Fluorescent ligands for GPCR arrays
    1.
    发明申请
    Fluorescent ligands for GPCR arrays 审中-公开
    GPCR阵列的荧光配体

    公开(公告)号:US20060148101A1

    公开(公告)日:2006-07-06

    申请号:US11363400

    申请日:2006-02-27

    IPC分类号: G01N33/543

    摘要: Microarrays employing a fluorescent ligand including 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 includes 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.

    摘要翻译: 使用荧光配体的微阵列,其包括具有约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。

    Fluorescent ligands for GPCR arrays
    2.
    发明申请
    Fluorescent ligands for GPCR arrays 审中-公开
    GPCR阵列的荧光配体

    公开(公告)号:US20070238197A9

    公开(公告)日:2007-10-11

    申请号:US11363400

    申请日:2006-02-27

    IPC分类号: G01N33/543

    摘要: Microarrays employing a fluorescent ligand including 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 includes 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.

    摘要翻译: 使用荧光配体的微阵列,其包括具有约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。