Progress with peptide scanning to study structure-activity relationships: the implications for drug discovery

作者: Stéphanie Eustache , Jérôme Leprince , Pierre Tufféry

DOI: 10.1080/17460441.2016.1201058

关键词: Functional rolePeptideComputational biologyPeptide drugBiochemistryChemistryDrug discovery

摘要: ABSTRACTIntroduction: Peptides have gained renewed interest as candidate therapeutics. However, to bring them a broader clinical use, challenges such the rational optimization of their pharmacological properties remain. Peptide scanning techniques offer systematic framework gain information on functional role individual amino acids peptide. Due progress in mastering new chemical synthesis routes targeting acid backbone, they are currently diversified. Structure-activity relationship (SAR) analyses alanine- or enantioneric- can now be supplemented by N-substitution, lactam cyclisation- aza-amino procedures addressing not only SAR considerations but also peptide properties.Areas covered: This review highlights different available and illustrates how impact drug discovery.Expert opinion: Progress opens perspectives for development. It come...

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