Carprofen Analogues As Sirtuin Inhibitors: Enzyme and Cellular Studies

Overview

Journal ChemMedChem

Specialties Chemistry
Pharmacology

Date 2013 Oct 25

PMID 24155041

Citations 6

Authors

Paolo Mellini

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

Affiliations

Soon will be listed here.

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.

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

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