Novel Starting Points for Human Glycolate Oxidase Inhibitors, Revealed by Crystallography-Based Fragment Screening

Novel Starting Points for Human Glycolate Oxidase Inhibitors, Revealed by Crystallography-Based Fragment Screening

Primary hyperoxaluria type I (PH1) is caused by AGXT gene mutations that decrease the functional activity of alanine:glyoxylate aminotransferase. A build-up of the enzyme’s substrate, glyoxylate, results in excessive deposition of calcium oxalate crystals in the renal tract, leading to debilitating...

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Bibliographic Details
Main Authors: Sabrina R. Mackinnon, Gustavo A. Bezerra, Tobias Krojer, Tamas Szommer, Frank von Delft, Paul E. Brennan, Wyatt W. Yue
Format: Article
Language:English
Published: Frontiers Media S.A. 2022-05-01
Series:Frontiers in Chemistry
Subjects:
glycolate oxidase
glyoxylate metabolism
primary hyperoxaluria
fragment-based drug discovery
substrate reduction therapy
Online Access:https://www.frontiersin.org/articles/10.3389/fchem.2022.844598/full

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https://www.frontiersin.org/articles/10.3389/fchem.2022.844598/full

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