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Start Over Author "Ross L. Stein" Publisher american chemical society
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1. Kinetic mechanistic studies of wild-type leucine-rich repeat kinase2: characterization of the kinase and GTPase activities

Author

Min Liu, Brittany Dobson, Marcie A. Glicksman, Zhenyu Yue, and Ross L. Stein

Subjects
Catalysis -- Analysis, Enzyme inhibitors -- Structure, Enzyme inhibitors -- Chemical properties, Leucine -- Chemical properties, Phosphorylation -- Analysis, Phosphotransferases -- Chemical properties, Phosphotransferases -- Structure, Biological sciences, Chemistry
Abstract

The leucine-rich repeat kinase2 gene (LRRK2) protein purified from murine brain was used to characterize the kinetic mechanisms for the LRRK2-catalyzed phosphorylation of two peptide substrates, PLK-derived peptide and LRRKtide. The study identified compound LDN-73794 through screen of LRRK2 kinase inhibitors is found be a competitive inhibitor of the binding of ATP and inhibits the kinase activity without affecting the GTPase activity.

Published
2010

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