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    • 5. 发明申请
    • A METHOD FOR THE PREPARATION OF IMAGING PROBES USING CLICK CHEMISTRY
    • 使用单一化学制备成像探针的方法
    • WO2006116736A3
    • 2007-02-01
    • PCT/US2006016428
    • 2006-04-27
    • SIEMENS MEDICAL SOLUTIONSKOLB HARTMUTH CMOCHARLA VANI PWALSH JOSEPH C
    • KOLB HARTMUTH CMOCHARLA VANI PWALSH JOSEPH C
    • G01N33/534G01N33/532
    • G01N33/532A61K51/0453A61K51/0455G01N33/533G01N33/534G01N2800/2821
    • The invention provides a method for identifying a candidate imaging probe, the method comprising: a) contacting a first library of candidate compounds with a target biomacromolecule, b) identifying a first member from the first library exhibiting affinity for the first binding site; c) contacting the first member identified from the first library affinity for the first binding site with the target biomacromolecule; d) contacting a second library of candidate compounds with the first member and the target biomacromolecule, e) reacting the complementary first functional group with the second functional group via a biomacromolecule induced click chemistry reaction to form the candidate imaging probe; f) isolating and identifying the candidate imaging probe; g) preparing the candidate imaging probe by chemical synthesis; and h) for imaging applications, converting the candidate imaging probe into an imaging probe.
    • 本发明提供了一种用于鉴定候选成像探针的方法,所述方法包括:a)使候选化合物的第一文库与靶生物大分子接触,b)鉴定第一个文库对第一结合位点表现出亲和性; c)将从第一文库鉴定的第一结合位点与第一结合位点接触的目标生物大分子; d)使候选化合物的第二文库与第一成员和靶生物大分子接触,e)通过生物大分子诱导的点击化学反应使互补的第一官能团与第二官能团反应以形成候选成像探针; f)分离和识别候选成像探针; g)通过化学合成制备候选成像探针; 和h)用于成像应用,将候选成像探针转换成成像探针。