The Identification of the SIRT1 Activator SRT2104 as a Clinical Candidate
Pui Yee Ng,
Jean E. Bemis,
Jeremy S. Disch,
Chi B. Vu,
Christopher J. Oalmann,
Amy V. Lynch,
David P. Carney,
Thomas V. Riera,
Jesse J. Smith,
Peter J. Elliot,
Jill C. Milne,
Joseph J. Nunes,
Michael R. Jirousek,
George P. Vlasuk,
James L. Ellis,
Robert B. Perni.
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.
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