Journal
CURRENT MEDICINAL CHEMISTRY
Volume 11, Issue 21, Pages 2785-2798Publisher
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/0929867043364270
Keywords
constrained amino acids; constrained peptides; ligand-receptor interactions; drug design
Funding
- NIDA NIH HHS [DA13449, DA12394, DA06248] Funding Source: Medline
- NIDDK NIH HHS [DK17420] Funding Source: Medline
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Ligand binding and concomitant changes in receptor structure provide the means to target signal transduction pathways. With appropriate refinement of the ligand's 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.
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