6sbv

X-ray Structure of Human LDH-A with an Allosteric Inhibitor (Compound 7)

spinqualitylabelsall models 6sbv, resolution 2.60Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 6sbv is a 8 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 2.6Å Ligands: L5K Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Disease LDHA_HUMAN Defects in LDHA are the cause of glycogen storage disease type 11 (GSD11) [MIM:612933. A metabolic disorder that results in exertional myoglobinuria, pain, cramps and easy fatigue. Function LDHA_HUMAN Publication Abstract from PubMed Lactate dehydrogenase A (LDHA) is frequently overexpressed in tumors, thereby sustaining high glycolysis rates, tumor growth, and chemoresistance. High-throughput screening resulted in the identification of phthalimide and dibenzofuran derivatives as novel lactate dehydrogenase inhibitors, selectively inhibiting the activity of the LDHA isoenzyme. Cocrystallization experiments confirmed target engagement in addition to demonstrating binding to a novel allosteric binding site present in all four LDHA subunits of the LDH5 homotetramer. Structural Evidence for Isoform-Selective Allosteric Inhibition of Lactate Dehydrogenase A.,Friberg A, Rehwinkel H, Nguyen D, Putter V, Quanz M, Weiske J, Eberspacher U, Heisler I, Langer G ACS Omega. 2020 May 27;5(22):13034-13041. doi: 10.1021/acsomega.0c00715., eCollection 2020 Jun 9. PMID:32548488 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Lactate dehydrogenase 3D structures

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