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LG1980
- Development stage
- Preclinical
- Lead developer
- MetCure Therapeutics
- Modality
- PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01
Overview
LG1980 is a preclinical-stage small molecule inhibitor and degrader developed by MetCure Therapeutics for the treatment of chemoresistant cancers, with a primary focus on chemoresistant prostate cancer. The compound functions by disrupting the interaction between Embryonic Ectoderm Development (EED) and Enhancer of Zeste Homolog 2 (EZH2), which are core components of the Polycomb Repressive Complex 2 (PRC2). By targeting this protein-protein interaction, LG1980 modulates the noncanonical EZH2 signaling axis, which regulates downstream effectors including STAT3, SKP2, ABCB1 (P-glycoprotein), and survivin. This mechanism is designed to overcome drug resistance mechanisms and inhibit tumor progression in advanced, treatment-refractory malignancies.
- Other names
- LG1980 AnalogsLG-1980 AnalogsLG 1980 Analogs
02
Targets
EED (Embryonic ectoderm development protein)ABCB1 (P-glycoprotein)BIRC5 (Survivin)STAT3 (Signal Transducer and Activator of Transcription 3)SKP2EZH2 (Histone-lysine N-methyltransferase EZH2)
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