Slow-, Tight-Binding Inhibition of CYP17A1 by Abiraterone Redefines Its Kinetic Selectivity and Dosing Regimen

Substantial evidence underscores the clinical efficacy of inhibiting CYP17A1-mediated androgen biosynthesis by abiraterone for treatment of prostate oncology. Previous structural analysis and in vitro assays revealed inconsistencies surrounding the nature and potency of CYP17A1 inhibition by abirate...

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Vydáno v:J Pharmacol Exp Ther
Hlavní autoři: Cheong, Eleanor Jing Yi, Nair, Pramod C., Neo, Rebecca Wan Yi, Tu, Ho Thanh, Lin, Fu, Chiong, Edmund, Esuvaranathan, Kesavan, Fan, Hao, Szmulewitz, Russell Z., Peer, Cody J., Figg, William D., Chai, Christina Li Lin, Miners, John O., Chan, Eric Chun Yong
Médium: Artigo
Jazyk:Inglês
Vydáno: The American Society for Pharmacology and Experimental Therapeutics 2020
Témata:
Drug Discovery and Translational Medicine
On-line přístup:https://ncbi.nlm.nih.gov/pmc/articles/PMC7469252/
https://ncbi.nlm.nih.gov/pubmed/32554434
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1124/jpet.120.265868
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