Health AI Central
Peer-Reviewed Publication
J Med Chem2026;69(17):20494-20519.September 10, 2026Journal Article

Discovery of Highly Potent and Selective, Orally Bioavailable BTK-Targeting PROTACs Featuring Novel CRBN-Binding Warheads.

Alexey B Mantsyzov1, Pei Zhao2, Chris G Kruse1, Rostislav Petrov1, Fubao Huang2, Jiaojiao Yu2, Xin Cai2, Xiao Ding1,2, Vladimir Aladinskiy1, Alex Aliper1, Feng Ren2,3, Alex Zhavoronkov1,2,3
1Insilico Medicine AI Ltd. , Abu Dhabi145748, United Arab Emirates.
2Insilico Medicine Shanghai Ltd. , Shanghai200120, China.
3Insilico Medicine Hong Kong Ltd., Pak Shek Kok, New Territories999077, Hong Kong.
PubMed DOI

Abstract

Drugs targeting Bruton's tyrosine kinase (BTK) are recognized as key tools in hematological oncology. The clinical efficacy of BTK inhibitors is limited, however, by the emerging resistance driven by BTK mutations and the severe toxicity attributed to off-target kinase inhibition. PROteolysis TArgeting Chimeras (PROTACs) offer an alternative modality to address these major drawbacks. Herein, we pr…

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