Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells

Author:

Foulkes Daniel M.1ORCID,Byrne Dominic P.1,Yeung Wayland2ORCID,Shrestha Safal2ORCID,Bailey Fiona P.1,Ferries Samantha13,Eyers Claire E.13ORCID,Keeshan Karen4ORCID,Wells Carrow5ORCID,Drewry David H.5ORCID,Zuercher William J.56ORCID,Kannan Natarajan2,Eyers Patrick A.1ORCID

Affiliation:

1. Department of Biochemistry, Institute of Integrative Biology, University of Liverpool, Liverpool L69 7ZB, UK.

2. Institute of Bioinformatics and Department of Biochemistry and Molecular Biology, University of Georgia, Athens, GA 30602, USA.

3. Centre for Proteome Research, Institute of Integrative Biology, University of Liverpool, Liverpool L69 7ZB, UK.

4. Paul O’Gorman Leukaemia Research Centre, Institute of Cancer Sciences, University of Glasgow, Scotland, UK.

5. Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.

6. Lineberger Comprehensive Cancer Center, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.

Abstract

Covalent EGFR family inhibitors bind to and induce the degradation of the pseudokinase TRIB2 to kill cancer cells.

Funder

North West Cancer Research Fund

BBSRC

Publisher

American Association for the Advancement of Science (AAAS)

Subject

Cell Biology,Molecular Biology,Biochemistry

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