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Machine translation
1. (WO1980000351) ANALYTICAL FLUOROGENIC SUBSTRATES FOR PROTEOLYTIC ENZYMES
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/1980/000351    International Application No.:    PCT/US1979/000421
Publication Date: 06.03.1980 International Filing Date: 15.06.1979
IPC:
C07K 5/083 (2006.01), C07K 5/087 (2006.01), C07K 5/093 (2006.01), C07K 5/097 (2006.01), C07K 5/103 (2006.01), C12Q 1/37 (2006.01), C12Q 1/56 (2006.01)
Applicants:
Inventors:
Priority Data:
930826 03.08.1978 US
Title (EN) ANALYTICAL FLUOROGENIC SUBSTRATES FOR PROTEOLYTIC ENZYMES
(FR) SUBSTRAT FLUOROGEE ANALYTIQUE POUR ENZYMES PROTEOLYTIQUES
Abstract: front page image
(EN)Fluorogenic substrates for proteolytic enzymes having the formula: (FORMULA) or acid salts thereof wherein: R1 is hydrogen-L, hydrogen-D, benzoyl, benzenesulfonyl, glutaryl, pyroglutamyl, carbobenzoxy, D-serine, or carbobenzoxyserine; R2 is hydrogen, phenyl, a straight, branched or cyclic alkyl having 1 to 4 carbons, or propionic acid; R3 is hydrogen, straight or branched or cyclic alkyl having 1 to 4 carbons, 4-aminobutane, or 3-guanidylpropane; R4 is methyl, 4-aminobutane, or 3-quanidylpropane; R5 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 R5 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 Xa, XIa, & XIIa, kallikrein, trypsin, elastase, urokinase, and cathepsin B1.
(FR)Substrats fluorogenes pour enzymes proteolytiques ayant la formule: (FORMULE) ou leurs sels acides ou: R1 est l"hydrogene-L, l"hydrogene-D, le benzoyle, le benzene-sulfonyle, le glutaryle, le pyroglutamyle, le carbobenzoxy, la D-serine, ou la carbobenzoxyserine; R2 est l"hydrogene, la phenyle, un alkyle lineaire ramifie ou cyclique ayant 1 a 4 atomes de carbone, ou l"acide propionique; R3 est l"hydrogene, un alkyle lineaire ou ramifie ou cyclique ayant 1 a 4 atomes de carbone, 4-aminobutane, ou 3-guanidylpropane; R4 est le methyle, 4-aminobutane, ou 3-guanidylpropane; R5 est une fraction fluorogenique, separable dudit compose par un enzyme proteolytique et ayant une propriete fluorescente differente lorsqu"elle est separee dudit compose que lorsqu"elle en fait partie. Les enzymes lorsqu"ils reagissent avec le substrat, enlevent le groupe fluorogene R5 produisant une augmentation de sa fluorescence. L"augmentation de la fluorescence est une indication de l"activite de l"enzyme present. Des enzymes specifiques ainsi detectables comprennent la plasmine, la thrombine, les facteurs Xa, XIa, & XIIa, la callicreine, la trypsine, l"elastase, l"uroquinase, et la cathepsine B1.
Designated States:
Publication Language: English (EN)
Filing Language: English (EN)