Synthesis of a statistically exhaustive fluorescent peptide substrate library for profiling protease specificity.
A statistically exhaustive, 8800 compound tripeptidal amidomethylcoumarin library was synthesized as discreet compounds using solid-phase combinatorial chemistry. A subset of the compounds was purified by HPLC and tested in a high-throughput fluorometric assay against several known serine and cysteine proteases to demonstrate the utility of this library for profiling protease substrate specificity.
Sheppeck
J E
JE
ChemRx Advanced Technologies, South San Francisco, CA 94080, USA. jim_sheppeck@axystech.com
Kar
H
H
Gosink
L
L
Wheatley
J B
JB
Gjerstad
E
E
Loftus
S M
SM
Zubiria
A R
AR
Janc
J W
JW
D002851:Chromatography, High Pressure Liquid; D020650:Combinatorial Chemistry Techniques; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry; D010450:Endopeptidases / Q000378:metabolism*; D005456:Fluorescent Dyes / Q000138:chemical synthesis* / Q000737:chemistry; D015335:Molecular Probes; D013379:Substrate Specificity
D003374:Coumarins; D005456:Fluorescent Dyes; D015335:Molecular Probes; C030123:coumarin; D010450:Endopeptidases