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ID: ALA1131831

Journal: Bioorg Med Chem Lett

Title: A rapid method to identify exo-protease inhibitors.

Authors: Pryor KE, La Clair JJ.

Abstract: A new approach to the evaluation of exo-protease inhibitor candidates is presented. The application of new water-soluble substrates that release organic-soluble fluorescent groups upon proteolytic cleavage allows amplification of the assay signal via concentration of the cleavage product. A combinatorial library of disubstituted xanthenes designed to resemble a known inhibitor was screened and a new HLE inhibitor (Ki = 79 microM) was identified.

CiteXplore: 10476856

DOI: 10.1016/s0960-894x(99)00387-x