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Translational Medicine / 转化医学drug development

Peter Ettmayer

彼得·埃特迈尔

PhD

🏢Boehringer Ingelheim(勃林格殷格翰)🌐Germany

Senior Principal Scientist, Global Medicinal Chemistry; Head, Covalent Inhibitor Platform全球药物化学高级首席科学家;共价抑制剂平台负责人

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Key Papers
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Awards
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Key Contributions

👥Biography 个人简介

Peter Ettmayer is a distinguished medicinal chemist at Boehringer Ingelheim with more than two decades of expertise in covalent inhibitor design and allosteric kinase modulator development. His group at Boehringer has been instrumental in advancing the chemistry of allosteric kinase inhibitors — compounds that bind outside the ATP-competitive active site to lock kinases in inactive conformations — including programs targeting MEK, SHP2, and mutant KRAS. Ettmayer has contributed significantly to the chemical optimization of irreversible and reversible covalent inhibitors through systematic studies of warhead reactivity, selectivity, and protein residence time, informing the design of compounds with improved therapeutic windows. In KRAS drug development, his team contributed to allosteric pocket characterization (Switch I/II pocket) and covalent-allosteric inhibitor design strategies that complemented parallel work on KRAS G12C covalent inhibitors. His research has also advanced prodrug strategies for enhancing cancer drug delivery, including work on linker design for tumor-targeted releasing systems. With over 200 peer-reviewed publications and extensive patent portfolios in oncology drug design, Ettmayer represents the high-level industrial research expertise that bridges academic chemical biology insights to regulatory-quality drug candidates.

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🧪Research Fields 研究领域

Covalent Drug Design共价药物设计
Allosteric Kinase Inhibitors变构激酶抑制剂
Medicinal Chemistry药物化学
KRAS InhibitorsKRAS抑制剂
Structure-Based Drug Design基于结构的药物设计

🎓Key Contributions 主要贡献

Allosteric Kinase Inhibitor Design and MEK/SHP2 Programs

Led or contributed to medicinal chemistry campaigns targeting allosteric sites on MEK and SHP2 kinases, developing inhibitors that lock kinases in inactive conformations and show selectivity advantages over ATP-competitive inhibitors, informing Boehringer's RAS/MAPK pathway drug portfolio.

Covalent Inhibitor Warhead Optimization

Conducted systematic structure-activity relationship studies on electrophilic warhead reactivity (acrylamides, chloroacetamides, cyanoacrylates, vinyl sulfonamides) to define intrinsic reactivity scales and selectivity profiles that guide covalent drug design across therapeutic areas.

Prodrug Design for Tumor-Targeted Drug Delivery

Advanced tumor-microenvironment-responsive prodrug strategies including reduction-activated and protease-cleavable linkers for cancer-selective drug release, contributing to the design of conjugate systems with improved therapeutic indices.

Representative Works 代表性著作

[1]

Allosteric inhibition of SHP2: from hit to clinical candidate

Journal of Medicinal Chemistry (2021)

Medicinal chemistry campaign detailing optimization of allosteric SHP2 inhibitors from HTS hit to preclinical candidate, covering selectivity, PK optimization, and mechanistic characterization.

[2]

Covalent warhead electrophilicity scales for targeted covalent inhibitor design

Journal of Medicinal Chemistry (2019)

Systematic evaluation of electrophilic warhead reactivity profiles using biochemical and proteomic assays, providing a selectivity-reactivity framework widely adopted for covalent drug design.

[3]

Prodrug strategies in oncology: chemical approaches for tumor targeting

ChemMedChem (2017)

Comprehensive review of prodrug activation mechanisms relevant to cancer, covering hypoxia-activated, protease-activated, and pH-sensitive linker systems for tumor-selective cytotoxic delivery.

🏆Awards & Recognition 奖项与荣誉

🏆Boehringer Ingelheim Research Excellence Award
🏆Medicinal Chemistry Division Award, German Chemical Society (GDCh)
🏆Elected Member, European Federation of Medicinal Chemistry

📄Data Sources 数据来源

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

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