.University of Milano  Department of Biomolecular Sciences and Biotechnology  
 
 
 

head of the group: Prof. Martino Bolognesi

 

 

 

 


 


DESIGNING PRO-APOPTOTIC smac-MIMETICS (DSM)

REFERENCES:

 
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Cossu F, Mastrangelo E, Milani M, et al. Designing smac-mimetics as antagonists of XIAP, cIAP1, and cIAP2. Biochemical and Biophysical Research Communications 2009;378(2):162-7.

Cossu F, Milani M, Mastrangelo E, et al. Structural basis for bivalent smac-mimetics recognition in the IAP protein family. J Mol Biol 2009; in press.

Daniotti M, Oggionni M, Ranzani T, et al. BRAF alterations are associated with complex mutational profiles in malignant melanoma. Oncogene 2004;23(35):5968-77. 
 
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Galbán S, Hwang C, Rumble JM, Oetjen KA, Wright CW, Boudreault A, Durkin J, Gillard JW, Jaquith JB, Morris SJ, Duckett CS. Cytoprotective effects of IAPs revealed by a small molecule antagonist. Biochem J. 2009; 417(3):765-71.
 
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Li L, Thomas RM, Suzuki H, De Brabander JK, Wang X, Harran PG. A small molecule smac mimic potentiates TRAIL- and TNF{alpha}-mediated cell death. Science 2004;305(5689):1471-4.  
 
Lu J, Bai L, Sun H, et al. SM-164: A novel, bivalent smac mimetic that induces apoptosis and tumor regression by concurrent removal of the blockade of cIAP-1/2 and XIAP. Cancer Res 2008;68(22):9384-93.
 
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Mastrangelo E, Cossu F, Milani M, et al. Targeting the X-linked inhibitor of apoptosis protein through 4-substituted azabicyclo[5.3.0]alkane smac mimetics. structure, activity, and recognition principles. Journal of Molecular Biology 2008;384(3):673-89.
 
Nikolovska-Coleska Z, Wang R, Fang X, et al. Development and optimization of a binding assay for the XIAP BIR3 domain using fluorescence polarization. Analytical Biochemistry 2004;332(2):261-73.
 
Nikolovska-Coleska Z, Meagher JL, Jiang S, et al. Design and characterization of bivalent smac-based peptides as antagonists of XIAP and development and validation of a fluorescence polarization assay for XIAP containing both BIR2 and BIR3 domains. Analytical Biochemistry 2008;374(1):87-98.
 
Petersen SL, Wang L, Yalcin-Chin A, et al. Autocrine TNFα signaling renders human cancer cells susceptible to smac-mimetic-induced apoptosis. Cancer Cell 2007;12(5):445-56.
 
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Sun H, Nikolovska-Coleska Z, Yang C, et al. Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the X-linked inhibitor of apoptosis Protein/Caspase-9 interaction site. J Med Chem 2004;47(17):4147-50.  
 
Sun H, Nikolovska-Coleska Z, Yang C, et al. Structure-based design of potent, conformationally constrained smac mimetics. J Am Chem Soc 2004;126(51):16686-7.  (b)
 
Sun H, Nikolovska-Coleska Z, Lu J, Qiu S, Yang C-Y, Gao W, Meagher J, Stuckey J, Wang S. Design, synthesis and evaluation of a potent, cell-permeable, conformationally constrained Second Mitochondria Derived Activator of Caspase (Smac) mimetic. J. Med. Chem. 2006;49(26):7916-20.
 
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Varfolomeev E, Blankenship JW, Wayson SM, et al. IAP antagonists induce autoubiquitination of c-IAPs, NF-κB activation, and TNFα-dependent apoptosis. Cell 2007;131(4):669-81.
 
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Vince JE, Wong WW, Khan N, et al. IAP antagonists target cIAP1 to induce TNFα-dependent apoptosis. Cell 2007;131(4):682-93.
 
Wang L, Du F, Wang X. TNF-α induces two distinct caspase-8 activation pathways. Cell 2008;133(4):693-703.
 
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