A selective inhibitor of SIRT1 over SIRT2 and SIRT3
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Free Base
REVIEW 6-Chloro-2,3,4,9-tetrahydro-1H-carbazole-1-carboxamide is a potent and selective deacetylase sirtin 1 (SIRT1) inhibitor that has shown benefit across a range of preclinical models for Huntingdon''s Disease. The compound has become a useful tool for studying the relationship between SIRT1 and cell regulation as well as a potential agent for the treatment of Huntington's Disease.
REFERENCES
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Sakkiah, Sugunadevi; Baek, Ayoung; Lee, Keun Woo. Pharmacophore modeling and molecular dynamics simulation to identify the critical chemical features against human sirtuin 2 inhibitors. Journal of Molecular Structure. (2012) 1011: 66-75.
[2]
Napper, Andrew D.; Hixon, Jeffrey; McDonagh, Thomas; Keavey, Kenneth; Pons, Jean-Francois; Barker, Jonathan; Yau, Wei Tsung; Amouzegh, Patricia; Flegg, Adam; Hamelin, Estelle; et al. Discovery of indoles as potent and selective inhibitors of the deacetylase SIRT1. Journal of Medicinal Chemistry. (2005) 48(25): 8045-8054.
[3]
'Smith MR, Syed A, Lukacsovich T, Purcell J, Barbaro BA, Worthge SA, Wei SR, Pollio G, Magnoni L, Scali C, Massai L, Franceschini D, Camarri M, Gianfriddo M, Diodato E, Thomas R, Gokce O, Tabrizi SJ, Caricasole A, Landwehrmeyer B, Menalled L, Murphy C, Ramboz S, Luthi-Carter R, Westerberg G, Marsh JL. A potent and selective Sirtuin 1 inhibitor alleviates pathology in multiple animal and cell models of Huntington''s disease. Hum Mol Genet. (2014) Jan 29.'
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