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    • 6. 发明申请
    • IDENTIFICATION OF DRUGS USING COMPLEMENTARY COMBINATORIAL LIBRARIES
    • 使用补充组合图书馆鉴定药物
    • WO1998019162A1
    • 1998-05-07
    • PCT/US1997019638
    • 1997-10-31
    • NOVALON PHARMACEUTICAL CORPORATIONFOWLKES, Dana, M.KAY, Brian, K.FRELINGER, Jeffrey, A.HYDE-DERUYSCHER, Robin, Parish
    • NOVALON PHARMACEUTICAL CORPORATION
    • G01N33/53
    • C07K1/047G01N33/53
    • The present invention is directed to the identification of compounds in a compound library which can mediate the biological activity of a target receptor protein, even when the ligands which mediate that activity through binding to that receptor are not already known. The method comprises three steps: (1) Screen at least one potential surrogate combinatorial library for members (preferably peptides or nucleic acids) binding to the target protein (TP) and hence capable of use as surrogates for the unknown ligand in steps (2) and (3). (2) Screen at least one complementary library, preferably a combinatorial library (which is not limited to, and may not even include, peptides, or nucleic acids and hence is referred to on occasion as a "compound library"), for compounds which inhibit the binding of one or more surrogates from step (1) to TP, and, optionally, (3) determine whether the inhibitory compound mediates the biological activity of the said TP.
    • 本发明涉及可以介导靶受体蛋白的生物活性的化合物文库中的化合物的鉴定,即使当通过结合该受体介导该活性的配体不是已知的时。 该方法包括三个步骤:(1)筛选结合靶蛋白(TP)并因此能够用作步骤(2)中未知配体的替代物的成员(优选肽或核酸)的至少一个潜在替代组合文库, 和(3)。 (2)筛选至少一个互补文库,优选组合文库(其不限于,甚至可以不包括肽或核酸,因此有时称为“化合物文库”),对于化合物 抑制来自步骤(1)的一种或多种替代物与TP的结合,以及任选地(3)确定抑制性化合物是否介导所述TP的生物活性。