Mckeown, Stephen, Zecri, Frederic, Fortier, Eric, Taggart, Andrew, Sviridenko, Lilya, Adams, Christopher, Mcallister, Kathryn and Pin, Sokhom (2014) The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor. Bioorganic and Medicinal Chemistry Letters, 24 (20). pp. 4871-4875. ISSN 1464-3405

Abstract

This Letter describes methodology to enable the identification of tool or therapeutic lipopeptides which modulate the function of membrane bound proteins. The choice of lipopeptides as a chemotype is the amalgamation of multiple medicinal chemistry considerations including duration of action, low systemic exposure and access to intracellular components. The 'lipopeptide shuffle' has been applied here to the APJ receptor and has rapidly resulted in the discovery of a 33 nM APJ agonist hit from an initial 369 member lipopeptide synthetic array.

Item Type:	Article
Keywords:	Apelin APJ agonist Lipopeptide Pepducin Peptide Protein protein interactions
Date Deposited:	25 Nov 2017 00:45
Last Modified:	25 Jan 2019 00:46
URI:	https://oak.novartis.com/id/eprint/22429