Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.

doi:10.1021/acs.jmedchem.2c01422

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Article

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.

Journal of medicinal chemistry - 22 Dec 2022

Hanan Emily J, Braun Marie-Gabrielle, Heald Robert A, MacLeod Calum, Chan Connie, Clausen Saundra, Edgar Kyle A, Eigenbrot Charles, Elliott Richard, Endres Nicholas, Friedman Lori S, Gogol Emily, Gu Xiao-Hui, Thibodeau Rebecca Hong, Jackson Philip S, Kiefer James R, Knight Jamie D, Nannini Michelle, Narukulla Raman, Pace Amanda, Pang Jodie, Purkey Hans E, Salphati Laurent, Sampath Deepak, Schmidt Stephen, Sideris Steve, Song Kyung, Sujatha-Bhaskar Swathi, Ultsch Mark, Wallweber Heidi, Xin Jianfeng, Yeap SiewKuen, Young Amy, Zhong Yu, Staben Steven T

Abstract excerpt

Small molecule inhibitors that target the phosphatidylinositol 3-kinase (PI3K) signaling pathway have received significant interest for the treatment of cancers. The class I isoform PI3Kα is most commonly associated with solid tumors via gene amplification or activating mutations. However, inhibitors demonstrating both PI3K isoform and mutant specificity have remained elusive. Herein, we describe the optimization...

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PMID: 36455032
DOI: 10.1021/acs.jmedchem.2c01422

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