Ontology highlight
ABSTRACT:
SUBMITTER: Ketcham JM
PROVIDER: S-EPMC10983000 | biostudies-literature | 2024 Mar
REPOSITORIES: biostudies-literature
Ketcham John M JM Harwood Stephen J SJ Aranda Ruth R Aloiau Athenea N AN Bobek Briana M BM Briere David M DM Burns Aaron C AC Caddell Haatveit Kersti K Calinisan Andrew A Clarine Jeffery J Elliott Adam A Engstrom Lars D LD Gunn Robin J RJ Ivetac Anthony A Jones Benjamin B Kuehler Jon J Lawson J David JD Nguyen Natalie N Parker Cody C Pearson Kelly E KE Rahbaek Lisa L Saechao Barbara B Wang Xiaolun X Waters Anna A Waters Laura L Watkins Ashlee H AH Olson Peter P Smith Christopher R CR Christensen James G JG Marx Matthew A MA
Journal of medicinal chemistry 20240313 6
The H1047R mutation of <i>PIK3CA</i> is highly prevalent in breast cancers and other solid tumors. Selectively targeting PI3Kα<sup>H1047R</sup> over PI3Kα<sup>WT</sup> is crucial due to the role that PI3Kα<sup>WT</sup> plays in normal cellular processes, including glucose homeostasis. Currently, only one PI3Kα<sup>H1047R</sup>-selective inhibitor has progressed into clinical trials, while three pan mutant (H1047R, H1047L, H1047Y, E542K, and E545K) selective PI3Kα inhibitors have also reached the ...[more]