A low background high-throughput screening (HTS) fluorescence assay for lipases and esterases using acyloxymethylethers of umbelliferone.
Esters and acyloxymethyl ethers of umbelliferone were evaluated as fluorogenic substrates for lipases and esterases with respect to stability and resistance to non-specific hydrolysis. Isobutyryloxymethyl ether 1c and pivaloxymethyl ether 1d were found to be optimal substrates for enzyme assays, particularly with respect to HTS applications.
Leroy
Emmanuel
E
Department of Chemistry & Biochemistry, University of Bern, Freiestrasse 3, 3012, Bern, Switzerland.
Bensel
Nicolas
N
Reymond
Jean Louis
JL
D004353:Drug Evaluation, Preclinical; D004950:Esterases / Q000378:metabolism*; D004987:Ethers / Q000138:chemical synthesis*; D005456:Fluorescent Dyes / Q000138:chemical synthesis*; D006868:Hydrolysis; D007700:Kinetics; D008049:Lipase / Q000378:metabolism*; D011549:Pseudomonas / Q000201:enzymology; D012710:Serum Albumin, Bovine / Q000737:chemistry; D013379:Substrate Specificity; D014468:Umbelliferones / Q000138:chemical synthesis*
D004987:Ethers; D005456:Fluorescent Dyes; D014468:Umbelliferones; D012710:Serum Albumin, Bovine; D004950:Esterases; D008049:Lipase