Data di Pubblicazione:
2008
Citazione:
A NMR STUDY OF SMAC MIMICS TARGETING BOTH THE
BIR2 AND BIR3 DOMAINS IN XIAP PROTEIN / D. Potenza, F. Vasile, L. Belvisi, C. Drago, P. Seneci. ((Intervento presentato al convegno MAGNETIC RESONANCE IN THE
LIFE SCIENCES : WHAT’S NEW tenutosi a Montecatini , Lucca nel 2008.
Abstract:
XIAP is a central apoptosis regulator that inhibits apoptosis by binding to and inhibiting the effectors
caspase-3/-7 and an initiator caspase-9 through its BIR2 and BIR3 domains, respectively. Smac protein in
its dimeric form effectively antagonizes XIAP by concurrently targeting both its BIR2 and BIR3
domains1.
Novel proapoptotic Smac mimics/XIAP inhibitors have been designed, synthesized and characterized in
our group. These pseudopeptides, containing the 1-aza-2-oxobicyclo[4.3.0]nonane scaffold, were tested
by tr-NOE and STD-NMR experiments2.
Here, we show the binding evidence and the epitope mapping for a series of new compounds respect to
different fragments of XIAP protein: the STD spectra of selected Smac- mimics suggest different binding
interactions with BIR2 and BIR3 domains. So, we are able to design new higher affinity compounds.
Tipologia IRIS:
14 - Intervento a convegno non pubblicato
Keywords:
NMR ; SMAC ; Ligang-protein interaction
Elenco autori:
D. Potenza, F. Vasile, L. Belvisi, C. Drago, P. Seneci
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