A combinatorial approach toward the generation of ambiphilic peptide-based inhibitors of protein:geranylgeranyl transferase-1
article
A combinatorial synthesis of oligopeptide analogues and their evaluation as protein:geranylgeranyl transferase inhibitors is presented. The combinatorial strategy is based on the random mutation, in each new generation, of one of any of the four amino acid building blocks of which the most effective compounds of the previous generation are assembled. In this way, a progressive improvement of the average inhibitory activity was observed until the fifth generation. The most active inhibitors were found to inhibit PGGT-1 in the low micromolar range (IC50: 3.8-8.1 μM). © 2005 American Chemical Society. A combinatorial approach toward the generation. Chemicals / CAS: transferase, 9047-61-4; Alkyl and Aryl Transferases, EC 2.5.-; geranylgeranyltransferase type-I, EC 2.5.1.-; Oligopeptides
Topics
Biomedical Researchgeranylgeranyltransferase type Ioligopeptidetransferasechemistrycombinatorial chemistrydrug antagonismliquid chromatographymass spectrometrymethodologystructure activity relationsynthesisAlkyl and Aryl TransferasesAnimalsCattleChromatography, LiquidCombinatorial Chemistry TechniquesMass SpectrometryOligopeptidesStructure-Activity Relationship
TNO Identifier
238676
ISSN
15204766
Source
Journal of Combinatorial Chemistry, 7(5), pp. 703-713.
Pages
703-713
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