Literature DB >> 24155041

Carprofen analogues as sirtuin inhibitors: enzyme and cellular studies.

Paolo Mellini1, Vincenzo Carafa, Barbara Di Rienzo, Dante Rotili, Daniela De Vita, Roberto Cirilli, Bruno Gallinella, Donatella Paola Provvisiero, Salvatore Di Maro, Ettore Novellino, Lucia Altucci, Antonello Mai.   

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.
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

Entities:  

Keywords:  SIRT1/2; apoptosis; histone deacetylases; inhibitors; sirtuins

Mesh:

Substances:

Year:  2012        PMID: 24155041     DOI: 10.1002/cmdc.201200318

Source DB:  PubMed          Journal:  ChemMedChem        ISSN: 1860-7179            Impact factor:   3.466


  3 in total

1.  Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors.

Authors:  Mohammad A Khanfar; Luisa Quinti; Hua Wang; Soo Hyuk Choi; Aleksey G Kazantsev; Richard B Silverman
Journal:  Eur J Med Chem       Date:  2014-02-06       Impact factor: 6.514

2.  In Silico and Experimental Investigation of the Biological Potential of Some Recently Developed Carprofen Derivatives.

Authors:  Florea Dumitrascu; Ana-Maria Udrea; Mino R Caira; Diana Camelia Nuta; Carmen Limban; Mariana Carmen Chifiriuc; Marcela Popa; Coralia Bleotu; Anamaria Hanganu; Denisa Dumitrescu; Speranta Avram
Journal:  Molecules       Date:  2022-04-23       Impact factor: 4.927

3.  Biochemical mechanism and biological effects of the inhibition of silent information regulator 1 (SIRT1) by EX-527 (SEN0014196 or selisistat).

Authors:  Sylvain Broussy; Hanna Laaroussi; Michel Vidal
Journal:  J Enzyme Inhib Med Chem       Date:  2020-12       Impact factor: 5.051

  3 in total

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