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Targeting Multiple KRAS Mutations with High-Affinity Macrocyclic Inhibitors: From Discovery to Preclinical Validation.

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Title: Targeting Multiple KRAS Mutations with High-Affinity Macrocyclic Inhibitors: From Discovery to Preclinical Validation.
Authors: Phillips DP; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Alper PB; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Cho CY; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Borkin D; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Han D; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Kochanek SE; Novartis Biomedical Research, Cambridge, Massachusetts 02139, United States., Vidal-Biggart A; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Herath A; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Gurjar J; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Lu W; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Mathison CJN; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Nelson JM; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Pei W; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Yan S; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Nguyen BN; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Hoffman T; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Okram B; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Nguyen TN; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Jiang S; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Masick BT; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Wang Z; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Nikulin V; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Yin H; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Chen Y; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Juarez J; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Sarkisova Y; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Jia Y; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Zhou V; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Liu G; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Liu X; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Lu M; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Taylor BL; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Huynh L; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Wang Y; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Pacoma R; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Baaten J; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Topolewski K; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Wright C; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Nguyen T; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Knee DA; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Liu Q; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Liu J; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Li J; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Virata C; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Briones S; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., DiDonato M; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Bursulaya B; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Jones DH; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Witmer D; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Chu C; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Jin H; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Richmond W; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Westling L; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Hollenbeck T; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Chong A; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Franey S; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Groessl T; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Shapiro M; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Effenberger K; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Arroyo K; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Bretz A; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Honda A; Novartis Biomedical Research, Cambridge, Massachusetts 02139, United States., Brown J; Novartis Biomedical Research, Cambridge, Massachusetts 02139, United States., Sanchez CC; Novartis Biomedical Research, Cambridge, Massachusetts 02139, United States., Gordon WP; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Matzen JT; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Osterman N; Novartis Biomedical Research, Basel CH-4056, Switzerland., Cotesta S; Novartis Biomedical Research, Basel CH-4056, Switzerland., Brachmann SM; Novartis Biomedical Research, Basel CH-4056, Switzerland., Wilcken R; Novartis Biomedical Research, Basel CH-4056, Switzerland., Zecri F; Novartis Biomedical Research, Cambridge, Massachusetts 02139, United States., Beyer KS; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Molteni V; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States., Haling JR; Novartis Biomedical Research, 10675 John Jay Hopkins Drive, San Diego, California 92121, United States.
Source: Journal of medicinal chemistry [J Med Chem] 2026 Jun 11; Vol. 69 (11), pp. 13165-13187. Date of Electronic Publication: 2026 May 19.
Publication Type: Journal Article
Journal Info: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE
Database: MEDLINE Ultimate
Description
ISSN:1520-4804
DOI:10.1021/acs.jmedchem.6c00127