کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1991243 | 1540987 | 2016 | 19 صفحه PDF | دانلود رایگان |
• Known structures of androgen metabolizing enzymes are reviewed.
• Structural analysis of enzyme-ligand complexes are included.
• Structural insights used in inhibitor design are discussed.
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.
Journal: The Journal of Steroid Biochemistry and Molecular Biology - Volume 161, July 2016, Pages 54–72