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Open Access item Characterization of dequalinium as a XIAP antagonist that targets the BIR2 domain

Authors:Orzáez, Mar
Gortat, Anna
Sancho, Mónica
Carbajo, Rodrigo J.
Pineda-Lucena, Antonio
Palacios-Rodríguez, Yadira
Pérez-Payá, Enrique
Keywords:Anti-tumour, apoptosis, dequalinium, IAP, inhibitor, screening, XIAP
Issue Date:22-Feb-2011
Publisher:Springer
Citation:Apoptosis - Heidelberg 16(5): 460-7 (2011)
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
Description:8 páginas, 5 figuras, 1 tabla. PMID:21340509[PubMed]
Publisher version (URL):The original publication is available at www.springerlink.com; http://dx.doi.org/10.1007/s10495-011-0582-4
URI:http://hdl.handle.net/10261/47022
ISSN:1360-8185
E-ISSNmetadata.dc.identifier.doi = DOI:1573-675X
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Appears in Collections:(IBV) Artículos

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