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

Abstract : Peptides have gained renewed interest as candidate therapeutics. However, to bring them to a broader clinical use, challenges such as the rational optimization of their pharmacological properties remain. Peptide scanning techniques offer a systematic framework to gain information on the functional role of individual amino acids of a peptide. Due to progress in mastering new chemical synthesis routes targeting amino acid backbone, they are currently diversified. Structure-activity relationship (SAR) analyses such as alanine- or enantioneric- scanning can now be supplemented by N-substitution, lactam cyclisation- or aza-amino scanning procedures addressing not only SAR considerations but also the peptide pharmacological properties.
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Contributor : Jérôme Leprince <>
Submitted on : Thursday, December 20, 2018 - 6:08:32 PM
Last modification on : Tuesday, April 7, 2020 - 3:36:03 PM

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Stéphanie Eustache, Jérôme Leprince, Pierre Tufféry. Progress with peptide scanning to study structure-activity relationships: the implications for drug discovery. Expert Opinion on Drug Discovery, Informa Healthcare, 2016, 11 (8), pp.771-784. ⟨10.1080/17460441.2016.1201058⟩. ⟨hal-01962730⟩

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