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PEPTIDOMIMETICS A WEAPON OF DRUG DESIGN AND DISCOVERY. Manshu Narang, Ankur Gera and Sandeep Arora

PEPTIDOMIMETICS A WEAPON OF DRUG DESIGN AND DISCOVERY.

Manshu Narang, Ankur Gera and Sandeep Arora

International Journal of Natural Product Science 2012: Spl Issue 1:127.

Abstract(RBIP-127)

Peptides perform various biological roles as neurotransmitters, neuromodulators, hormones, enzyme inhibitors, substrates. Binding to their corresponding receptors or enzymes, they can influence cell-cell communication and control a series of vital functions such as metabolism, immune defense, digestion, respiration, sensitivity to pain, reproduction, behavior, and electrolyte levels. Peptidomimetics are compounds whose important element mimic a natural peptide or protein in 3D space while retaining the ability to interact with the biological target and produce the same biological effect. Peptidomimetics are designed to overcome the problems associated with a native peptide: for example stability against proteolysis, poor bioavailability, poor transport through cellular membranes, increased excretion rates, receptor selectivity or potency often can be substantially improved. Various peptidomimetic strategies can be used to decrease the complexity of native peptide which is conformationally flexible. Small mimic can be obtained by incorporating conformationally restricted units such as unnatural amino acids, cyclization of peptides, replacement of peptide bond with various amide isosteres, transformation of peptide to non peptide. Peptide mimicry is a promising approach with versatile applications for the generation of peptide secondary structure analogues.
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