UCL Discovery
UCL home » Library Services » Electronic resources » UCL Discovery

Precision Targeting of Mutant PI3Kα in Cancer by Selective Degradation

Vanhaesebroeck, Bart; Burke, John E; Madsen, Ralitsa R; (2022) Precision Targeting of Mutant PI3Kα in Cancer by Selective Degradation. Cancer Discovery , 12 (1) pp. 20-22. 10.1158/2159-8290.CD-21-1411.

[thumbnail of Vanhaesebroeck_Cancer Discovery_mutant PI3Ka degraders_Nov 15_QC.pdf] Text
Vanhaesebroeck_Cancer Discovery_mutant PI3Ka degraders_Nov 15_QC.pdf
Access restricted to UCL open access staff until 13 January 2023.

Download (324kB)

Abstract

PIK3CA, which encodes the p110α catalytic subunit of PI3Kα, is one of the most frequently genetically activated kinases in solid tumors. In this issue of Cancer Discovery, Song and colleagues report that the related PI3Kα inhibitors taselisib and inavolisib trigger receptor tyrosine kinase (RTK)-dependent degradation of the mutant p110α protein in breast cancer cells that are positive for HER2 RTK, limiting feedback-mediated drug resistance and potentially widening the therapeutic index of PI3Kα inhibition.See related article by Song et al., p. 204.

Type: Article
Title: Precision Targeting of Mutant PI3Kα in Cancer by Selective Degradation
Location: United States
DOI: 10.1158/2159-8290.CD-21-1411
Publisher version: https://doi.org/10.1158/2159-8290.CD-21-1411
Language: English
Keywords: Science & Technology, Life Sciences & Biomedicine, Oncology
UCL classification: UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Cancer Institute > Research Department of Oncology
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences
UCL
UCL > Provost and Vice Provost Offices > School of Life and Medical Sciences > Faculty of Medical Sciences > Cancer Institute
URI: https://discovery.ucl.ac.uk/id/eprint/10143833
Downloads since deposit
1Download
Download activity - last month
Download activity - last 12 months
Downloads by country - last 12 months

Archive Staff Only

View Item View Item