Jamonnak Nuttara, Fatkins David G, Wei Lanlan, Zheng Weiping
Department of Chemistry, University of Akron, 190 E. Buchtel Commons, Akron, OH 44325, USA.
Org Biomol Chem. 2007 Mar 21;5(6):892-6. doi: 10.1039/b617185k. Epub 2007 Feb 5.
Through parallel studies on peptides containing N(epsilon)-methanesulfonyl-lysine or N(epsilon)-acetyl-lysine, N(epsilon)-methanesulfonyl-lysine as a replacement for N(epsilon)-acetyl-lysine was shown i) not to compromise the binding affinity for a bromodomain, ii) to confer resistance to human HDAC8 and SIRT1 (two distinct protein deacetylases), and iii) to confer only weak inhibition against human HDAC8 and SIRT1. These results suggested N(epsilon)-methanesulfonyl-lysine as a non-hydrolyzable functional surrogate for N(epsilon)-acetyl-lysine.
通过对含有N(ε)-甲磺酰基赖氨酸或N(ε)-乙酰基赖氨酸的肽进行平行研究，结果表明，用N(ε)-甲磺酰基赖氨酸替代N(ε)-乙酰基赖氨酸：i) 不会损害对溴结构域的结合亲和力；ii) 赋予对人HDAC8和SIRT1（两种不同的蛋白质脱乙酰酶）的抗性；iii) 仅对人HDAC8和SIRT1产生微弱抑制作用。这些结果表明N(ε)-甲磺酰基赖氨酸可作为N(ε)-乙酰基赖氨酸的不可水解功能替代物。
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