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ENZYME SUBSTRATES FOR THE DETERMINATION OF ACTIVITY OF STAPHYLOCOCCUS SP. EXTRACELLULAR PROTEASE

机译:酶基质测定葡萄球菌SP的活性。胞外蛋白酶

摘要

Compounds of general formula (I): A) A compound of general formula (I) Y-AA1-AA2-AA3-AA4-R-Glu-NH2, Y-A1-A2-A3-A4-R-Glu-NH2 wherein Y and R are reporter groups; A1 is either the D-isomer or the L-isomer form of isoleucine; each of A2 and A3 is independently Ala or 2-aminobutyric acid (Abu); A4 is Pro, L-3-hydroxyproline (Pro(3-OH)), L-4-hydroxyproline (Pro (4-OH)), L-tetrahydroisoquinoline-1-carboxylic acid (THIQ), L-tetrahydroisoquinoline-3-carboxylic acid (Tic), L-pipecolic acid (Pip), 1-amino-1-cyclopentane carboxylic acid (1-ACP) or D-Pro; and any one of A1, A2, A3 and A4 can be replaced by any other amino acid group (Xaa); and the other protein based substrates are cleavable by Staphyococcus sp. extracellular cysteine protease and are therefore likely to be of use in monitoring enzyme activity for purposes such as investigating candidate enzyme modulators and screening for therapeutic agents.
机译:通式(I)的化合物:A)通式(I)的化合物Y-AA1-AA2-AA3-AA4-R-Glu-NH2,Y-A1-A2-A3-A4-R-Glu-NH2,其中Y和R是报告者组; A1是异亮氨酸的D-异构体或L-异构体形式; A2和A3各自独立地为Ala或2-氨基丁酸(Abu); A4是脯氨酸,L-3-羟基脯氨酸(Pro(3-OH)),L-4-羟基脯氨酸(Pro(4-OH)),L-四氢异喹啉-1-羧酸(THIQ),L-四氢异喹啉-3-羧酸(Tic),L-哌酸(Pip),1-氨基-1-环戊烷羧酸(1-ACP)或D-Pro; A1,A2,A3和A4中的任何一个可以被任何其他氨基酸基团(Xaa)取代;其他基于蛋白质的底物可被葡萄球菌(Staphyococcus sp。)裂解。细胞外半胱氨酸蛋白酶,因此可能用于监测酶活性,以用于诸如研究候选酶调节剂和筛选治疗剂的目的。

著录项

  • 公开/公告号WO03062267A3

    专利类型

  • 公开/公告日2003-09-04

    原文格式PDF

  • 申请/专利权人 AMURA THERAPEUTICS LIMITED;RAMJEE MANOJ KUMAR;

    申请/专利号WO2003GB00120

  • 发明设计人 RAMJEE MANOJ KUMAR;

    申请日2003-01-16

  • 分类号C07K7/06;C07K5/06;C12Q1/37;

  • 国家 WO

  • 入库时间 2022-08-21 23:52:06

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