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Researchers from Scripps Research Institute Report on Findings in Proteomics (Positive allosteric modulators to peptide GPCRs: a promising class of...

August 20, 2014

Researchers from Scripps Research Institute Report on Findings in Proteomics (Positive allosteric modulators to peptide GPCRs: a promising class of drugs)

By a News Reporter-Staff News Editor at Biotech Week -- Researchers detail new data in Proteomics. According to news reporting out of La Jolla, California, by NewsRx editors, research stated, "The task of finding selective and stable peptide receptor agonists with low molecular weight, desirable pharmacokinetic properties and penetrable to the blood-brain barrier has proven too difficult for many highly coveted drug targets, including receptors for endothelin, vasoactive intestinal peptide and galanin. These receptors and ligand-gated ion channels activated by structurally simple agonists such as glutamate, glycine and GABA present such a narrow chemical space that the design of subtype-selective molecules capable of distinguishing a dozen of glutamate and GABA receptor subtypes and possessing desirable pharmacokinetic properties has also been problematic."

Our news journalists obtained a quote from the research from Scripps Research Institute, "In contrast, the pharmaceutical industry demonstrates a remarkable success in developing 1,4-benzodiazepines, positive allosteric modulators (PMAs) of the GABAA receptor. They were synthesized over 50 years ago and discovered to have anxiolytic potential through an in vivo assay. As exemplified by Librium, Valium and Dormicum, these allosteric ligands of the receptor became the world's first blockbuster drugs. Through molecular manipulation over the past 2 decades, including mutations and knockouts of the endogenous ligands or their receptors, and by in-depth physiological and pharmacological studies, more peptide and glutamate receptors have become well-validated drug targets for which an agonist is sought. In such cases, the pursuit for PAMs has also intensified, and a working paradigm to identify drug candidates that are designed as PAMs has emerged."

According to the news editors, the research concluded: "This review, which focuses on the general principles of finding PAMs of peptide receptors in the 21st century, describes the workflow and some of its resulting compounds such as PAMs of galanin receptor 2 that act as potent anticonvulsant agents."

For more information on this research see: Positive allosteric modulators to peptide GPCRs: a promising class of drugs. Acta Pharmacologica Sinica, 2013;34(7):880-5. (Nature Publishing Group -; Acta Pharmacologica Sinica -

Our news journalists report that additional information may be obtained by contacting T. Bartfai, Dept. of Chemical Physiology, The Scripps Research Institute, La Jolla, CA 92037, United States (see also Proteomics).

Keywords for this news article include: Pharmaceuticals, Drugs, Therapy, La Jolla, Peptides, Proteins, California, Glutamates, Proteomics, United States, Glutamic Acid, Pharmacokinetics, North and Central America.

Our reports deliver fact-based news of research and discoveries from around the world. Copyright 2014, NewsRx LLC

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Source: Biotech Week

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