Anchor Therapeutics
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Pepducin Technology

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Anchor's proprietary pepducin technology platform is being used to develop novel, small lipopeptides to greatly expand the scope of G protein coupled receptor (GPCR) drug development. GPCRs are a large class of well validated pharmaceutical targets with enormous untapped potential due to the difficulty in selectively modulating the pharmacology of these membrane-bound receptors using traditional approaches, including small molecules and biologics, which target the extracellular ligand binding sites.

 

Pepducin technology comprises a short peptide derived from a GPCR intracellular loop tethered to a hydrophobic moiety. This structure allows pepducin lipopeptides to anchor in the cell membrane lipid bilayer and target the GPCR/G protein interface via a unique intracellular allosteric mechanism. Pepducins for over 15 different GPCRs have been successfully produced, several of which have shown impressive activity in preclinical in vivo models. Anchor's pepducin technology platform represents an entirely new paradigm for disrupting GPCR signal transduction from the inside surface of the cell, potentially transforming the scope of GPCR therapeutics to treat a much wider range of serious illnesses.

 

Given that pepducin lipopeptides are based on known receptor intracellular loop sequences, the technology bears similarities to biologics but in a small molecular construct that is readily synthesized using traditional peptide synthesis techniques. The ability to use cost effective chemical synthesis approaches enables facile optimization of the pepducin pharmacophore. In addition, pepducin pharmacokinetic properties can be tuned by altering the chemical structure of the hydrophobic membrane tether for any peptide sequence.

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