LRRK2 dynamics analysis identifies allosteric control of the crosstalk between its catalytic domains.


Journal

PLoS biology
ISSN: 1545-7885
Titre abrégé: PLoS Biol
Pays: United States
ID NLM: 101183755

Informations de publication

Date de publication:
02 2022
Historique:
received: 11 09 2021
accepted: 14 01 2022
entrez: 22 2 2022
pubmed: 23 2 2022
medline: 22 3 2022
Statut: epublish

Résumé

The 2 major molecular switches in biology, kinases and GTPases, are both contained in the Parkinson disease-related leucine-rich repeat kinase 2 (LRRK2). Using hydrogen-deuterium exchange mass spectrometry (HDX-MS) and molecular dynamics (MD) simulations, we generated a comprehensive dynamic allosteric portrait of the C-terminal domains of LRRK2 (LRRK2RCKW). We identified 2 helices that shield the kinase domain and regulate LRRK2 conformation and function. One helix in COR-B (COR-B Helix) tethers the COR-B domain to the αC helix of the kinase domain and faces its activation loop, while the C-terminal helix (Ct-Helix) extends from the WD40 domain and interacts with both kinase lobes. The Ct-Helix and the N-terminus of the COR-B Helix create a "cap" that regulates the N-lobe of the kinase domain. Our analyses reveal allosteric sites for pharmacological intervention and confirm the kinase domain as the central hub for conformational control.

Identifiants

pubmed: 35192607
doi: 10.1371/journal.pbio.3001427
pii: PBIOLOGY-D-21-02428
pmc: PMC8863276
doi:

Substances chimiques

Leucine-Rich Repeat Serine-Threonine Protein Kinase-2 EC 2.7.11.1

Types de publication

Journal Article Research Support, N.I.H., Extramural Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

e3001427

Déclaration de conflit d'intérêts

The authors have declared that no competing interests exist.

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Auteurs

Jui-Hung Weng (JH)

Department of Pharmacology, University of California, San Diego, California, United States of America.

Phillip C Aoto (PC)

Department of Pharmacology, University of California, San Diego, California, United States of America.

Robin Lorenz (R)

Department of Biochemistry, University of Kassel, Kassel, Germany.

Jian Wu (J)

Department of Pharmacology, University of California, San Diego, California, United States of America.

Sven H Schmidt (SH)

Department of Biochemistry, University of Kassel, Kassel, Germany.

Jascha T Manschwetus (JT)

Department of Biochemistry, University of Kassel, Kassel, Germany.

Pallavi Kaila-Sharma (P)

Department of Pharmacology, University of California, San Diego, California, United States of America.

Steve Silletti (S)

Department of Chemistry and Biochemistry, University of California, San Diego, California, United States of America.

Sebastian Mathea (S)

Institute for Pharmaceutical Chemistry, Goethe University Frankfurt, Frankfurt am Main, Germany.

Deep Chatterjee (D)

Institute for Pharmaceutical Chemistry, Goethe University Frankfurt, Frankfurt am Main, Germany.

Stefan Knapp (S)

Institute for Pharmaceutical Chemistry, Goethe University Frankfurt, Frankfurt am Main, Germany.

Friedrich W Herberg (FW)

Department of Biochemistry, University of Kassel, Kassel, Germany.

Susan S Taylor (SS)

Department of Pharmacology, University of California, San Diego, California, United States of America.

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Classifications MeSH