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Cover Picture: 2‐Anilinobenzamides as SIRT Inhibitors (ChemMedChem 10/2006)
Author(s) -
Suzuki Takayoshi,
Imai Keiko,
Nakagawa Hidehiko,
Miyata Naoki
Publication year - 2006
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200690035
Subject(s) - benzamide , acetylation , nicotinamide , resveratrol , histone , lysine , chemistry , substrate (aquarium) , cancer research , biochemistry , combinatorial chemistry , stereochemistry , enzyme , biology , dna , amino acid , ecology , gene
The cover picture shows the model of a SIRT inhibitor, 2‐anilinobenzamide, bound to the catalytic core of a SIRT homologue. SIRTs catalyze the deacetylation of several proteins such as histones, p53, and γ‐tubulin, and are involved in certain disease states including cancer. SIRT inhibitors can be considered as potential therapeutic agents. This simple compound, which was discovered from a nicotinamide‐ and benzamide‐focused chemical library, shows potent SIRT1 inhibition competitive with the acetylated lysine substrate and causes p53 acetylation in human colon cancer HCT116 cells. For more details, see the Communication by T. Suzuki, N. Miyata et al. on p. 1059 ff.