From KRASG12D to Pan-KRAS Inhibitors─A Journey Enabled by Synthetic Innovation and Structure-Based Drug Design.

doi:10.1021/acs.jmedchem.5c03662

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Article

From KRASG12D to Pan-KRAS Inhibitors─A Journey Enabled by Synthetic Innovation and Structure-Based Drug Design.

Journal of medicinal chemistry - 23 Apr 2026

Ma Xiaoshen, Sloman David L, Henderson Timothy J, Bennett D Jonathan, Chessari Gianni, Day Philip J, Duggal Ruchia, Edelstein Emma, Gathiaka Symon, Hoover Andrew, Howard Steven, Kawamura Shuhei, Kobayakawa Yu, Lacey Brian M, Lyons Thomas W, Mansueto My S, Miller Richard, Mizuarai Shinji, Munsell Erik V, O'Reilly Marc, Oshima Tsuyoshi, Otte Ryan D, Palani Anandan, Rees David C, Sagara Takeshi, Sather Aaron, Schopf Patrick, Shibata Kazuaki, Shikata Yuki, Solban Nicolas, Venkataraman Sriraman, Su Dan, Swaminathan Uma, Ye Yingchun, Stoeck Alexander, Han Yongxin

Abstract excerpt

KRAS, a significant oncology target, has been challenging to develop drugs for until recent discoveries of KRASG12C mutant-specific covalent inhibitors, including MK-1084. This article describes efforts toward the discovery of KRASG12D mutant-specific inhibitors and how synthetic innovations and structure-based drug design were utilized to facilitate the discovery of pan-KRAS inhibitors.

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PMID: 41954203
DOI: 10.1021/acs.jmedchem.5c03662

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KRAS

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