4yvp | pdb_00004yvp

Crystal Structure of AKR1C1 complexed with glibenclamide

spinqualitylabelsall models 4yvp, resolution 2.60Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 4yvp is a 2 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: GBM, NAP Related: 4yvv, 4yvx Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum Function [AK1C1_HUMAN] Converts progesterone to its inactive form, 20-alpha-dihydroxyprogesterone (20-alpha-OHP). In the liver and intestine, may have a role in the transport of bile. May have a role in monitoring the intrahepatic bile acid concentration. Has a low bile-binding ability. May play a role in myelin formation. Publication Abstract from PubMed Recent 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 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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