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Pin1 degrader
- Development stage
- Preclinical
- Lead developer
- Larkspur Biosciences
- Modality
- PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01
Overview
Larkspur Biosciences is developing a first-in-class targeted protein degrader (TPD) directed at Pin1 (peptidylprolyl cis/trans isomerase, NIMA-interacting 1). Pin1 is a prolyl isomerase enzyme that plays a critical role in oncogenic signaling and the maintenance of an immunosuppressive tumor microenvironment. This small molecule is a hetero-bifunctional cereblon-based degrader designed to eliminate Pin1 protein, thereby disrupting cancer cell fitness and reprogramming cancer-associated fibroblasts (CAFs) to promote a pro-immune response. The program is currently in IND-enabling development for the treatment of various cancers, including colorectal, breast, and pancreatic cancer, as well as fibrosis.
- Other names
- Pin1-targeted protein degraderPin-1-targeted protein degraderPin 1-targeted protein degrader
02
Targets
PIN1 (Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1)CRBN (Cereblon)
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