[EN] NITROXIDES FOR USE AS CONTRAST AGENTS FOR OVERHAUSER MAGNETIC RESONANCE IMAGING (OMRI)<br/>[FR] NITROXYDES DESTINÉS À ÊTRE UTILISÉS COMME AGENTS DE CONTRASTE POUR L'IMAGERIE PAR RÉSONANCE MAGNÉTIQUE OVERHAUSER (OMRI)
申请人:UNIV AIX MARSEILLE
公开号:WO2017005879A1
公开(公告)日:2017-01-12
The present invention relates to an in vitro method for detecting and/ or quantifying the catalytic activity of an enzyme E, said method comprising the steps of: i) Contacting enzyme E with a compound of formula (la), or (lb): ii) Monitoring the conversion of compound (la) or (lb) into compound (IlIa) or (lllb) by Electron Paramagnetic Resonance (EPR) or Overhauser-enhanced Magnetic Resonance Imaging (OMRI), or by Proton Electron Double Resonance Imaging (PEDRI) thereby detecting or quantifying the activity of enzyme E wherein: Y is OC(=O), S(C=O), NR7; X is CH or N; R1, R2, R3, are each independently selected from C1-C6 alkyl optionally substituted by OH, NRe, COOH; R4, R5 are each independently selected from H, C1-C6 alkyl, C1-C6 alkoxy, NR8R9, SR10;R6 is H or C1-C6 alkyl; ==W is =W or is absent; W is O, S, or NR11; R7, R8, R9, R10, R11 are each independently selected from C1-C6 alkyl; n is 0, 1, 2 or 3, Z is a substrate residue of an enzyme E.
本发明涉及一种体外方法,用于检测和/或定量酶E的催化活性,所述方法包括以下步骤:i) 将酶E与化合物(la)或(lb)的公式接触;ii) 通过电子顺磁共振(EPR)或Overhauser增强磁共振成像(OMRI),或通过质子电子双共振成像(PEDRI)监测化合物(la)或(lb)转化为化合物(IIIa)或(IIIb),从而检测或定量酶E的活性,其中:Y为OC(=O),S(C=O),NR7;X为CH或N;R1、R2、R3分别独立选择自C1-C6烷基,可选择性地被OH,NRe,COOH取代;R4、R5分别独立选择自H,C1-C6烷基,C1-C6烷氧基,NR8R9,SR10;R6为H或C1-C6烷基;==W为=W或不存在;W为O,S或NR11;R7、R8、R9、R10、R11分别独立选择自C1-C6烷基;n为0,1,2或3,Z为酶E的底物残基。