A mechanism-based potent sirtuin inhibitor containing Nε-thiocarbamoyl-lysine (TuAcK)
作者： Brett M. Hirsch , Yujun Hao , Xiaopeng Li , Chrys Wesdemiotis , Zhenghe Wang
DOI: 10.1016/J.BMCL.2011.06.069
关键词:
摘要: In the current study, we have identified Ne-thiocarbamoyl-lysine (TuAcK) as a general sirtuin inhibitory warhead which was shown to be able confer potent inhibition. This inhibition also mechanism-based in that TuAck residue processed by enzyme with formation of stalled S-alkylamidate intermediate.
elsevier.com
sci-hub.se 参考文章(62)
M Wasil, B Halliwell, M Grootveld, C P Moorhouse, D C S Hutchison, H Baum, The specificity of thiourea, dimethylthiourea and dimethyl sulphoxide as scavengers of hydroxyl radicals. Their protection of alpha 1-antiproteinase against inactivation by hypochlorous acid. Biochemical Journal. ,vol. 243, pp. 867- 870 ,(1987) , 10.1042/BJ2430867
Donald A. Wellings, Eric Atherton, Standard Fmoc protocols. Methods in Enzymology. ,vol. 289, pp. 44- 67 ,(1997) , 10.1016/S0076-6879(97)89043-X
Bertram G. Katzung, Basic And Clinical Pharmacology ,(1982)
Hui Nie, Weihai Ying, Heyu Chen, Jin Han, Weiliang Xia, Yingxin Ma, Yunyi Hong, Silencing of SIRT2 induces cell death and a decrease in the intracellular ATP level of PC12 cells. International journal of physiology, pathophysiology and pharmacology. ,vol. 3, pp. 65- 70 ,(2011)
M. Dixon, The determination of enzyme inhibitor constants Biochemical Journal. ,vol. 55, pp. 170- 171 ,(1953) , 10.1042/BJ0550170
David J Bonda, Hyoung-gon Lee, Antoni Camins, Mercè Pallàs, Gemma Casadesus, Mark A Smith, Xiongwei Zhu, The sirtuin pathway in ageing and Alzheimer disease: mechanistic and therapeutic considerations Lancet Neurology. ,vol. 10, pp. 275- 279 ,(2011) , 10.1016/S1474-4422(11)70013-8
Mahadevan Lakshminarasimhan, Clemens Steegborn, Emerging mitochondrial signaling mechanisms in physiology, aging processes, and as drug targets. Experimental Gerontology. ,vol. 46, pp. 174- 177 ,(2011) , 10.1016/J.EXGER.2010.08.024
Anthony A. Sauve, Sirtuin Chemical Mechanisms Biochimica et Biophysica Acta. ,vol. 1804, pp. 1591- 1603 ,(2010) , 10.1016/J.BBAPAP.2010.01.021
Fei Wang, Margaret Nguyen, F. Xiao-Feng Qin, Qiang Tong, SIRT2 deacetylates FOXO3a in response to oxidative stress and caloric restriction Aging Cell. ,vol. 6, pp. 505- 514 ,(2007) , 10.1111/J.1474-9726.2007.00304.X
Anthony Sauve, Pharmaceutical Strategies for Activating Sirtuins Current Pharmaceutical Design. ,vol. 15, pp. 45- 56 ,(2009) , 10.2174/138161209787185797