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    Method for producing and screening mass-coded combinatorial libraries for drug discovery and target validation
    6.
    发明申请
    Method for producing and screening mass-coded combinatorial libraries for drug discovery and target validation 审中-公开
    用于生产和筛选用于药物发现和目标验证的大规模组合文库的方法

    公开(公告)号：US20060063169A1

    公开(公告)日：2006-03-23

    申请号：US11061499

    申请日：2005-02-18

    申请人： Huw Nash ,  Seth Birnbaum ,  Edward Wintner ,  Krishna Kalghatgi ,  Gerald Shipps ,  Satish Jindal

    发明人： Huw Nash ,  Seth Birnbaum ,  Edward Wintner ,  Krishna Kalghatgi ,  Gerald Shipps ,  Satish Jindal

    IPC分类号： C40B40/08 ,  C40B40/10

    CPC分类号： G01N33/6845 ,  B01J19/0046 ,  B01J2219/00581 ,  B01J2219/00585 ,  B01J2219/00596 ,  B01J2219/00599 ,  B01J2219/00695 ,  B01J2219/00722 ,  B01J2219/00725 ,  C40B20/04 ,  C40B30/10 ,  C40B40/06 ,  C40B70/00 ,  G01N33/6848 ,  G01N2458/15

    摘要： The present invention provides a method for producing a mass-coded combinatorial library comprising a set of compounds having the general formula X(Y)n, where X is a scaffold, each Y is, independently, a peripheral moiety, and n is an integer greater than 1. The method comprises selecting a peripheral moiety precursor subset from a peripheral moiety precursor set. The subset includes a sufficient number of peripheral moiety precursors that at least about 50 distinct combinations of n peripheral moieties derived from the peripheral moiety precursors in the subset exist. The subset of peripheral moiety precursors is selected so that at least about 90% of all possible combinations of n peripheral moieties derived from the subset have a molecular mass sum which is distinct from the molecular mass sums of all of the other combinations of n peripheral moieties. The method further comprises contacting the peripheral moiety precursor subset with a scaffold precursor which has n reactive groups. Methods of use of the mass-coded combinatorial library produced by this method for identifying a ligand to a particular biomolecule are also disclosed.

    摘要翻译： 本发明提供一种生产大量编码的组合文库的方法，该组合文库包含一组具有通式X（Y）N n的化合物，其中X是支架，每个Y独立地是外周 部分，并且n是大于1的整数。该方法包括从外周部分前体组选择外周部分前体子集。 该子集包括足够数量的外周部分前体，其存在衍生自该子集中的外周部分前体的n个外周部分的至少约50个不同组合。 选择外周部分前体的子集，使得衍生自子集的n个外围部分的所有可能组合的至少约90％具有不同于n个外围部分的所有其它组合的分子质量和的分子质量和 。 该方法还包括使外周部分前体子集与具有n个反应性基团的支架前体接触。 还公开了通过该方法产生的用于鉴定特定生物分子的配体产生的批量编码的组合文库的方法。