4yvv
From Proteopedia
Crystal structure of AKR1C3 complexed with glibenclamide
Structural highlights
FunctionAK1C3_HUMAN Catalyzes the conversion of aldehydes and ketones to alcohols. Catalyzes the reduction of prostaglandin (PG) D2, PGH2 and phenanthrenequinone (PQ) and the oxidation of 9-alpha,11-beta-PGF2 to PGD2. Functions as a bi-directional 3-alpha-, 17-beta- and 20-alpha HSD. Can interconvert active androgens, estrogens and progestins with their cognate inactive metabolites. Preferentially transforms androstenedione (4-dione) to testosterone. Publication Abstract from PubMedRecent epidemiological studies show conflicting data for the first-line anti-diabetic sulphonylureas drugs in treating cancer progression in type II diabetes patients. How sulphonylureas promote or diminish tumor growth is not fully understood. Here, we report that seven sulphonylureas exhibit different in vitro inhibition towards AKR1Cs (AKR1C1, AKR1C2, AKR1C3), which are critical steroid hormone metabolism enzymes that are related to prostate cancer, breast cancer and endometrial diseases. Interactions of the sulphonylureas and AKR1Cs were analyzed by X-ray crystallography. In vitro inhibition of AKR1Cs by sulphonylureas and the structural basis.,Zhao Y, Zheng X, Zhang H, Zhai J, Zhang L, Li C, Zeng K, Chen Y, Li Q, Hu X Chem Biol Interact. 2015 Oct 5;240:310-5. doi: 10.1016/j.cbi.2015.09.006. Epub, 2015 Sep 8. PMID:26362498[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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Categories: Homo sapiens | Large Structures | Hu X | Zhang H | Zhao Y | Zheng X
