title: Androgen-metabolizing enzymes: A structural perspective.
abstract: 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.
authors.affiliation: Département de Biochimie, de Microbiologie et de Bio-informatique, PROTEO, Université Laval, Québec City, QC G1V 0A6, Canada; Institut de Biologie Intégrative et des Systèmes (IBIS), Université Laval, Pavillon Charles-Eugène-Marchand, Québec City, QC G1V 0A6, Canada.
authors.forename: Mahder Seifu
authors.initials: MS
authors.lastname: Manenda
authors.affiliation: Département de Biochimie, de Microbiologie et de Bio-informatique, PROTEO, Université Laval, Québec City, QC G1V 0A6, Canada; Institut de Biologie Intégrative et des Systèmes (IBIS), Université Laval, Pavillon Charles-Eugène-Marchand, Québec City, QC G1V 0A6, Canada.
authors.forename: Charles Jérémie
authors.initials: CJ
authors.lastname: Hamel
authors.affiliation: Département de Biochimie, de Microbiologie et de Bio-informatique, PROTEO, Université Laval, Québec City, QC G1V 0A6, Canada; Institut de Biologie Intégrative et des Systèmes (IBIS), Université Laval, Pavillon Charles-Eugène-Marchand, Québec City, QC G1V 0A6, Canada.
authors.forename: Loreleï
authors.initials: L
authors.lastname: Masselot-Joubert
authors.affiliation: Département de Biochimie, de Microbiologie et de Bio-informatique, PROTEO, Université Laval, Québec City, QC G1V 0A6, Canada; Institut de Biologie Intégrative et des Systèmes (IBIS), Université Laval, Pavillon Charles-Eugène-Marchand, Québec City, QC G1V 0A6, Canada.
authors.forename: Marie-Ève
authors.initials: MÈ
authors.lastname: Picard
authors.affiliation: Département de Biochimie, de Microbiologie et de Bio-informatique, PROTEO, Université Laval, Québec City, QC G1V 0A6, Canada; Institut de Biologie Intégrative et des Systèmes (IBIS), Université Laval, Pavillon Charles-Eugène-Marchand, Québec City, QC G1V 0A6, Canada. Electronic address: rong.shi@bcm.ulaval.ca.
authors.forename: Rong
authors.initials: R
authors.lastname: Shi
mesh_terms: D015067:17-Hydroxysteroid Dehydrogenases / Q000737:chemistry / Q000378:metabolism*; D015096:3-Hydroxysteroid Dehydrogenases / Q000737:chemistry / Q000378:metabolism*; D000728:Androgens / Q000737:chemistry / Q000378:metabolism*; D000818:Animals; D003577:Cytochrome P-450 Enzyme System / Q000737:chemistry / Q000378:metabolism*; D006801:Humans; D053858:Metabolic Networks and Pathways; D008958:Models, Molecular; D010088:Oxidoreductases / Q000737:chemistry / Q000378:metabolism*
chemical_list: D000728:Androgens; D003577:Cytochrome P-450 Enzyme System; D010088:Oxidoreductases; D015067:17-Hydroxysteroid Dehydrogenases; D015096:3-Hydroxysteroid Dehydrogenases; C021936:3-oxo-5 beta-steroid delta 4-dehydrogenase
keywords: AKRs; Androgen; Aromatase; Inhibitors; P450s; PDB; Structure