Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1).

doi:10.1021/acs.jmedchem.7b01186

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Article

Design of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors Using a Crystallographic Surrogate Derived from Checkpoint Kinase 1 (CHK1).

Journal of medicinal chemistry - 9 Nov 2017

Williamson Douglas S, Smith Garrick P, Acheson-Dossang Pamela, Bedford Simon T, Chell Victoria, Chen I-Jen, Daechsel Justus C A, Daniels Zoe, David Laurent, Dokurno Pawel, Hentzer Morten, Herzig Martin C, Hubbard Roderick E, Moore Jonathan D, Murray James B, Newland Samantha, Ray Stuart C, Shaw Terry, Surgenor Allan E, Terry Lindsey, Thirstrup Kenneth, Wang Yikang, Christensen Kenneth V

Abstract excerpt

Mutations in leucine-rich repeat kinase 2 (LRRK2), such as G2019S, are associated with an increased risk of developing Parkinson's disease. Surrogates for the LRRK2 kinase domain based on checkpoint kinase 1 (CHK1) mutants were designed, expressed in insect cells infected with baculovirus, purified, and crystallized. X-ray structures of the surrogates complexed with known LRRK2 inhibitors rationalized compound...

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PMID: 29023112
DOI: 10.1021/acs.jmedchem.7b01186

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026. Manifest publication-graph-cohort-2026-09-06.1.

Source receipt: pubmed, retrieved 6 Sept 2026.

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