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Oct 4, 2010

Innovations in Peptide Structure Pushing Candidates through Development

Companies are taking aim at otherwise untractable targets.

Innovations in Peptide Structure Pushing Candidates through Development

Anchor Therapeutics and Arkitek Studios

  • Innovations to enhance the performance of peptide therapeutics continue to evolve as they attract more development deals. Changes have occurred in peptide chemistry, formulation, synthesis, manufacturing, and delivery. Peptide fans say they have multiple advantages compared to small molecule drugs, including relatively high activity, specificity, and potency as well as lower toxicity.  Drawbacks that peptide companies are working to overcome include low bioavailability, instability, poor solubility, delivery challenges, and manufacturing costs.

    Innovations in peptide structure include Anchor Therapeutics pepducin technology, which has demonstrated the ability to prevent breast cancer, blood clotting, and sepsis in animal models. On August 20, the company drew $10 million in a Series B financing. On September 9, Ortho-McNeil-Janssen Pharmaceuticals signed on to use pepducin technology to develop GPCR-targeted therapeutics for oncology and metabolic disorders. Anchor will receive an up-front payment as well as research support and could be eligible for development and regulatory milestone payments of up to $480 million. 

    Pepducins are short peptides containing a lipid moiety. This allows them to bind to the intracellular portion of receptors and change their conformation, a process known as allosteric modification, unlike classical ligands that bind to the extracellular surface of receptors. Pepducins were developed in the late 1990s by Athan Kuliopulos, M.D., Ph.D., and his colleagues at Tufts University Medical Center.

    “Because pepducins can penetrate the cell and can either agonize or antagonize their targets, they are a potent tool both for research and therapeutic applications,” Dr. Kuliopulos explained. “Pepducins can greatly increase both the range of tractable targets and the specificity with which we can modulate their effect.”


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