Analytical fluorogenic substrates for proteolytic enzymes
US4336186A · kind A · utility
Inventors
Key dates
| Filing date | Feb 9, 1981 |
| Grant date | Jun 22, 1982 |
| Priority date | — |
| Expiry date | Feb 9, 2001 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY10S930/28
- WIPO fieldBiotechnology
- WIPO sectorChemistry
Abstract
Fluorogenic substrates for proteolytic enzymes having the formula: ##STR1## or acid salts thereof wherein: R.sub.1 is hydrogen-L, hydrogen-D, benzoyl, benzenesulfonyl, glutaryl, pyroglutamyl, carbobenzoxy, D-serine, or carbobenzoxy-serine; PA1 R.sub.2 is hydrogen, phenyl, a straight, branched or cyclic alkyl having 1 to 4 carbons, or propionic acid; PA1 R.sub.3 is hydrogen, straight or branched or cyclic alkyl having 1 to 4 carbons, 4-aminobutane, or 3-guanidylpropane; PA1 R.sub.4 is methyl, 4-aminobutane, or 3-guanidylpropane; PA1 R.sub.5 is a fluorogenic moiety, severable from said compound by a proteolytic enzyme and having different fluorescent property when severed from said compound than when forming part of said compound. The enzymes, when reacting with the substrate, remove the fluorogenic group R.sub.5 producing an increase in its fluorescence. The increase of the fluorescence is an indication of the activity of the enzyme present. Specific enzymes thusly detectable include plasmin, thrombin, the factors X.sub.a, XI.sub.a, and XII.sub.a, kallikrein, trypsin, elastase, urokinase, and cathepsin B.sub.1.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.