Design of beta-turn based therapeutic agents.
Peptides and proteins are essential to many biological processes. The interaction between the peptide ligands and their receptor targets commonly involves beta-turn structures. Yet poor bioavailability and unfavorable pharmacokinetics significantly compromise the use of peptides as drugs. Thus, there has been a great deal of interest in the design of peptidomimetics (modified peptides) as therapeutic agents by mimicking beta-turn structures. This review highlights the importance of beta-turn in the design of various peptidomimetics for many diseases. This review also outlines several beta-turn mimicking strategies and its application in the design of potent peptide analogues. beta-turn mimetics often tend to be more rigid in positioning the critically important amino acid residues and thus optimize the surface conformation for productive interaction with the receptors.
Kee
K Suat
KS
Department of Pharmacy, 18 Science drive 4, National University of Singapore, Singapore 117543.
Jois
Seetharama D S
SD
D015195:Drug Design; D006801:Humans; D008024:Ligands; D018716:Molecular Mimicry; D010455:Peptides / Q000737:chemistry* / Q000627:therapeutic use*; D017433:Protein Structure, Secondary; D013329:Structure-Activity Relationship
D008024:Ligands; D010455:Peptides