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Article

β-Glucocerebrosidase Modulators Promote Dimerization of β-Glucocerebrosidase and Reveal an Allosteric Binding Site.

Journal of the American Chemical Society - 9 May 2018

Zheng Jianbin, Chen Long, Skinner Owen S, Ysselstein Daniel, Remis Jonathan, Lansbury Peter, Skerlj Renato, Mrosek Michael, Heunisch Ursula, Krapp Stephan, Charrow Joel, Schwake Michael, Kelleher Neil L, Silverman Richard B, Krainc Dimitri

Abstract excerpt

β-Glucocerebrosidase (GCase) mutations cause Gaucher's disease and are a high risk factor in Parkinson's disease. The implementation of a small molecule modulator is a strategy to restore proper folding and lysosome delivery of degradation-prone mutant GCase. Here, we present a potent quinazoline modulator, JZ-4109, which stabilizes wild-type and N370S mutant GCase and increases GCase abundance in patient-derived...

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Identifiers

PMID: 29676907
DOI: 10.1021/jacs.7b13003
PMCID: PMC6098685

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