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Discovering inhibitors of human sirtuin type 2: novel structural scaffolds.
J Med Chem. 2006 Nov 30; 49(24):7239-41.JM

Abstract

A successful virtual screening experiment of novel SIRT2 inhibitors is described. Four out of 11 experimentally tested compounds showed in vitro inhibitory activity toward SIRT2 in a micromolar level, resulting in an experimental hit ratio of 36%. Two of these compounds inhibited SIRT2 with IC50 (microM) values of 51 and 91; moreover, one of the new inhibitors was comprised of an entirely new SIRT2-inhibiting structural scaffold.

Authors+Show Affiliations

Tervo AJ
Department of Pharmaceutical Chemistry, University of Kuopio, and Department of Neurology, Kuopio University Hospital, Post Office Box 1777, 70211 Kuopio, Finland.
Suuronen T
No affiliation info available
Kyrylenko S
No affiliation info available
Kuusisto E
No affiliation info available
Kiviranta PH
No affiliation info available
Salminen A
No affiliation info available
Leppänen J
No affiliation info available
Poso A
No affiliation info available

MeSH

Benzhydryl CompoundsBenzimidazolesBinding SitesEnzyme InhibitorsHumansModels, MolecularPyridinesRecombinant ProteinsSirtuin 2SirtuinsStructure-Activity RelationshipThiazoles

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

17125277

Citation

Tervo, Anu J., et al. "Discovering Inhibitors of Human Sirtuin Type 2: Novel Structural Scaffolds." Journal of Medicinal Chemistry, vol. 49, no. 24, 2006, pp. 7239-41.
Tervo AJ, Suuronen T, Kyrylenko S, et al. Discovering inhibitors of human sirtuin type 2: novel structural scaffolds. J Med Chem. 2006;49(24):7239-41.
Tervo, A. J., Suuronen, T., Kyrylenko, S., Kuusisto, E., Kiviranta, P. H., Salminen, A., Leppänen, J., & Poso, A. (2006). Discovering inhibitors of human sirtuin type 2: novel structural scaffolds. Journal of Medicinal Chemistry, 49(24), 7239-41.
Tervo AJ, et al. Discovering Inhibitors of Human Sirtuin Type 2: Novel Structural Scaffolds. J Med Chem. 2006 Nov 30;49(24):7239-41. PubMed PMID: 17125277.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Discovering inhibitors of human sirtuin type 2: novel structural scaffolds. AU - Tervo,Anu J, AU - Suuronen,Tiina, AU - Kyrylenko,Sergiy, AU - Kuusisto,Erkki, AU - Kiviranta,Päivi H, AU - Salminen,Antero, AU - Leppänen,Jukka, AU - Poso,Antti, PY - 2006/11/28/pubmed PY - 2007/2/16/medline PY - 2006/11/28/entrez SP - 7239 EP - 41 JF - Journal of medicinal chemistry JO - J Med Chem VL - 49 IS - 24 N2 - A successful virtual screening experiment of novel SIRT2 inhibitors is described. Four out of 11 experimentally tested compounds showed in vitro inhibitory activity toward SIRT2 in a micromolar level, resulting in an experimental hit ratio of 36%. Two of these compounds inhibited SIRT2 with IC50 (microM) values of 51 and 91; moreover, one of the new inhibitors was comprised of an entirely new SIRT2-inhibiting structural scaffold. SN - 0022-2623 UR - https://www.unboundmedicine.com/medline/citation/17125277/Discovering_inhibitors_of_human_sirtuin_type_2:_novel_structural_scaffolds_ L2 - https://doi.org/10.1021/jm060686r DB - PRIME DP - Unbound Medicine ER -