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CDD-1272
- Development stage
- Preclinical
- Lead developer
- Baylor College of Medicine
- Modality
- Small Molecules
01
Overview
CDD-1272 is a small molecule inhibitor of wild-type and mutant estrogen receptor alpha (ERα) discovered via DNA-encoded chemical library (DEL) screening. Developed by researchers at the Baylor College of Medicine, CDD-1272 is a 'di-synthon' compound (comprising building blocks 2 and 3 of the DEL hit series) that targets the ligand-binding domain (LBD) of ERα, including the constitutively active Y537S and D538G mutants. It acts by preventing the recruitment of the steroid receptor coactivator 3 (SRC3) peptide to the mutant ERα LBD, thereby inhibiting estrogen receptor-mediated signaling and cell growth in ER-positive breast cancer models.
- Other names
- 21-di
02
Targets
ESR1 (ERα)
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