G protein coupled receptors (GPCRs) are the largest, most important, and best validated class of pharmaceutical targets. When functioning properly, GPCRs are responsible for mediating signal transduction, a critical biological process for maintaining health, whereas improper GPCR signaling is causally implicated in several therapeutic areas including oncology, inflammation, metabolism, heart disease and pain.

Many advances have been made in the development of GPCR-targeted therapeutics, but, while an estimated 30% of marketed drugs target fifty GPCRs and represent annual sales over $40 billion dollars, roughly 90% of the four hundred known GPCRs related to human health have been intractable to traditional small molecule and antibody drug approaches, until now.

Pepducins
Most currently marketed GPCR-based therapeutics act at the receptor's extracellular ligand binding site (the orthosteric site). Pepducins, in contrast, are deliberately designed to modulate GPCRs through their intracellular domain (an allosteric site), altering the GPCR's downstream signaling pathways. Anchor's novel pepducin approach to previously intractable GPCRs may greatly expand the number therapeutically accessible GPCR-related disease pathways, hence better disease treatments. Our discovery platform has proven broadly applicable to producing pepducins that either positively or negatively modulate signaling of a specific GPCR by utilizing this highly selective allosteric mechanism.

Our strategy is to discover and advance pepducin pharmaceutical candidates to treat GPCR-related diseases with high unmet medical needs. Where targeting GPCRs through conventional means has failed, Anchor’s novel approach may prevail.

Anchor Unlocks Enormous New GPCR Market Potential