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Current Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

Exploring Ramachandran and Chi Space: Conformationally Constrained Amino Acids and Peptides in the Design of Bioactive Polypeptide Ligands

Author(s): S. M. Cowell, Y. S. Lee, J. P. Cain and V. J. Hruby

Volume 11, Issue 21, 2004

Page: [2785 - 2798] Pages: 14

DOI: 10.2174/0929867043364270

Price: $65

Abstract

Ligand binding and concomitant changes in receptor structure provide the means to target signal transduction pathways. With appropriate refinement of the ligands interaction with the “receptor,” one in theory could produce ligands that have greater therapeutic benefits. This review will discuss how, when these ligands are amino acids and peptides, the introduction of appropriate conformational constraints provides a powerful strategy for improved drug design. This review will discuss how various constraints on amino acids can provide a powerful tool for ligand design, determination of the three dimensional pharmacophore and new insights into receptor systems and information transduction. Through the use of constrained ligands, new information regarding their interaction with their “receptor” systems, and further refinement of the use of constraints, scientists can produce more beneficial drugs for mankind.

Keywords: constrained amino acids, constrained peptides, ligand-receptor interactions, drug design

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