TY - JOUR
T1 - Designing βpep peptides
T2 - A rational approach to the discovery of novel pharmaceutical agents and small molecules
AU - Mayo, Kevin H.
AU - Griffioen, Arjan W.
PY - 2003/4/1
Y1 - 2003/4/1
N2 - 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 (βpep peptides) as potential pharmaceutical drugs. βpep peptides generally fold as β-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, βpep peptides can function as antibacterials, antiangiogenics, 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.
AB - 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 (βpep peptides) as potential pharmaceutical drugs. βpep peptides generally fold as β-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, βpep peptides can function as antibacterials, antiangiogenics, 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.
UR - http://www.scopus.com/inward/record.url?scp=0038573729&partnerID=8YFLogxK
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U2 - 10.1358/dof.2003.028.04.740190
DO - 10.1358/dof.2003.028.04.740190
M3 - Review article
AN - SCOPUS:0038573729
SN - 0377-8282
VL - 28
SP - 337
EP - 346
JO - Drugs of the Future
JF - Drugs of the Future
IS - 4
ER -