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Wiley, ChemMedChem, 2(5), p. 195-199, 2010

DOI: 10.1002/cmdc.200900516

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Chelator Fragment Libraries for Targeting Metalloproteinases

Journal article published in 2010 by Arpita Agrawal, Sherida L. Johnson, Jennifer A. Jacobsen, Melissa T. Miller, Li-Hsing Chen, Maurizio Pellecchia, Seth M. Cohen ORCID
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This paper is available in a repository.

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Abstract

A chelator fragment library based on a variety of metal binding groups was screened against a metalloproteinase. Lead hits were identified and an expanded library of select compounds was synthesized, resulting in numerous high-affinity hits against several metalloprotein targets. The findings clearly demonstrate that chelators can be used to generate libraries suitable for fragment-based lead design (FBLD) directed at important metalloproteins.