Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA.
ChemMedChem. 2010 Feb 1;5(2):195-9. doi: 10.1002/cmdc.200900516.
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.
基于多种金属结合基团的螯合剂片段库针对金属蛋白酶进行了筛选。鉴定出先导化合物，并合成了选择化合物的扩展文库，得到了针对几种金属蛋白酶靶标的许多高亲和力化合物。研究结果清楚地表明，螯合剂可用于生成适用于基于片段的先导设计（FBLD）的文库，以针对重要的金属蛋白酶。
