eprintid: 10143833
rev_number: 10
eprint_status: archive
userid: 699
dir: disk0/10/14/38/33
datestamp: 2022-02-18 11:28:14
lastmod: 2023-01-13 07:10:31
status_changed: 2022-02-18 11:28:14
type: article
metadata_visibility: show
sword_depositor: 699
creators_name: Vanhaesebroeck, Bart
creators_name: Burke, John E
creators_name: Madsen, Ralitsa R
title: Precision Targeting of Mutant PI3Kα in Cancer by Selective Degradation
ispublished: pub
divisions: C10
divisions: G99
divisions: B02
divisions: UCL
divisions: D19
keywords: Science & Technology, Life Sciences & Biomedicine, Oncology
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.
date: 2022-01-12
date_type: published
publisher: American Association for Cancer Research
official_url: https://doi.org/10.1158/2159-8290.CD-21-1411
oa_status: green
full_text_type: other
language: eng
primo: open
primo_central: open_green
verified: verified_manual
elements_id: 1916371
doi: 10.1158/2159-8290.CD-21-1411
medium: Print
pii: 12/1/20
lyricists_name: Vanhaesebroeck, Bart
lyricists_id: BAMVA48
actors_name: Vanhaesebroeck, Bart
actors_id: BAMVA48
actors_role: owner
funding_acknowledgements: 220464 [Wellcome Trust]
full_text_status: public
publication: Cancer Discovery
volume: 12
number: 1
pagerange: 20-22
event_location: United States
issn: 2159-8274
citation:        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 <https://doi.org/10.1158/2159-8290.CD-21-1411>.       Green open access   
 
document_url: https://discovery.ucl.ac.uk/id/eprint/10143833/1/Vanhaesebroeck_Cancer%20Discovery_mutant%20PI3Ka%20degraders_Nov%2015_QC.pdf