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ESKM, a novel therapeutic agent for sensitive and resistant PH+ leukemias

The mechanism of resistance to JAK2 inhibitor in myeloproliferative neoplasms patients

Effects of PARP inhibitors in BRCA gene-mutated ovarian cancer

DASATINIB; An inhibitor of Receptor Tyrosine Kinase

GP130/JAK/STAT3 signaling pathway induces multiple myeloma

P-gp

MDR1 Inhibition Reverses Doxorubicin-Resistance in Six Doxorubicin-Resistant Canine Prostate and Bladder Cancer Cell Lines

192 views | Jul 13 2023

This study generated doxorubicin-resistant sublines of canine prostate adenocarcinoma and urothelial cell carcinoma cell lines, identifying drug efflux via MDR1 overexpression as a common mechanism, and suggesting the use of MDR1 inhibitors and combination therapies to address acquired chemoresistance. [Read the Full Post]

Novel hybrids of sclareol and 1,2,4-triazolo[1,5-a]pyrimidine show collateral sensitivity in multidrug-resistant glioblastoma cells

186 views | Jul 13 2023

This study describes the synthesis and evaluation of hybrid molecules combining sclareol and synthetic 1,2,4-triazolo[1,5-a]pyrimidines, resulting in compounds with improved cytotoxic properties, selectivity towards glioblastoma cells, and evasion of multidrug resistance. [Read the Full Post]

Characterization of Potent ABCG2 Inhibitor Derived from Chromone: From the Mechanism of Inhibition to Human Extracellular Vesicles for Drug Delivery

150 views | Jun 27 2023

This study characterizes a potent ABCG2 inhibitor, C4a, and demonstrates its selectivity and efficacy in inhibiting ABCG2-mediated drug efflux, utilizing liposomes and extracellular vesicles for improved delivery and highlighting the potential of plasma circulating EVs as a drug delivery system for hydrophobic drugs targeting membrane proteins. [Read the Full Post]

Synthesis and Preclinical Positron Emission Tomography Imaging of the p38 MAPK Inhibitor [11C]Talmapimod: Effects of Drug Efflux and Sex Differences

185 views | Jun 27 2023

The development of the first positron emission tomography (PET) radiotracer for imaging MAPK p38α/β, synthesized through radiolabeling the inhibitor talmapimod with carbon-11, showed promising results but faced challenges regarding its non-displaceable binding and P-gp efflux. [Read the Full Post]

Renal tubular epithelial cells treated with calcium oxalate up-regulate S100A8 and S100A9 expression in M1-polarized macrophages via interleukin 6

163 views | May 23 2023

This study demonstrates that M1-polarized macrophages are the main source of S100A8 and S100A9 in the kidneys of nephrolithiasis patients, and that COM-induced IL6 secretion from renal tubular epithelial cells can up-regulate their expression in macrophages. [Read the Full Post]

The study of Raddeanin A cerebrovascular endothelial cell trafficking through P-glycoprotein

194 views | Feb 22 2023

Raddeanin A, a natural triterpenoid, is transported through the brain-blood barrier by P-glycoprotein and its transport is affected by its expression and function, providing important guidance on its pharmacodynamic effect in human brains. [Read the Full Post]

Combinational Inhibition of P-Glycoprotein-Mediated Etoposide Transport by Zosuquidar and Polysorbate 20

190 views | Feb 22 2023

The study found that while combination of zosuquidar and polysorbate 20 showed additive P-gp inhibition in vitro, oral etoposide bioavailability decreased when co-administered with both agents in vivo due to high level of nonspecific zosuquidar adsorption. [Read the Full Post]

P-Glycoprotein (ABCB1/MDR1) and BCRP (ABCG2) Limit Brain Accumulation and Cytochrome P450-3A (CYP3A) Restricts Oral Exposure of the RET Inhibitor Selpercatinib (RETEVMO)

233 views | Feb 28 2022

Yaogeng Wang et al. thought that CYP3A-mediated metabolism could limit selpercatinib oral exposure and hence its tissue concentrations. [Read the Full Post]

Acyclovir Brain Disposition: Interactions with P-gp, Bcrp, Mrp2, and Oat3 at the Blood-Brain Barrier

350 views | Feb 27 2022

Yuheng Shan et al. demonstrated that P-gp, Bcrp, Mrp2, and Oat3 inhibition increased the penetration of acyclovir across the BBB, supporting the hypothesis that these efflux pumps restrict the distribution of acyclovir in the brain. [Read the Full Post]

PET imaging to assess the impact of P-glycoprotein on pulmonary drug delivery in rats

333 views | Jan 24 2022

Irene Hernández-Lozano et al. found that P-gp could affect the pulmonary disposition of inhaled P-gp substrates. [Read the Full Post]