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SGR-2290

Development stage: Preclinical
Lead developer: Schrödinger
Modality: PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration: Oral

Overview

SGR-2290 is a preclinical-stage targeted protein degrader (TPD) developed by Schrodinger for the treatment of cancers characterized by methylthioadenosine phosphorylase (MTAP) deletion. This genetic deficiency leads to the accumulation of the metabolite methylthioadenosine (MTA), which binds to the Protein Arginine Methyltransferase 5 (PRMT5) enzyme. SGR-2290 is designed to cooperatively bind to the PRMT5-MTA complex and trigger its proteasomal degradation, a synthetic lethality approach that selectively targets tumor cells while sparing normal, MTAP-proficient cells. By inducing the degradation of the specific PRMT5-MTA complex, SGR-2290 aims to overcome the limitations and off-target toxicities associated with non-selective PRMT5 inhibitors.

Other names: PRMT5-MTA degraderPRMT-5-MTA degraderPRMT 5-MTA degrader

Targets

PRMT5 (Protein arginine N-methyltransferase 5)

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