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首页> 外文期刊>Journal of peptide science: An official publication of the European Peptide Society >Probing the structure-activity relationship of endogenous histone deacetylase complexes with immobilized peptide-inhibitors
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Probing the structure-activity relationship of endogenous histone deacetylase complexes with immobilized peptide-inhibitors

机译：探索内源性组蛋白脱乙酰酶复合物与固定化肽抑制剂的构效关系

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摘要

Histone deacetylases (HDACs) are key regulators of numerous cellular proteins by removing acetylation marks from modified lysine residues. Peptide-based HDAC probes containing alpha-aminosuberic acid omega-hydroxamate have been established as useful tools for investigating substrate selectivity and composition of endogenous HDAC complexes in cellular lysates. Here we report a structure-activity study of potential HDAC-probes containing derivatives of the hydroxamate moieties. While most of these probes did not recruit significant amounts of endogenous HDACs from cellular lysates, peptides containing N epsilon-acetyl-N epsilon-hydroxy-L-lysine served as HDAC probe. The recruitment efficiency varied between HDACs and was generally lower than that of alpha-aminosuberic acid omega-hydroxamate probes, but showed a similar global interaction profile. These findings indicate that N epsilon-acetyl-N epsilon-hydroxy-L-lysine might be a useful tool for investigations on HDAC complexes and the development of HDAC inhibitors. Copyright (C) 2016 European Peptide Society and John Wiley & Sons, Ltd.
机译：组蛋白脱乙酰基酶（HDAC）通过去除修饰的赖氨酸残基上的乙酰化标记，成为许多细胞蛋白的关键调节剂。已经建立了包含α-氨基磺酸ω-异羟肟酸酯的基于肽的HDAC探针，作为研究细胞裂解液中底物选择性和内源HDAC复合物组成的有用工具。在这里，我们报告潜在的HDAC探针包含异羟肟酸酯部分的衍生物的结构活性研究。尽管大多数这些探针没有从细胞裂解物中募集大量内源性HDAC，但是含有Nε-乙酰基-Nε-羟基-L-赖氨酸的肽用作HDAC探针。 HDAC之间的募集效率各不相同，通常低于α-氨基磺酸酸ω-异羟肟酸酯探针的募集效率，但显示出相似的全局相互作用曲线。这些发现表明，Nε-乙酰基-Nε-羟基-L-赖氨酸可能是研究HDAC复合物和开发HDAC抑制剂的有用工具。版权所有（C）2016欧洲肽学会和John Wiley＆Sons，Ltd.

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