A rapid method to identify exo-protease inhibitors

¹The Skaggs Institute for Chemical Biology, Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.

Bioorganic & Medicinal Chemistry Letters

|September 7, 1999

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.

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Abstract:

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