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targeted-therapy / targeted-therapyKRAS Inhibitors

Kevan Shokat

凯文·肖卡特

PhD

🏢University of California, San Francisco(加州大学旧金山分校)🌐USA

Professor, Department of Cellular and Molecular Pharmacology细胞与分子药理学系教授

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h-index
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Key Papers
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Awards
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Key Contributions

👥Biography 个人简介

Kevan Shokat is a pioneering chemical biologist at UCSF who cracked the 'undruggable' KRAS problem by discovering the G12C covalent binding pocket. His work directly enabled sotorasib and adagrasib, the first approved KRAS inhibitors, transforming lung cancer treatment.

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🧪Research Fields 研究领域

Targeted Therapy靶向治疗
KRAS InhibitionKRAS抑制剂
Covalent Inhibitor Chemistry共价抑制剂化学
Chemical Biology化学生物学

🎓Key Contributions 主要贡献

KRAS G12C Covalent Inhibitor Discovery

Identified a cryptic switch-II pocket on KRAS G12C, enabling covalent inhibitor design. This breakthrough directly led to FDA-approved sotorasib and adagrasib for NSCLC.

Covalent Chemical Biology

Pioneered chemical strategies for targeting oncoproteins previously considered undruggable, establishing a new paradigm for covalent warhead-based drug discovery across oncology.

Representative Works 代表性著作

[1]

Drugging an undruggable pocket on KRAS

Nature (2013)

Seminal paper identifying the switch-II pocket on KRAS G12C that enabled the first covalent KRAS inhibitors, launching a new therapeutic era.

[2]

Allele-specific inhibitors inactivate mutant RAS isoforms

Science (2015)

Demonstrated selective inhibition of KRAS G12C with covalent compounds, validating the therapeutic strategy that reached clinical approval.

🏆Awards & Recognition 奖项与荣誉

🏆Breakthrough Prize in Life Sciences (2019)
🏆Wolf Prize in Chemistry (2023)
🏆NCI Outstanding Investigator Award
🏆AACR Award for Outstanding Achievement in Chemistry in Cancer Research

📄Data Sources 数据来源

Last updated: 2026-01-15 | All information from publicly available academic sources

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