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The Substrate-Activity-Screening methodology applied to receptor tyrosine kinases: A proof-of-concept study.

Chapelat, Julien and Berst, Frederic and Marzinzik, Andreas and Moebitz, Henrik and Drueckes, Peter and Trappe, Joerg and Fabbro, Doriano and Seebach, Dieter (2012) The Substrate-Activity-Screening methodology applied to receptor tyrosine kinases: A proof-of-concept study. European Journal of Medicinal Chemistry. ISSN 0223-5234

Abstract

Protein kinases are widely recognized as important therapeutic targets due to their involvement in signal transduction pathways. These pathways are tightly controlled and regulated, notably by the ability of kinases to selectively phosphorylate a defined set of substrates. A wide variety of disorders can arise as a consequence of abnormal kinase-mediated phosphorylation and numerous kinase inhibitors have earned their place as key components of the modern pharmacopeia. Although “traditional” kinase inhibitors typically act by preventing the interaction between the kinase and ATP, thus stopping substrate phosphorylation, an alternative approach consists in disrupting the protein-protein interaction between the kinase and its downstream partners. We herein report a proof-of-concept application of the Substrate Activity Screening methodology to Insulin-like Growth Factor 1 Receptor as a tool for the discovery of substrate-site-directed tyrosine kinase inhibitors.

Item Type: Article
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Keywords: Kinase inhibitor Substrate-Activity-Screening Protein-Protein Interactions Michaelis-Menten kinetics Insulin-like Growth Factor 1 Receptor
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Date Deposited: 13 Oct 2015 13:14
Last Modified: 13 Oct 2015 13:14
URI: https://oak.novartis.com/id/eprint/6796

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