title: A rapid method to identify exo-protease inhibitors.
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.
authors.affiliation: The Skaggs Institute for Chemical Biology, Department of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, USA.
authors.forename: K E
authors.initials: KE
authors.lastname: Pryor
authors.forename: J J
authors.initials: JJ
authors.lastname: La Clair
mesh_terms: D003124:Colorimetry; D006868:Hydrolysis; D011480:Protease Inhibitors / Q000737:chemistry*; D013050:Spectrometry, Fluorescence; D013056:Spectrophotometry, Ultraviolet
chemical_list: D011480:Protease Inhibitors