BRAF inhibitors promote intermediate BRAF(V600E) conformations and binary interactions with activated RAS-Reference-Cited by-同舟云学术

BRAF inhibitors promote intermediate BRAF(V600E) conformations and binary interactions with activated RAS

Published:2019-08-02 Issue:8 Volume:5 Page:
ISSN:2375-2548
Container-title:Science Advances
language:en
Short-container-title:Sci. Adv.

Author:

Röck Ruth¹^ORCID,Mayrhofer Johanna E.¹^ORCID,Torres-Quesada Omar¹^ORCID,Enzler Florian¹^ORCID,Raffeiner Andrea¹,Raffeiner Philipp¹,Feichtner Andreas¹^ORCID,Huber Roland G.²^ORCID,Koide Shohei³^ORCID,Taylor Susan S.⁴^ORCID,Troppmair Jakob⁵^ORCID,Stefan Eduard¹^ORCID

Affiliation:

1. Institute of Biochemistry and Center for Molecular Biosciences, University of Innsbruck, Innrain 80/82, 6020 Innsbruck, Austria.

2. Bioinformatics Institute (BII), Agency for Science Technology and Research (A*STAR), Singapore 138671, Singapore.

3. Department of Biochemistry and Molecular Pharmacology, New York University School of Medicine and Laura and Isaac Perlmutter Cancer Center, New York University Langone Medical Center, New York, NY 10016, USA.

4. Department of Pharmacology, Department of Chemistry and Biochemistry, and Howard Hughes Medical Institute, University of California, San Diego, San Diego, CA 92093, USA.

5. Daniel Swarovski Research Laboratory, Department of Visceral, Transplant and Thoracic Surgery, Innsbruck Medical University, Innrain 66, 6020 Innsbruck, Austria.

Abstract

Patient mutation–specific BRAF inhibitors alter full-length kinase conformations and promote interactions with GTP-loaded RAS.

Funder

National Institutes of Health

Austrian Science Fund

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Multidisciplinary

Reference53 articles.

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2. Mutations of the BRAF gene in human cancer