Target Validation Information
TTD ID	T81892
Target Name	XIAP messenger RNA (XIAP mRNA)
Type of Target	Clinical trial
Drug Potency against Target	ARPFAQK-FAM	Drug Info	IC50 = 570 nM	[1]
	AVPIAQKSEK-FAM	Drug Info	IC50 = 2800 nM	[1]
	EMBELIN	Drug Info	IC50 = 4100 nM	[1]
	SM-122	Drug Info	IC50 = 635.7 nM	[3]
	SM-131	Drug Info	Ki = 61 nM	[2]
	SM-337	Drug Info	Ki = 110.9 nM	[3]
Action against Disease Model	AEG35156	Drug Info	AEG35156 (a second-generation antisense oligonucleotide targeting X-linked inhibitor of apoptosis) reduced XIAP mRNA levels with an EC50 of 8 to 32 nmol/L and decreased XIAP protein levels by >80%. Loss of XIAP protein correlated with increased sensitization to t uMor necrosis factor-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis in Panc-1 pancreatic carcinoma cells. AEG35156 exhibited potent antit uMor activity relative to control oligonucleotides in three h uMan cancer xenograft models (prostate, colon, and lung) and was capable of inducing complete t uMor regression when combined with taxanes. Antit uMor effects of AEG35156 correlated with suppression of t uMor XIAP levels.	[4]
References
REF 1	Discovery of embelin as a cell-permeable, small-molecular weight inhibitor of XIAP through structure-based computational screening of a traditional... J Med Chem. 2004 May 6;47(10):2430-40.
REF 2	Design, synthesis, and evaluation of tricyclic, conformationally constrained small-molecule mimetics of second mitochondria-derived activator of ca... J Med Chem. 2008 Dec 11;51(23):7352-5.
REF 3	Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins. J Med Chem. 2010 Sep 9;53(17):6361-7.
REF 4	Preclinical characterization of AEG35156/GEM 640, a second-generation antisense oligonucleotide targeting X-linked inhibitor of apoptosis. Clin Cancer Res. 2006 Sep 1;12(17):5231-41.

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