Title : Mechanism of the Dual Activities of Human CYP17A1 and Binding to Anti-Prostate Cancer Drug Abiraterone Revealed by a Novel V366M Mutation Causing 17,20 Lyase Deficiency.

Pub. Date : 2018 Apr 29

PMID : 29710837






4 Functional Relationships(s)
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1 Mechanism of the Dual Activities of Human CYP17A1 and Binding to Anti-Prostate Cancer Drug Abiraterone Revealed by a Novel V366M Mutation Causing 17,20 Lyase Deficiency. abiraterone cytochrome P450 family 17 subfamily A member 1 Homo sapiens
2 The CYP17A1 gene regulates sex steroid biosynthesis in humans through 17α-hydroxylase/17,20 lyase activities and is a target of anti-prostate cancer drug abiraterone. abiraterone cytochrome P450 family 17 subfamily A member 1 Homo sapiens
3 Abiraterone could not bind and inhibit the 17α-hydroxylase activity of the CYP17A1-V366M mutant. abiraterone cytochrome P450 family 17 subfamily A member 1 Homo sapiens
4 The V366M mutant also explained the effectiveness of the anti-prostate cancer drug abiraterone as a potent inhibitor of CYP17A1 by binding tightly at the active site in the WT enzyme. abiraterone cytochrome P450 family 17 subfamily A member 1 Homo sapiens