1. Carprofen analogues as sirtuin inhibitors: enzyme and cellular studies
- Author
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Barbara Di Rienzo, Salvatore Di Maro, Paolo Mellini, Roberto Cirilli, Vincenzo Carafa, Lucia Altucci, Daniela De Vita, Ettore Novellino, Antonello Mai, Donatella Paola Provvisiero, Bruno Gallinella, Dante Rotili, Mellini, P, Carafa, V, Di Rienzo, B, Rotili, D, De Vita, D, Cirilli, R, Gallinella, B, Provvisiero, Dp, DI MARO, Salvatore, Novellino, E, Altucci, Lucia, Mai, A., P., Mellini, V., Carafa, B., Di Rienzo, D., Rotili, D., De Vita, R., Cirilli, B., Gallinella, D. P., Provvisiero, S., Di Maro, Novellino, Ettore, L., Altucci, and A., Mai
- Subjects
Drug ,Inhibitor ,media_common.quotation_subject ,Carbazoles ,Antineoplastic Agents ,Apoptosis ,Biochemistry ,03 medical and health sciences ,0302 clinical medicine ,Sirtuin 2 ,Sirtuin 1 ,Tubulin ,Cell Line, Tumor ,Neoplasms ,Drug Discovery ,medicine ,Sirtuin ,Humans ,Carprofen ,Histone deacetylase ,General Pharmacology, Toxicology and Pharmaceutics ,030304 developmental biology ,media_common ,Pharmacology ,chemistry.chemical_classification ,SIRT1/2 ,0303 health sciences ,U937 cell ,biology ,Selisistat ,Organic Chemistry ,Anti-Inflammatory Agents, Non-Steroidal ,Apoptosi ,Acetylation ,3. Good health ,Histone Deacetylase Inhibitors ,Enzyme ,chemistry ,030220 oncology & carcinogenesis ,biology.protein ,Molecular Medicine ,Tumor Suppressor Protein p53 ,medicine.drug - Abstract
The best of both: SIRT1/2 inhibitors were developed by combining chemical features of selisistat (SIRT1-selective inhibitor; blue) and carprofen (anti-inflammatory drug; red). The most potent compound (shown) increased acetyl-p53 and acetyl-α-tubulin levels, and induced slight apoptosis at 50 μM in U937 cells, differently from selisistat and carprofen.
- Published
- 2012