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Oct 2026

Discovery and Optimization of Isoform Selective ULK1 Degraders to Enhance Antitumor Activity in KRAS-Mutant Cancer

Selective targeting of ULK1 represents a promising approach to overcome autophagy-mediated resistance in KRAS-driven cancers. However, achieving selectivity over the closely related ULK2 isoform with ATP-competitive inhibitors remains challenging due to the high sequence homology within their kinase domains. Here, we...

Sean Chin Chan, S. Bayle, Micheal Lamptey et al. · 0 citations
Jul 2026

Abstract A053: Discovery and modular design of CDK12–DDB1 molecular glues for targeted Cyclin K degradation

Advanced lead molecules across these series achieve a rare combination of high CDK12/13 selectivity, potent and durable cyclin K degradation, and favorable physicochemical, in vitro ADME, and in vivo PK properties, supporting progression toward IND-enabling preclinical safety evaluation.

Thiyagamurthy Pandurangan, Anna Iermolaieva, Pompom Ghosh et al. · 0 citations

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