Transcreener™:: screening enzymes involved in covalent regulation
Transcreener™:: screening enzymes involved in covalent regulation
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DOI：
10.1517/14728222.10.1.179
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发表时间：
2006-02-01
影响因子：
5.8
通讯作者：
Kleman-Leyer, K
中科院分区：
文献类型：
--
作者：
Lowery, RG;Kleman-Leyer, K
催化基团转移反应的酶占人类蛋白质组的很大一部分，并且由于它们在共价调节循环中的作用而成为药物靶标的丰富来源。磷酸化、糖基化、磺化、甲基化和乙酰化代表了通过共价修饰调节不同生物分子功能的一些关键类型的基团转移反应。由于受体底物的多样性，开发这些酶的高通量筛选方法一直存在问题。最近，作者开发了一种名为 Transcreener (TM) 的新型检测平台，该平台依赖于基团转移反应的不变反应产物（通常是核苷酸）的荧光检测。该平台能够使用相同的检测试剂，使用任何受体底物筛选基团转移酶家族中的任何异构体。
Enzymes that catalyse group transfer reactions comprise a significant fraction of the human proteome and are a rich source of drug targets because of their role in covalent regulatory cycles. Phosphorylation, glycosylation, sulfonation, methylation and acetylation represent some of the key types of group transfer reactions that modulate the function of diverse biomolecules through covalent modification. Development of high-throughput screening methods for these enzymes has been problematic because of the diversity of acceptor substrates. Recently, the authors developed a novel assay platform called Transcreener (TM) that relies upon fluorescence detection of the invariant reaction product of a group transfer reaction, usually a nucleotide. This platform enables screening of any isoform in a family of group transfer enzymes, with any acceptor substrate, using the same assay reagents.