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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Discovery of Thrombin Inhibitor Fragments from Chemical Microarray Screening

Author(s): Thomas Neumann, Hans-Dieter Junker, Oliver Keil, Klaus Burkert, Holger Ottleben, Jurgen Gamer, Renate Sekul, Holger Deppe, Achim Feurer, Dirk Tomandl and Gunther Metz

Volume 2, Issue 8, 2005

Page: [590 - 594] Pages: 5

DOI: 10.2174/157018005774717343

Price: $65

Abstract

Surface plasmon resonance imaging, a low affinity screening method, allows the highly parallel detection of small molecules binding to a target protein. The screening of a fragment based compound library immobilized on chemical microarrays resulted in the discovery of binding fragments for the serine protease thrombin. Functional assays confirmed enzymatic inhibition of microarray hits and crystallography established the binding mode of a non-basic S1 motif providing a starting point for medicinal chemistry.

Keywords: Fragment discovery, chemical microarrays, surface plasmon resonance, thrombin, non-basic S1 binder


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