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    • 5. 发明申请
    • FLUORESCENT LIGANDS FOR GPCR ARRAYS
    • 用于GPCR阵列的荧光配体
    • WO2005066633A2
    • 2005-07-21
    • PCT/US2004/041935
    • 2004-12-13
    • CORNING INCORPORATEDFANG, YeHONG, YulongPENG, Jinlin
    • FANG, YeHONG, YulongPENG, Jinlin
    • G01N33/543
    • G01N33/582C07K7/083C07K14/63G01N33/6845G01N33/74G01N2333/63G01N2333/726
    • A fluorescent ligand includes a material having a binding affinity in the range of about 0.01 to about 25 nM, or about 0.1 to about 10 nM; a specificity to its cognate receptor in the range of about 50 to about 99%, or about 65 to about 99%; a cross-activity to other receptors of 0 to about 20%, or 0 to about 10%; a net charge per ligand of about -3 to about +5, or more preferably, about -2 to about +2 or most preferably for small compound ligands about -1 to about +2. The ligand may also have a hydrophobicity in the range of about 3 to about 55 minutes eluting time (as measured under specified eluting conditions) . In some embodiments, the ligand including fluorescently labeled motilin 1-16 labeled with Bodipy-TMR, rhodamine or Cy5-. Other embodiments include fluorescently labeled Cy5-naltrexone, Cy5-neurotensin 2-13, N-terminal labeled neurotensin 2-13 or lys-labeled labeled neurotensin 2-13.
    • 荧光配体包括具有约0.01至约25nM,或约0.1至约10nM范围内的结合亲和力的材料; 在约50至约99%,或约65至约99%的范围内对其同源受体的特异性; 与其他受体的交叉活性为0至约20%,或0至约10%; 每个配体的净电荷为约-3至约+5,或更优选约-2至约+2,或最优选约为-1至约+2的小化合物配体。 配体还可以具有约3至约55分钟洗脱时间(在规定的洗脱条件下测量)的疏水性。 在一些实施方案中,配体包括用Bodipy-TMR,罗丹明或Cy5-标记的荧光标记的胃动素1-16。 其他实施方案包括荧光标记的Cy5-纳曲酮,Cy5-神经丝氨酸2-13,N-末端标记的神经丝氨酸蛋白酶2-13或lys-标记的标记的神经丝氨酸素2-13。