Apoptosis 2011-05-01

Characterization of dequalinium as a XIAP antagonist that targets the BIR2 domain.

Mar Orzáez, Anna Gortat, Mónica Sancho, Rodrigo J Carbajo, Antonio Pineda-Lucena, Yadira Palacios-Rodríguez, Enrique Pérez-Payá

Index: Apoptosis 16(5) , 460-7, (2011)

Full Text: HTML

Abstract

Inhibitor of apoptosis proteins (IAPs) regulate the activity of caspases in apoptosis. The human X chromosome-encoded IAP (XIAP) is one of the more potent members of the IAP family and it has been described as a central regulator of apoptosis. Thus, molecules that inhibit XIAP could offer therapeutic opportunities to treat unwanted apoptosis inhibition. In the present study we have applied the selective optimization of side activities (SOSA) approach to the discovery of XIAP inhibitors. In this sense, we have identified dequalinium hydrochloride (Dq) as an inhibitor of the XIAP/caspase-3 interaction both in vitro and in cellular assays.

Related Compounds

  • DEQUALINIUM...
  • Dequalinium chlori...
  • Dequalinium Chlor...

Related Articles:

Antimicrobial topical agents used in the vagina.

2011-01-01

[Curr. Probl. Dermatol. 40 , 36-47, (2011)]

Dequalinium induces cytotoxicity in human leukemia NB4 cells by downregulation of Raf/MEK/ERK and PI3K/Akt signaling pathways and potentiation of specific inhibitors of these pathways.

2014-07-01

[Leuk. Res. 38(7) , 795-803, (2014)]

N-palmitoyl-ethanolamine (PEA) induces peripheral antinociceptive effect by ATP-sensitive K+-channel activation.

2012-01-01

[J. Pharmacol. Sci. 118(2) , 156-60, (2012)]

New method for the quantification of dequalinium cations in pharmaceutical samples by absorption and fluorescence diode array thin-layer chromatography.

2009-06-19

[J. Chromatogr. A. 1216(25) , 5052-6, (2009)]

Exercise-induced cardioprotection is impaired by anabolic steroid treatment through a redox-dependent mechanism

2013-11-01

[J. Steroid Biochem. Mol. Biol. 138 , 267-72, (2013)]

More Articles...