Chelator fragment libraries for targeting metalloproteinases.

Chelator fragment libraries for targeting metalloproteinases.
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DOI:
10.1002/cmdc.200900516
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发表时间:
2010-02-01
期刊:
影响因子:
3.4
通讯作者:
Cohen, Seth M.
Cohen, Seth M.
中科院分区:
医学4区
文献类型:
--
作者:
Agrawal, Arpita;Johnson, Sherida L.;Jacobsen, Jennifer A.;Miller, Melissa T.;Chen, Li-Hsing;Pellecchia, Maurizio;Cohen, Seth M.

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基于多种金属结合基团的螯合剂片段文库针对金属蛋白酶进行筛选。铅命中鉴定和选择化合物的扩大库合成,导致许多高亲和力命中几个金属蛋白质的目标。研究结果清楚地表明,螯合剂可用于产生适合于针对重要金属蛋白的基于片段的先导设计(FBLD)的文库。
A chelator fragment library based on a variety of metal binding groups was screened against a metalloproteinase. Lead hits were identified and an expanded library of select compounds was synthesized, resulting in numerous high-affinity hits against several metalloprotein targets. The findings clearly demonstrate that chelators can be used to generate libraries suitable for fragment-based lead design (FBLD) directed at important metalloproteins.
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