A high affinity pan-PI3K binding module supports selective targeted protein degradation of PI3Kα-Reference-Cited by-同舟云学术

A high affinity pan-PI3K binding module supports selective targeted protein degradation of PI3Kα

Published:2024 Issue:2 Volume:15 Page:683-691
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Jauslin Werner Theodor¹^ORCID,Schild Matthias¹^ORCID,Schaefer Thorsten²^ORCID,Borsari Chiara²^ORCID,Orbegozo Clara²,Bissegger Lukas²^ORCID,Zhanybekova Saule¹,Ritz Danilo³,Schmidt Alexander³,Wymann Matthias²^ORCID,Gillingham Dennis¹^ORCID

Affiliation:

1. Department of Chemistry, University of Basel, 4056 Basel, Switzerland

2. Department of Biomedicine, University of Basel, 4031 Basel, Switzerland

3. Proteomics Core Facility, Biozentrum, University of Basel, 4056 Basel, Switzerland

Abstract

Bifunctional degraders built from unselective inhibitors of the phosphoinositide 3-kinase (PI3K) family can support selective degradation of specific isoforms, such as the frequently mutated oncoprotein PI3Kα.

Funder

Schweizerischer Nationalfonds zur Förderung der Wissenschaftlichen Forschung

H2020 European Research Council

Krebsliga Schweiz

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2024/SC/D3SC04629J

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1. A multidisciplinary approach to optimizing care of patients treated with alpelisib