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Title

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

AuthorsOrzáez, Mar; Gortat, Anna; Sancho, Mónica; Carbajo, Rodrigo J.; Pineda-Lucena, Antonio; Palacios-Rodríguez, Yadira; Pérez-Payá, Enrique
KeywordsAnti-tumour
apoptosis
dequalinium
IAP
inhibitor
screening
XIAP
Issue Date22-Feb-2011
PublisherSpringer
CitationApoptosis - Heidelberg 16(5): 460-7 (2011)
AbstractInhibitor 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
Description8 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
URIhttp://hdl.handle.net/10261/47022
DOI10.1007/s10495-011-0582-4
ISSN1360-8185
E-ISSN1573-675X
Appears in Collections:(IBV) Artículos
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