Category

Archives

Transferase

Inhibition of Diacylglycerol Acyltransferase 2 Versus Diacylglycerol Acyltransferase 1: Potential Therapeutic Implications of Pharmacology

182 views | Nov 26 2023

DGAT2 inhibitors, exemplified by ervogastat, offer a promising and well-tolerated therapeutic approach for patients with nonalcoholic fatty liver disease (NAFLD), nonalcoholic steatohepatitis (NASH), and NASH with liver fibrosis, in contrast to limited efficacy and adverse effects associated with DGAT1 inhibitors. [Read the Full Post]

Targeting GSTP1 as Therapeutic Strategy against Lung Adenocarcinoma Stemness and Resistance to Tyrosine Kinase Inhibitors

292 views | Nov 07 2023

The study reveals that upregulation of Glutathione S-transferase pi (GSTP1) in lung adenocarcinoma (LUAD) supports cancer stem cells, tumor self-renewal, metastasis, and resistance to targeted therapies, making it a promising therapeutic target for long-term control of LUAD. [Read the Full Post]

Tumor-Suppressive Effect of Metformin via the Regulation of M2 Macrophages and Myeloid-Derived Suppressor Cells in the Tumor Microenvironment of Colorectal Cancer

190 views | Oct 17 2023

Metformin inhibits the populations of myeloid-derived suppressor cells (MDSCs) and M2 macrophages in the tumor microenvironment of colon cancers through AMPK activation, mTOR inhibition, and downregulation of the mevalonate pathway. [Read the Full Post]

Construction and Validation of Protein Expression-related Prognostic Models in Clear Cell Renal Cell Carcinoma

321 views | Oct 10 2023

The study developed a prognostic evaluation model for ccRCC patients using bioinformatics methods, identified 13 independent prognostic proteins, and demonstrated their strong predictive ability for patient survival, while also identifying potential drugs for targeted therapy. [Read the Full Post]

Bioassay-Guided Isolation of Anthelmintic Components from Semen pharbitidis, and the Mechanism of Action of Pharbitin

71 views | Oct 07 2023

This study identified the anthelmintic compound pharbitin from Semen pharbitidis and revealed that its target in Caenorhabditis elegans is likely UNC-63, supporting the traditional use of Semen pharbitidis for treating intestinal parasites. [Read the Full Post]

Design of OSMI-4 Analogs Using Scaffold Hopping: Investigating the Importance of the Uridine Mimic in the Binding of OGT Inhibitors

203 views | Sep 29 2023

This study introduces a modified peptide part of OSMI-4 and incorporates new sulfonamide UDP mimics to design and evaluate a small library of OSMI-4 derivatives, providing insights into the OGT binding pocket and its specificity towards quinolone-4-carboxamides. [Read the Full Post]

ZBTB7C m6A modification incurred by METTL3 aberration promotes osteosarcoma progression

108 views | Sep 25 2023

The study reveals that elevated METTL3 and increased m6A modification, particularly on ZBTB7C mRNA, play a crucial role in promoting osteosarcoma progression, suggesting that targeting the METTL3/ZBTB7C axis could be a potential therapeutic strategy. [Read the Full Post]

Synergistic apoptosis by combination of metformin and an O-GlcNAcylation inhibitor in colon cancer cells

105 views | Sep 24 2023

The combinatorial treatment of metformin and OSMI-1 synergistically induced apoptosis in colon cancer cells by enhancing ER stress-induced signaling and disrupting autophagy, as evidenced by in vitro and xenograft tumor experiments. [Read the Full Post]

Proteasome Inhibition Sensitizes Liposarcoma to MDM2 Inhibition with Nutlin-3 by Activating the ATF4/CHOP Stress Response Pathway

259 views | Jul 03 2023

The study suggests that combining MDM2 inhibitors with proteasome inhibitors could improve the efficacy of treatment for liposarcoma by inducing apoptosis through activation of the ATF4/CHOP stress response axis. [Read the Full Post]

Lonafarnib improves cardiovascular function and survival in a mouse model of Hutchinson-Gilford progeria syndrome

221 views | Apr 06 2023

This study reports the positive effects of lonafarnib on cardiovascular structure, properties, and function in a mouse model of progeria, leading to 100% survival of treated mice and improved arterial structure and function, while rapamycin did not improve outcomes. [Read the Full Post]