Target Validation Information
TTD ID	T23995
Target Name	Protein kinase C theta (PRKCQ)
Type of Target	Clinical trial
Drug Potency against Target	Sotrastaurin acetate	Drug Info	Ki = 0.22 nM	[6]
		Drug Info	IC50 = 3 nM	[2]
	LY-317644	Drug Info	IC50 = 6400 nM
	LY-326449	Drug Info	IC50 = 630 nM	[5]
	RO-316233	Drug Info	IC50 = 550 nM	[4]
	Ro-32-0557	Drug Info	IC50 = 6.8 nM
	RO-320432	Drug Info	IC50 = 21 nM
	[2,2':5',2'']Terthiophen-4-yl-methanol	Drug Info	IC50 = 3000 nM	[1]
	[2,2':5',2'']Terthiophene-4,5''-dicarbaldehyde	Drug Info	IC50 = 700 nM	[1]
	[2,2':5',2'']Terthiophene-4-carbaldehyde	Drug Info	IC50 = 5000 nM	[1]
Action against Disease Model	Sotrastaurin acetate	Drug Info	A significant fraction of ABC DLBCL cell lines exhibited strong sensitivity to sotrastaurin (STN), and we found that the molecular nature of NF-|?B pathway lesions predicted responsiveness. CD79A/B mutations correlated with STN sensitivity, whereas CARD11 mutations rendered ABC DLBCL cell lines insensitive. Growth inhibitory effects of PKC inhibition correlated with NF-|?B pathway inhibition and were mediated by induction of G?-phase cell-cycle arrest and/or cell death. We found that STN produced significant antit uMor effects in a mouse xenograft model of CD79A/B-mutated DLBCL.	[3]
References
REF 1	Novel protein kinase C inhibitors: synthesis and PKC inhibition of beta-substituted polythiophene derivatives. Bioorg Med Chem Lett. 1999 Aug 2;9(15):2279-82.
REF 2	Mixed lineage kinase activity of indolocarbazole analogues. Bioorg Med Chem Lett. 2002 Jan 21;12(2):147-50.
REF 3	Advanced c-myc antisense (AVI-4126)-eluting phosphorylcholine-coated stent implantation is associated with complete vascular healing and reduced ne... Catheter Cardiovasc Interv. 2004 Apr;61(4):518-27.
REF 4	Inhibitors of protein kinase C. 1. 2,3-Bisarylmaleimides. J Med Chem. 1992 Jan;35(1):177-84.
REF 5	(S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H... J Med Chem. 1996 Jul 5;39(14):2664-71.
REF 6	The PKC inhibitor AEB071 may be a therapeutic option for psoriasis. J Clin Invest. 2008 Sep;118(9):3151-9.

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