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Design of β-turn Based Therapeutic Agents

[ Vol. 9 , Issue. 15 ]

Author(s):

K. Kee Suat and Seetharama D.S. Jois   Pages 1209 - 1224 ( 16 )

Abstract:


Peptides and proteins are essential to many biological processes. The interaction between the peptide ligands and their receptor targets commonly involves β-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 β-turn structures. This review highlights the importance of β-turn in the design of various peptidomimetics for many diseases. This review also outlines several β-turn mimicking strategies and its application in the design of potent peptide analogues. β-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.

Keywords:

proteins, peptidomimetics, amino acid, pharmacokinetics, melanocyte-stimulating hormone, bradykinin, lutenizing, circular dichroism(cd)

Affiliation:

Department of Pharmacy, 18 Science drive 4,National University of Singapore,Singapore 117543.



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