Tremendous advances have been made in the discovery of novel ligands for G-protein-coupled receptors (GPCRs) that act at allosteric sites to regulate receptor function. Small molecules can act at ...

Positive and negative allosteric modulators (PAMs and NAMs) have now been identified for members of each major subfamily of G protein-coupled receptors (GPCRs). Multiple allosteric modulators have ...

G protein-coupled receptors (GPCRs) are intrinsically allosteric proteins. Through spatially distinct, but conformationally linked, binding sites they have evolved to transduce signals from one ...

It has become apparent that potentially all GPCRs possess allosteric binding sites that are topographically distinct to the location where the endogenous ligand binds, and are less conserved than ...

A publication from Acta Pharmaceutica Sinica B discusses allosteric modulation of G protein-coupled receptors as a novel therapeutic strategy in neuropathic pain. Neuropathic pain is a debilitating ...

“Our technology is making GPCR R&D timelines comparable to those for enzyme targets, which is exciting.” In the future, the company is looking to generate co-structures with allosteric ...

Explore GPCR-targeting therapies and their untapped potential in drug development, making up 30-35 percent of approved drugs.

Capturing the conformational dynamics of GPCRs, describing various functional states, and understanding allosteric mechanisms and their role in G protein selectivity, coupling promiscuity ...

The data tool or protocol will uncover a novel class of compounds -- allosteric drugs in G protein-coupled receptors (GPCRs). GPCRs are the largest membrane protein family that transduce a signal ...

RELATED: Tectonic Therapeutic banks $80M to shift GPCR drug discovery toward biologics “The allosteric concept means you can drill all over the country rather than just in that one tiny little ...

Very few approved GPCR-targeting drugs bind to allosteric sites, opening up a huge opportunity for Septerna, according to Finer. Against this backdrop, the company hopes to channel its series B ...

This new article publication from Acta Pharmaceutica Sinica B, discusses allosteric modulation of G protein-coupled receptors as a novel therapeutic strategy in neuropathic pain. Neuropathic pain ...