TTD Target ID: TTDC00145

Target Information
Name	Ribosomal protein S6 kinase
Type of target	Discontinued target
Synonyms	P70-S6K
	S6K
Disease	Cancer, unspecific    [1]
	Solid tumors    [2]
Drug(s)	XL418		Suspended in Phase I	Solid Tumors	[3]
BioChemical Class	Transferases transferring phosphorus-containing groups
EC Number	EC 2.7.1.-
	EC 2.7.1.37
Pathway	Acute myeloid leukemia
	ErbB signaling pathway
	Insulin signaling pathway
	TGF-beta signaling pathway
	mTOR signaling pathway
UniProt ID	P23443
Function	Phosphorylates specifically ribosomal protein s6.
Sequence	MRRRRRRDGFYPAPDFRDREAEDMAGVFDIDLDQPEDAGSEDELEEGGQLNESMDHGGVG PYELGMEHCEKFEISETSVNRGPEKIRPECFELLRVLGKGGYGKVFQVRKVTGANTGKIF AMKVLKKAMIVRNAKDTAHTKAERNILEEVKHPFIVDLIYAFQTGGKLYLILEYLSGGEL FMQLEREGIFMEDTACFYLAEISMALGHLHQKGIIYRDLKPENIMLNHQGHVKLTDFGLC KESIHDGTVTHTFCGTIEYMAPEILMRSGHNRAVDWWSLGALMYDMLTGAPPFTGENRKK TIDKILKCKLNLPPYLTQEARDLLKKLLKRNAASRLGAGPGDAGEVQAHPFFRHINWEEL LARKVEPPFKPLLQSEEDVSQFDSKFTRQTPVDSPDDSTLSESANQVFLGFTYVAPSVLE SVKEKFSFEPKIRSPRRFIGSPRTPVSPVKFSPGDFWGRGASASTANPQTPVEYPMETSG IEQMDVTMSGEASAPLPIRQPNSGPYKKQAFPMISKRPEHLRMNL
Target Validation	Click to Find Target Validation Information.
Inhibitor	4,5,6,7-tetrabromobenzotriazole		[4]
	4-[ (3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol		[5]
	BISINDOLYLMALEIMIDE IX		[6]
	CI-1040,   PD-18435,   PD-184352		[6]
	KN-62		[6]
	KT-5720		[6]
	LY-294002		[6]
	PD-98059		[6]
	PHA-767491		[7]
	RO-316233		[6]
	SB-202190		[6]
	SB-203580		[6]
	SB-415286		[8]
	SB-747651A		[9]
	STAUROSPORINONE		[6]
	U-0126		[6]
	XL418		[3]
Multitarget	XL418		[3]
Cross References	3D Structure Related Literature On-Line Medical Dictionary
Ref 1	Identification of novel cellular targets in biliary tract cancers using global gene expression technology. Am J Pathol. 2003 Jul;163(1):217-29. To Reference
Ref 2	CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference
Ref 3	Drug information of XL418. National Cancer Institute. 2009 To Reference
Ref 4	J Med Chem. 2004 Dec 2;47(25):6239-47.Optimization of protein kinase CK2 inhibitors derived from 4,5,6,7-tetrabromobenzimidazole. To Reference
Ref 5	J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. To Reference
Ref 6	Biochem J. 2000 Oct 1;351(Pt 1):95-105.Specificity and mechanism of action of some commonly used protein kinase inhibitors. To Reference
Ref 7	J Med Chem. 2007 May 31;50(11):2647-54. Epub 2007 May 5.Pyrrolopyridine inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2). To Reference
Ref 8	Bioorg Med Chem Lett. 2001 Mar 12;11(5):635-9.3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3). To Reference
Ref 9	Bioorg Med Chem Lett. 2005 Jul 15;15(14):3407-11.(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: further optimisation as highly potent and selective MSK-1-inhibitors. To Reference

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Professor in Department of Pharmacy
National University of Singapore, Singapore

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