Novel MRGPRX2 Antagonists for Itch and Inflammation

Technology Description

The MRGPRX (mas-related G protein-coupled receptor X) subfamily is only expressed in primates including humans and belongs to the group of orphan receptors, for which the cognate agonists are unknown. The MRGX2 receptor subtype exhibits unique features that distinguish it from other GPCRs. It is involved in mast cell degranulation, nociception and itching, and represents a fundamentally new drug target.

UCSF scientists developed novel potent and selective antagonists of the MRGPRX2 receptor with affinities in the 50 nM range. These molecules show robust activity in cell culture models. Preliminary studies indicate that the molecules may be active against itch and inflammation in non-human primates.

Looking for Partners

To develop and commercialize the technology

Stage of Development

Proof of concept

Data Availability

Under NDA

Patent Status

Patent Pending