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Discovery of BBO-8520, a first-in-class direct and covalent dual inhibitor of GTP-bound (ON) and GDP-bound (OFF) KRASG12C.
Maciag AE, Stice JP, Wang B, Sharma AK, Chan AH, Lin K, Singh D, Dyba M, Yang Y, Setoodeh S, Smith BP, Ju JH, Jeknic S, Rabara D, Zhang Z, Larsen EK, Esposito D, Denson JP, Ranieri M, Meynardie M, Mehdizadeh S, Alexander PA, Abreu Blanco M, Turner DM, Xu R, Lightstone FC, Wong KK, Stephen AG, Wang K, Simanshu DK, Sinkevicius KW, Nissley DV, Wallace E, McCormick F, Beltran PJ. Maciag AE, et al. Among authors: stephen ag. Cancer Discov. 2024 Dec 6. doi: 10.1158/2159-8290.CD-24-0840. Online ahead of print. Cancer Discov. 2024. PMID: 39642212
Comprehensive structure-function analysis reveals gain- and loss-of-function mechanisms impacting oncogenic KRAS activity.
Kwon JJ, Dilly J, Liu S, Kim E, Bian Y, Dharmaiah S, Tran TH, Kapner KS, Ly SH, Yang X, Rabara D, Waybright TJ, Giacomelli AO, Hong AL, Misek S, Wang B, Ravi A, Doench JG, Beroukhim R, Lemke CT, Haigis KM, Esposito D, Root DE, Nissley DV, Stephen AG, McCormick F, Simanshu DK, Hahn WC, Aguirre AJ. Kwon JJ, et al. Among authors: stephen ag. bioRxiv [Preprint]. 2024 Oct 25:2024.10.22.618529. doi: 10.1101/2024.10.22.618529. bioRxiv. 2024. PMID: 39484452 Free PMC article. Preprint.
460 results