Precision Targeting of Mutant PI3Kα in Cancer by Selective Degradation.
| Autor: | Vanhaesebroeck B; University College London Cancer Institute, University College London, London, United Kingdom. bart.vanh@ucl.ac.uk., Burke JE; Department of Biochemistry and Microbiology, University of Victoria, Victoria, British Columbia, Canada.; Department of Biochemistry and Molecular Biology, University of British Columbia, Vancouver, British Columbia, Canada., Madsen RR; University College London Cancer Institute, University College London, London, United Kingdom. |
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| Jazyk: | angličtina |
| Zdroj: | Cancer discovery [Cancer Discov] 2022 Jan; Vol. 12 (1), pp. 20-22. |
| DOI: | 10.1158/2159-8290.CD-21-1411 |
| Abstrakt: | 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 . (©2022 American Association for Cancer Research.) |
| Databáze: | MEDLINE |
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