fold selectivity against 15 other protein methyltransferases. [Read the Full Post]

MS275 is a benzamide histone deacetylase inhibitor

3017 | Aug 08 2013

MS-275 shows inhibitory to HDACs by 2'-amino group. MS-275 induces accumulation of p21WAF1/CIP1 and gelsolin in K562 cell. MS-275 could reduce S-phase cells and induce G1-phase cells in A2780 cell. [Read the Full Post]

TOK001 is an experimental drug being developed by Tokai Pharmaceuticals

2721 | Jul 16 2013

Galeterone is effective at preventing binding of [3H]-R1881 to the mutant LNCaP AR (T877A) with IC50 of 845 nM. [Read the Full Post]

RG108 is a cell permeable specific DNA methyltransferase inhibitor

3025 | Jul 05 2013

RG108 effectively blocks DNA methyltransferases in vitro and does not cause covalent enzyme trapping in human cell lines. Incubation of cells with low micromolar concentrations of RG108 results in significant demethylation of genomic DNA without any detectable toxicity. [Read the Full Post]

MDV3100- AN ANTI PROSTATE CANCER AGENT

2507 | Apr 09 2012

ROLE OF ANDROGEN RECEPTORS Androgen receptors (ARs), a type of nuclear receptors that are involved in the regulation of expression of different types of genes that play role in the development and progress of male sexual characteristics. ARs can also be called as receptor subfamily number 3, C group, and member number 4 (NR3C4nuclear). Dihydrotestosterone or testosterone and androgenic hormones function as ligands for these receptors and are in turn translocated into the nucleus, where they directly or indirectly regulate the respective gene expression. Higher quantities of progestin inhibit these receptors. These receptors are known to effect many different types of genes and their expression e.g., AKT1, Cyclin D1, HDAC1, BRCA1, STAT3, SRC kinases and EGFR etc. they all are mostly cell cycle regulating proteins or oncoproteins which are malfunctioning in many different types of cancers. [Read the Full Post]

OSTARINE

4323 | Apr 05 2012

MODULATORS OF ANDROGEN RECEPTORS: Androgenic compounds are famous for their uses in banned drugs for sportsmen but very few people have knowledge to link these compounds for therapeutic purposes. Although androgen receptor modulators have restricted legitimate uses compared to anabolic steroids, many of these are undergoing clinical trials, these Selective androgen receptor modulators (SARMs) proved to be far more specific in their activities as well. The increases in knowledge about these modulators lead to the assessment in preclinical and clinical studies against different diseases. The structural diversity has been increased dramatically due to more application of SARMs for various modifying levels of androgen. The ability of SARMs as therapeutics is reported to enhance by anabolic dissociation and androgenic activities. In elder age the muscle wasting is being cured by using SARMs therefore their uses at a larger scale lead to the better drug design. Receptors of androgen are altered in a pleiotropic way in order to produce promising drugs against ageing, andropause, hypogonadism, muscle wasting, sarcopenia and osteoporosis. Keeping in mind this potential, these SARMs are becoming famous as potent and novel therapeutics. [Read the Full Post]