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8FW6

Human Lactate Dehydrogenase A in Complex with Inhibitor CHK-336

Summary for 8FW6
Entry DOI10.2210/pdb8fw6/pdb
DescriptorL-lactate dehydrogenase A chain, 1,4-DIHYDRONICOTINAMIDE ADENINE DINUCLEOTIDE, (2P)-2-{5-(cyclopropylmethyl)-3-(4-fluorophenyl)-4-[(3-fluoro-4-sulfamoylphenyl)methyl]-1H-pyrazol-1-yl}-1,3-thiazole-4-carboxylic acid, ... (6 entities in total)
Functional Keywordsldha hldha human lactate dehydrogenase a, oxidoreductase
Biological sourceHomo sapiens (human)
Total number of polymer chains2
Total formula weight78680.38
Authors
Lowther, W.T.,Gumpena, R. (deposition date: 2023-01-20, release date: 2024-01-24, Last modification date: 2025-09-17)
Primary citationCox, J.H.,Boily, M.O.,Caron, A.,Sheng, T.,Wu, J.,Ding, J.,Gaudreault, S.,Chong, O.,Surendradoss, J.,Gomez, R.,Lester, J.,Dumais, V.,Li, X.,Gumpena, R.,Hall, M.D.,Waterson, A.G.,Stott, G.,Flint, A.J.,Moore, W.J.,Lowther, W.T.,Knight, J.,Percival, M.D.,Tong, V.,Oballa, R.,Powell, D.A.,King, A.J.
Characterization of CHK-336, A First-in-Class, Liver-Targeted, Small-Molecule Lactate Dehydrogenase Inhibitor for Hyperoxaluria Treatment.
J Am Soc Nephrol, 36:1535-1547, 2025
Cited by
PubMed Abstract: Primary hyperoxalurias are genetic diseases defined by elevated hepatic oxalate production and higher incidence of kidney stones. Lactate dehydrogenase A catalyzes the final and committed step in hepatic oxalate synthesis and represents a potential therapeutic target for primary hyperoxalurias. CHK-336 is a liver-targeted, small-molecule lactate dehydrogenase A inhibitor with potential to treat diseases associated with elevated oxalate production.
PubMed: 40193200
DOI: 10.1681/ASN.0000000690
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.34 Å)
Structure validation

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