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