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PROTAX-E7
- Development stage
- Preclinical
- Lead developer
- University of Michigan
- Modality
- PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
PROTAX-E7 is a small-molecule proteolysis-targeting chimera (PROTAC) designed to induce the selective degradation of the Human Papillomavirus type 16 (HPV16) E7 oncoprotein. HPV16 E7 is a primary driver of oncogenesis in HPV-associated malignancies, including cervical cancer and head and neck squamous cell carcinomas, where it binds to and inactivates the retinoblastoma (pRb) tumor suppressor protein. PROTAX-E7 consists of a ligand for the HPV16 E7 protein linked to a ligand for the Cereblon (CRBN) E3 ubiquitin ligase. By bringing these two proteins into close proximity, the compound facilitates the polyubiquitination of E7 and its subsequent degradation by the 26S proteasome. This mechanism restores pRb levels, leading to cell cycle arrest and apoptosis in HPV16-transformed cells.
- Other names
- HPV16 E7-targeting PROTACHPV-16 E7-targeting PROTACHPV 16 E7-targeting PROTACE7 degraderE-7 degraderE 7 degrader
02
Targets
CRBN (Cereblon)HPV16 E7 (Human papillomavirus 16 E7 protein)
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