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EPIC-1042
- Development stage
- Preclinical
- Lead developer
- Tianjin Medical University General Hospital
- Modality
- Small Molecules
- Administration
- Intraperitoneal
01
Overview
EPIC-1042 is a small molecule inhibitor of Polymerase I and transcript release factor (PTRF/Cavin1) developed for the treatment of glioblastoma (GBM). Identified through computer-aided drug design (CADD), EPIC-1042 specifically disrupts the interaction between PTRF and caveolin-1. This disruption reduces the secretion of small extracellular vesicles (sEVs) and the efflux of temozolomide (TMZ), thereby overcoming chemoresistance. Additionally, EPIC-1042 promotes the autophagic degradation of PARP1 by enhancing p62 binding and facilitating its translocation into autolysosomes. In preclinical studies, EPIC-1042 has demonstrated the ability to suppress tumor growth and sensitize GBM cells to TMZ treatment.
02
Targets
CAV1 (Caveolin-1)PARP1 (Poly (adp-ribose) polymerase 1)PTRF (Polymerase I and transcript release factor)
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