公开(公告)号：US4336186A

公开(公告)日：1982-06-22

申请号：US232942

申请日：1981-02-09

申请人： Robert J. Gargiulo ,  Gary A. Mitchell ,  Patricia M. Hudson ,  Sharon P. Pochron ,  Rolf M. Huseby ,  Robert E. Smith

发明人： Robert J. Gargiulo ,  Gary A. Mitchell ,  Patricia M. Hudson ,  Sharon P. Pochron ,  Rolf M. Huseby ,  Robert E. Smith

IPC分类号： C07K5/083 ,  C07K5/087 ,  C07K5/093 ,  C07K5/097 ,  C07K5/103 ,  C12Q1/37 ,  C12Q1/56 ,  C07C103/52

CPC分类号： C07K5/0823 ,  C07K5/0804 ,  C07K5/0812 ,  C07K5/0819 ,  C07K5/1013 ,  C12Q1/37 ,  C12Q1/56 ,  C12Q2337/10 ,  C12Q2337/30 ,  G01N2333/968 ,  G01N2333/974 ,  G01N2400/40 ,  Y10S530/802 ,  Y10S930/28

摘要： 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;R.sub.2 is hydrogen, phenyl, a straight, branched or cyclic alkyl having 1 to 4 carbons, or propionic acid;R.sub.3 is hydrogen, straight or branched or cyclic alkyl having 1 to 4 carbons, 4-aminobutane, or 3-guanidylpropane;R.sub.4 is methyl, 4-aminobutane, or 3-guanidylpropane;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.

摘要翻译： 用于具有下式的蛋白水解酶的荧光底物：其中：R 1是氢-L，氢-D，苯甲酰基，苯磺酰基，戊二酰基，焦谷氨酰基，苄氧羰基，D-丝氨酸或苄氧羰基丝氨酸; R2是氢，苯基，具有1-4个碳原子的直链，支链或环状烷基或丙酸; R3是氢，具有1至4个碳的直链或支链或环状烷基，4-氨基丁烷或3-胍基丙烷; R4是甲基，4-氨基丁烷或3-胍基丙烷; R5是荧光部分，当与所述化合物形成一部分时，所述化合物与蛋白水解酶可从所述化合物中分离，并且在从所述化合物切断时具有不同的荧光特性。 酶与底物反应时，除去荧光基团R5，产生荧光增加。 荧光的增加是酶存在的活性的指示。 因此可检测的特异性酶包括纤溶酶，凝血酶，因子Xa，XIa和XIIa，激肽释放酶，胰蛋白酶，弹性蛋白酶，尿激酶和组织蛋白酶B1。

公开(公告)号：US4275153A

公开(公告)日：1981-06-23

申请号：US930826

申请日：1978-08-03

申请人： Robert J. Gargiulo ,  Gary A. Mitchell ,  Patricia M. Hudson ,  Sharon P. Pochron ,  Rolf M. Huseby ,  Robert E. Smith

发明人： Robert J. Gargiulo ,  Gary A. Mitchell ,  Patricia M. Hudson ,  Sharon P. Pochron ,  Rolf M. Huseby ,  Robert E. Smith

IPC分类号： C07K5/083 ,  C07K5/087 ,  C07K5/093 ,  C07K5/097 ,  C07K5/103 ,  C12Q1/37 ,  C12Q1/56 ,  C12Q1/36 ,  C07G7/00 ,  C12Q1/38

CPC分类号： C07K5/0823 ,  C07K5/0804 ,  C07K5/0812 ,  C07K5/0819 ,  C07K5/1013 ,  C12Q1/37 ,  C12Q1/56 ,  C12Q2337/10 ,  C12Q2337/30 ,  G01N2333/968 ,  G01N2333/974 ,  G01N2400/40 ,  Y10S530/802 ,  Y10S930/28

摘要： 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;R.sub.2 is hydrogen, phenyl, a straight, branched or cyclic alkyl having 1 to 4 carbons, or propionic acid;R.sub.3 is hydrogen, straight or branched or cyclic alkyl having 1 to 4 carbons, 4-aminobutane, or 3-guanidylpropane;R.sub.4 is methyl, 4-aminobutane, or 3-guanidylpropane;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, & XII.sub.a, kallikrein, trypsin, elastase, urokinase, and cathepsin B.sub.1.

摘要翻译： 用于具有下式的蛋白水解酶的荧光底物：其中：R 1是氢-L，氢-D，苯甲酰基，苯磺酰基，戊二酰基，焦谷氨酰基，苄氧羰基，D-丝氨酸或苄氧羰基丝氨酸; R2是氢，苯基，具有1-4个碳原子的直链，支链或环状烷基或丙酸; R3是氢，具有1至4个碳的直链或支链或环状烷基，4-氨基丁烷或3-胍基丙烷; R4是甲基，4-氨基丁烷或3-胍基丙烷; R5是荧光部分，当与所述化合物形成一部分时，所述化合物与蛋白水解酶可从所述化合物中分离，并且在从所述化合物切断时具有不同的荧光特性。

公开(公告)号：US4167449A

公开(公告)日：1979-09-11

申请号：US822057

申请日：1977-08-05

申请人： Robert J. Gargiulo ,  Richard C. Driscoll

发明人： Robert J. Gargiulo ,  Richard C. Driscoll

IPC分类号： C07K5/06 ,  C12Q1/37 ,  C12Q1/48 ,  G01N31/14 ,  G01N33/16

CPC分类号： C12Q1/37 ,  C07K5/06026 ,  C12Q1/48 ,  C12Q2337/10

摘要： Transferase and protease activity in homogenates and biological solutions is fluorometrically determined at wavelengths corresponding generally to those used for fluorometric NADH-linked determinations by utilizing novel substrate compositions consisting essentially of certain fluorogenic 5-aminoisophthalic acid derivatives coupled to amino acid constituents specific to the transferases and proteases under investigation.

摘要翻译： 在匀浆和生物溶液中的转移酶和蛋白酶活性通过利用新型底物组合物来进行荧光测定，所述波长通常对应于用于荧光测定NADH的测定的波长，所述新型底物组合物基本上由与转移酶特异的氨基酸成分偶联的某些荧光5-氨基间苯二甲酸衍生物组成， 正在调查的蛋白酶。