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RIPK2 degraders (PROTAC series)

Development stage
Preclinical
Lead developer
Aurigene Oncology
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Subcutaneous, Parenteral, Oral, Intramuscular, Intradermal, Intravitreal
01

Overview

Aurigene is developing a series of Proteolysis-Targeting Chimera (PROTAC) molecules designed to selectively induce the degradation of Receptor-Interacting Protein Kinase 2 (RIPK2). RIPK2 is a key signaling protein that mediates the activation of inflammatory pathways, specifically those triggered by the NOD1 and NOD2 intracellular pattern recognition receptors. By recruiting an E3 ubiquitin ligase to RIPK2, these PROTACs facilitate its polyubiquitination and subsequent degradation by the proteasome. This approach aims to provide more comprehensive inhibition of the NOD signaling pathway compared to traditional small-molecule inhibitors, which only block the kinase activity of RIPK2. The program is currently in the preclinical discovery phase, with potential applications in treating various autoimmune and inflammatory disorders, such as inflammatory bowel disease and sarcoidosis.

Other names
RIPK2 degradersRIPK-2 degradersRIPK 2 degradersRIPK2 PROTACsRIPK-2 PROTACsRIPK 2 PROTACs
02

Targets

RIPK2 (Receptor-interacting protein serine/threonine kinase 2)CRL4-CRBN (Cereblon-based E3 ubiquitin ligase complex)

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