Designing Ppep peptides: a rational approach to the discovery of novel pharmaceutical agents and small molecules

摘要

Approaches to drug discovery are varied and range from high-throughput screening of small molecule databases to rational design. This review is focused on our use of structural biology and principles of protein folding to rationally design novel peptides (Ppep peptides) as potential pharmaceutical drugs. Ppep peptides generally fold as beta-sheets that can be used as a scaffold with which to present amino acid residues in a functionally relevant fashion, thereby eliciting a desired biological activity. Presently, Ppep peptides can function as antibacterials, antiangiogen-ics, as well as antitumor and anticoagulation agents. Our design approach also allows for relatively easy development of structure-activity relationships, identification of pharmacophore sites and reduction of peptides to smaller molecules.