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2. 发明申请

WO0218946A3 IMMOBILISED PHOSPHATIDIC ACID PROBE 审中-公开
标题翻译：固定化磷酸探针
公开(公告)号：WO0218946A3
公开(公告)日：2002-10-24
申请号：PCT/GB0103791
申请日：2001-08-23
申请人： BABRAHAM INST , UNIV CAMBRIDGE TECH , STEPHENS LEN , HAWKINS PHILLIP THOMAS , HOLMES ANDREW BRUCE , MANIFAVA MARIA , LIM ZE YI , KTISTAKIS NICHOLAS , THURING JOHANNES WILHELMUS JOH
发明人： STEPHENS LEN , HAWKINS PHILLIP THOMAS , HOLMES ANDREW BRUCE , MANIFAVA MARIA , KTISTAKIS NICHOLAS , THURING JOHANNES WILHELMUS JOH
IPC分类号： G01N33/543 , G01N33/68 , G01N33/53
CPC分类号： G01N33/54353 , G01N33/68
摘要： Probes comprising an immobilised Phosphatidic Acid attached onto a solid support are described, for example, as shown in formula (I) and (V): (a) the linker consists of aryl, heteroaryl, alkyl with possible heteroatoms and/or unsaturations, preferably chains of (CH2)n, with n = 8-20, most preferably n = 11; (b) the heteroatom X maybe O, S, or most preferably NH; (c) the functional group (FG) is a carbonyl from a carboxylate (thiolo)ester, or, most preferably an amide; (d) the R-substituent carries an aryl, alkyl group, or a combination, preferably R=CmH2m+1, m = 8-20, m = 16 optimal; (e) the ion M represents any cation, preferably Na , NH4+; (f) unsaturations are allowed, such as in an arachidonyl side chain and (g) = solid support with attachment to functional group. where: R = aryl, alkyl group, or a combination, preferably R = CmH2m+1, m = 8-20, m = 16 is optimal. R3 is P(O)(OM)2; R5 = H(PI(3)P); R3 = H; R4 = P(O)(OM)2; R5 = H(PI(4)P); R3 = H; R4 = H; R5 = P(O)(OM)2 (PI(5)P); R3 = P(O)(OM)2; R4 = P(O)(OM)2; R5 = H(PI(3,4)P2); R3 = P(O)(OM)2; R4 = H; R5 = P(O)(OM)2 (PI(3,5)P2); R3 = H; R4 = P(O)(OM)2; R5 = P(O)(OM)2 (PI(4,5)P2); or R3 = P(O)(OM)2; R4 = P(O)(OM)2; R5 P(O)(OM)2 (PI(3,4,5)P3). M = any cation, preferably Na , NH4 *Denotes a stereogenic centre. More preferably a stereogenic centre with an R absolute configuration. Linker = aryl, heteroaryl, alkyl with possible heteroatoms and/or unsaturations. Preferably chains of (CH2)n with n = 8-20, most preferably n = 11. X = O, S, or, most preferably NH. FG = Carbonyl from a carboxylate, thiolo(ester), or, most preferably an amide. Unsaturations are allowed, such as in an arachidonyl side chain. = solid support with attachment to functional group. Use of the probes to identify Phosphatidic Acid binding protein or phosphoinositide binding proteins is also described.
摘要翻译：例如，如式（I）和（V）所示，包含固定在固体载体上的固定化磷脂酸的探针：（a）连接体由芳基，杂芳基，可能的杂原子和/或不饱和基团（CH 2）n的链，n = 8-20，最优选n = 11; （b）杂原子X可以是O，S，或最优选NH; （c）官能团（FG）是羧酸酯（thiolo）酯的羰基，或最优选酰胺; （d）R取代基带有芳基，烷基或组合，优选R = CmH2m + 1，m = 8-20，m = 16最优; （e）离子M表示任何阳离子，优选Na +，NH 4 +; （f）允许不饱和度，例如在花生四烯酰侧链中，（g）=与官能团连接的固体支持物。其中：R =芳基，烷基或组合，优选R = CmH2m + 1，m = 8-20，m = 16是最佳的。 R3是P（O）（OM）2; R5 = H（PI（3）P）; R3 = H; R4 = P（O）（OM）2; R5 = H（PI（4）P）; R3 = H; R4 = H; R5 = P（O）（OM）2（PI（5）P）; R3 = P（O）（OM）2; R4 = P（O）（OM）2; R5 = H（PI（3,4）P2）; R3 = P（O）（OM）2; R4 = H; R5 = P（O）（OM）2（PI（3,5）P2）; R3 = H; R4 = P（O）（OM）2; R5 = P（O）（OM）2（PI（4,5）P2）; 或R3 = P（O）（OM）2; R4 = P（O）（OM）2; R5 P（O）（OM）2（PI（3,4,5）P3）。 M =任何阳离子，优选Na +，NH 4 + *表示立体中心。更优选具有R绝对构型的立体中心。连接子=芳基，杂芳基，具有可能的杂原子和/或不饱和基团的烷基。优选（CH 2）n的链，n = 8-20，最优选n = 11.X = O，S，或最优选NH。 FG =羧酸羰基，硫代（酯），或最优选酰胺。允许不饱和度，例如在花生四烯酸侧链中。 =与功能基团相连的固体支持物。还描述了使用探针来鉴定磷脂酸结合蛋白或磷酸肌醇结合蛋白。

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