Application of a novel design paradigm to generate general nonpeptide combinatorial templates mimicking β-turns: Synthesis of ligands for melanocortin receptors

Thomas R. Webb, Luyong Jiang, Sergey Sviridov, Ruben E. Venegas, Anna V. Vlaskina, Douglas McGrath, John Tucker, Jian Wang, Alain Deschenes, Rongshi Li

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

We report the further application of a novel approach to template and ligand design by the synthesis of agonists of the melanocortin receptor. This design method uses the conserved structural data from the three-dimensional conformations of β-turn peptides to design rigid nonpeptide templates that mimic the orientation of the main chain C-α atoms in a peptide β-turn. We report details on a new synthesis of derivatives of template 1 that are useful for the synthesis of exploratory libraries. The utility of this technique is further exemplified by several iterative rounds of high-throughput synthesis and screening, which result in new partially optimized nonpeptide agonists for several melanocortin receptors.

Original languageEnglish (US)
Pages (from-to)704-710
Number of pages7
JournalJournal of Combinatorial Chemistry
Volume9
Issue number4
DOIs
StatePublished - Jul 1 2007

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Melanocortin Receptors
Receptor
Template
Paradigm
Synthesis
Ligands
Peptides
Libraries
Conformation
High Throughput
Design Method
Screening
Conformations
Throughput
Derivatives
Derivative
Atoms
Three-dimensional
Design

ASJC Scopus subject areas

  • Chemistry(all)

Cite this

Application of a novel design paradigm to generate general nonpeptide combinatorial templates mimicking β-turns : Synthesis of ligands for melanocortin receptors. / Webb, Thomas R.; Jiang, Luyong; Sviridov, Sergey; Venegas, Ruben E.; Vlaskina, Anna V.; McGrath, Douglas; Tucker, John; Wang, Jian; Deschenes, Alain; Li, Rongshi.

In: Journal of Combinatorial Chemistry, Vol. 9, No. 4, 01.07.2007, p. 704-710.

Research output: Contribution to journalArticle

Webb, Thomas R. ; Jiang, Luyong ; Sviridov, Sergey ; Venegas, Ruben E. ; Vlaskina, Anna V. ; McGrath, Douglas ; Tucker, John ; Wang, Jian ; Deschenes, Alain ; Li, Rongshi. / Application of a novel design paradigm to generate general nonpeptide combinatorial templates mimicking β-turns : Synthesis of ligands for melanocortin receptors. In: Journal of Combinatorial Chemistry. 2007 ; Vol. 9, No. 4. pp. 704-710.
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