[EN] FLUOROGENIC DIMER COMPOUND, USEFUL AS A PROBE FOR DETECTION OF ENDOGENOUS RECEPTORS<br/>[FR] COMPOSÉ DIMÈRE FLUOROGÈNE UTILE EN TANT QUE SONDE POUR LA DÉTECTION DE RÉCEPTEURS ENDOGÈNES
申请人:UNIV STRASBOURG
公开号:WO2021228939A1
公开(公告)日:2021-11-18
The present disclosure relates to a novel fluorogenic dimer compound, useful as a probe for detection of endogenous receptors, in particular G protein-coupled receptors. The present invention provides compositions and kits comprising such compound and methods of labeling a biomolecule, comprising the step of contacting the biomolecule with the compound of the invention. The compound is a fluorogenic dimer with two cyanine moieties (D), which is represented by the following formula (1): D-L-D (1); where (D) is represented by the following formula (I) or (I'): (formula (I) or (I')) wherein: (A) has the following formula: formula (A), (B) has the following formula: formula (B) where the dashed lines are present or not, and, when they are present, they represent single or double carbon bond. L is a saturated or unsaturated hydrocarbon group presenting three extremities and comprising from 2 to 40, preferably from 2 to 30, carbon atoms, where two extremities of said linker L are covalently bond to both cyanine moieties of formulae (I) or (I'), via both R1, and the third extremity is the remainder of the saturated or unsaturated hydrocarbon group and comprises a reactive group or is attached to a ligand.
本公开涉及一种新型荧光二聚物化合物,可用作探针检测内源性受体,特别是G蛋白偶联受体。本发明提供了包括该化合物的组合物和试剂盒以及标记生物分子的方法,其中包括将该发明的化合物与生物分子接触的步骤。该化合物是一种带有两个青霉烷基团(D)的荧光二聚体,由以下式子(1)表示:D-L-D(1);其中(D)由以下式子(I)或(I')表示:(式子(I)或(I')),其中:(A)具有以下式子:式子(A),(B)具有以下式子:式子(B),虚线存在或不存在,当存在时,它们表示单个或双键。L是一个饱和或不饱和的碳氢基团,具有三个端点,并且包含2到40个碳原子,优选2到30个碳原子,其中所述连接剂L的两个端部通过R1共价键连接到式(I)或(I')的两个青霉烷基团,第三个端部是饱和或不饱和的碳氢基团的剩余部分,并且包含反应性基团或连接到配体。