Chemical microarrays: a new tool for discovery enzyme inhibitors.

Chemical microarrays: a new tool for discovery enzyme inhibitors.
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化学微阵列:发现酶抑制剂的新工具。

DOI:
10.1007/978-1-60761-244-5_9
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发表时间:
2009
期刊:
Methods in molecular biology (Clifton, N.J.)
影响因子:
--
通讯作者:
Ma,Haiching
Ma,Haiching
中科院分区:
--
文献类型:
--
作者:
Liang,Shuguang;Xu,Wei;Horiuchi,KurumiY;Wang,Yuan;Ma,Haiching

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酶,催化蛋白质,在调节基本细胞功能中起着关键作用。抑制酶活性的药物涵盖疾病的各个方面,并提供潜在的治疗方法。高通量筛选是药物发现行业中用于寻找酶抑制剂的主要技术之一,由于基因组和蛋白质组学研究产生的药物靶标数量快速增长以及高通量合成产生的大型化学文库,高通量筛选面临着艰巨的挑战。化学微阵列作为一种新技术,可以用最少的材料同时筛选出更多的化合物,从而降低成本,提高生产率,是传统的基于井的筛选的一种很好的替代方法。在这一章中,我们介绍了化学微阵列的基本技术和应用,以及如何常规地使用它们来识别基于功能的分析的酶抑制剂。激酶,蛋白酶,组蛋白脱乙酰酶和磷酸酶的样品测定证明。
Enzymes, the catalytic proteins, are playing pivotal roles in regulating basic cell functions. Drugs that inhibit enzyme activities cover varying aspects of diseases and offer potential cures. One of the major technologies used in the drug discovery industry for finding the enzyme inhibitors is high-throughput screening, which is facing a daunting challenge due to the fast-growing numbers of drug targets arising from genomic and proteomic research and the large chemical libraries generated from high-throughput synthesis. Chemical microarray, as a new technology, could be an excellent alternative for traditional well-based screening, since the technology can screen more compounds against more targets in parallel with a minimum amount of materials, reducing cost and increasing productivity. In this chapter, we have introduced the basic techniques and applications of chemical microarrays, and how to use them routinely for identifying enzyme inhibitors with functional-based assays. Sample assays for kinases, proteases, histone deacetylases, and phosphatases are demonstrated.
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