Characterization of dequalinium as a XIAP antagonist that targets the BIR2 domain
Por:
M. ORZAEZ, A. GORTAT, M. SANCHO, R. CARBAJO, A. PINEDA-LUCENA, Y. PALACIOS-RODRIGUEZ and E. PEREZ-PAYA
Publicada:
1 may 2011
Resumen:
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.
Filiaciones:
:
Ctr Invest Principe Felipe, Lab Peptide & Prot Chem, Valencia 46012, Spain
A. GORTAT:
Ctr Invest Principe Felipe, Lab Peptide & Prot Chem, Valencia 46012, Spain
:
Ctr Invest Principe Felipe, Lab Peptide & Prot Chem, Valencia 46012, Spain
:
Ctr Invest Principe Felipe, Lab Struct Biochem, Valencia 46012, Spain
:
Ctr Invest Principe Felipe, Lab Struct Biochem, Valencia 46012, Spain
Y. PALACIOS-RODRIGUEZ:
Ctr Invest Principe Felipe, Lab Peptide & Prot Chem, Valencia 46012, Spain
IBV CSIC, Inst Biomed Valencia, Valencia 46010, Spain
:
Ctr Invest Principe Felipe, Lab Peptide & Prot Chem, Valencia 46012, Spain
IBV CSIC, Inst Biomed Valencia, Valencia 46010, Spain
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