Androgen-metabolizing enzymes: A structural perspective

被引：6

作者：

Manenda, Mander Seifu ^{[1
,2
]}

Hamel, Charles Jeremie ^{[1
,2
]}

Masselot--Joubert, Lorelei ^{[1
,2
]}

Picard, Marie-Eve ^{[1
,2
]}

Shi, Rong ^{[1
,2
]}

机构：

[1] Univ Laval, PROTEO, Dept Biochim Microbiol & Bioinformat, Quebec City, PQ G1V 0A6, Canada

[2] Univ Laval, IBIS, Pavillon Charles Eugene Marchand, Quebec City, PQ G1V 0A6, Canada

来源：

JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY | 2016年 / 161卷

基金：

加拿大自然科学与工程研究理事会;

关键词：

Androgen; PDB; Structure; Inhibitors; Aromatase; P450s; AKRs; SIDE-CHAIN CLEAVAGE; HUMAN AROMATASE CYTOCHROME-P-450; COMPOUND HETEROZYGOUS MUTATIONS; STEROID 5-BETA-REDUCTASE AKR1D1; CRYSTAL-STRUCTURE; 5; 17-BETA-HYDROXYSTEROID-DEHYDROGENASE; MOLECULAR-BIOLOGY; F-SYNTHASE; ADRENAL INSUFFICIENCY; SELECTIVE INHIBITORS;

D O I：

10.1016/j.jsbmb.2016.02.021

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Androgen-metabolizing enzymes convert cholesterol, a relatively inert molecule, into some of the most potent chemical messengers in vertebrates. This conversion involves thermodynamically challenging reactions catalyzed by P450 enzymes and redox reactions catalyzed by Aldo-Keto Reductases (AKRs). This review covers the structures of these enzymes with a focus on active site interactions and proposed mechanisms. Due to their role in a number of diseases, particularly in cancer, androgen-metabolizing enzymes have been targets of drug design. Hence we will also highlight how existing knowledge of structure is being used to this end. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：54 / 72

页数：19

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