Abstract
We have identified SRT2104 (4) as the first direct synthetic SIRT1 activator clinical candidate. The compound was derived from the optimization of a previously described imidazo[1,2-b]thiazole scaffold. SRT2104 was selected as a development candidate based on a combination of biochemical activity and pharmacokinetic profile. The in vivo characteristics of SRT2104 were superior to those of analogues with similar activation profiles. The overall preclinical profile suggests that the compound has potential to provide therapeutic benefit in a clinical setting.
Keywords: Activator, Imidazothiazole, SIRT1, Sirtuin, SRT1720, SRT2104.
Letters in Drug Design & Discovery
Title:The Identification of the SIRT1 Activator SRT2104 as a Clinical Candidate
Volume: 10 Issue: 9
Author(s): Meghan Duncan, Robert B. Perni, James L. Ellis, George P. Vlasuk, Michael R. Jirousek, Joseph J. Nunes, Jill C. Milne, Peter J. Elliot, Vipin Suri, Akanksha Gupta, Kristina Kriksciukaite, Marie Yeager, Pui Yee Ng, Angela Tornblom, Siva Lavu, Jesse J. Smith, Jeffrey Song, Thomas V. Riera, David P. Carney, Amy V. Lynch, Christopher J. Oalmann, Chi B. Vu, Jeremy S. Disch and Jean E. Bemis
Affiliation:
Keywords: Activator, Imidazothiazole, SIRT1, Sirtuin, SRT1720, SRT2104.
Abstract: We have identified SRT2104 (4) as the first direct synthetic SIRT1 activator clinical candidate. The compound was derived from the optimization of a previously described imidazo[1,2-b]thiazole scaffold. SRT2104 was selected as a development candidate based on a combination of biochemical activity and pharmacokinetic profile. The in vivo characteristics of SRT2104 were superior to those of analogues with similar activation profiles. The overall preclinical profile suggests that the compound has potential to provide therapeutic benefit in a clinical setting.
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Duncan Meghan, Perni B. Robert, Ellis L. James, Vlasuk P. George, Jirousek R. Michael, Nunes J. Joseph, Milne C. Jill, Elliot J. Peter, Suri Vipin, Gupta Akanksha, Kriksciukaite Kristina, Yeager Marie, Ng Yee Pui, Tornblom Angela, Lavu Siva, Smith J. Jesse, Song Jeffrey, Riera V. Thomas, Carney P. David, Lynch V. Amy, Oalmann J. Christopher, Vu B. Chi, Disch S. Jeremy and Bemis E. Jean, The Identification of the SIRT1 Activator SRT2104 as a Clinical Candidate, Letters in Drug Design & Discovery 2013; 10 (9) . https://dx.doi.org/10.2174/15701808113100990021
DOI https://dx.doi.org/10.2174/15701808113100990021 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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