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

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Orzaez M, Gortat A, Sancho M, Carbajo RJ, Pineda-Lucena A, Palacios-Rodriguez Y, Perez-Paya E

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

Apoptosis. 2011 May;16(5):460-7. doi: 10.1007/s10495-011-0582-4.

PubMed ID

21340509 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Dequalinium	E3 ubiquitin-protein ligase XIAP	Protein	Humans	Yes	Antagonist Inhibitor	Details