TTD Target ID: TTDR00296

Target Information
Name	Cell division protein kinase 5
Type of target	Research target
Synonyms	Cyclin-dependent kinase 5
	Cyclin-dependent kinase 5 (CDK5)
	PDPK
	Proline-directed protein kinase 33 kDa subunit
	Proline-directed protein kinase F(A) (PDPK F(A))
	Serine/threonine protein kinase PSSALRE
	Serine/threonine-protein kinase PSSALRE
	TPKII catalytic subunit
	Tau protein kinase II catalytic subunit
Disease	Alzheimer's disease    [1][2]
	Bladder cancer    [3]
BioChemical Class	Transferases transferring phosphorus-containing groups
EC Number	EC 2.7.1.-
	EC 2.7.1.37
Pathway	Alzheimer's disease
	Axon guidance
UniProt ID	Q00535
PDB Structure	1H4L; 1LFR; 1UNG; 1UNH; 1UNL.
Function	Probably involved in the control of the cell cycle. Interacts with d1 and d3-type g1 cyclins. Can phosphorylate histone h1, tau, map2 and nf-h and nf-m. Also interacts with p35 which activates the kinase.
Sequence	MQKYEKLEKIGEGTYGTVFKAKNRETHEIVALKRVRLDDDDEGVPSSALREICLLKELKH KNIVRLHDVLHSDKKLTLVFEFCDQDLKKYFDSCNGDLDPEIVKSFLFQLLKGLGFCHSR NVLHRDLKPQNLLINRNGELKLADFGLARAFGIPVRCYSAEVVTLWYRPPDVLFGAKLYS TSIDMWSAGCIFAELANAGRPLFPGNDVDDQLKRIFRLLGTPTEEQWPSMTKLPDYKPYP MYPATTSLVNVVPKLNATGRDLLQNLLKCNPVQRISAEEALQHPYFSDFCPP
Target Validation	Click to Find Target Validation Information.
Inhibitor	(R)-roscovitine		[2]
	1-phenyl-3- (2-		[4]
	3- (2-phenylthiazol-4-yl)quinolin-2		[5]
	6-PHENYL[5H]PYRROLO[2,3-B]PYRAZINE		[6]
	9-Nitropaullone		[2]
	AZAKENPAULLONE		[7]
	Alsterpaullone		[8]
	Aminopurvalanol (NG97)		[2]
	Flavopiridol		[9]
	Hymenialdisine		[8]
	Hymenialdisine		[2]
	Indirubin-3'-Monoxime		[8]
	Indirubin-3'-monoxime		[2]
	Indirubin-5-sulfonate		[2]
	KENPAULLONE		[7]
	MANZAMINE A		[10]
	Olomoucine		[11]
	Olomoucine		[2]
	Oxindole 16 (compound 3)		[2]
	Oxindole 95		[2]
	Purvalanol B		[2]
	SU9516		[2]
	SU9516		[8]
	Thieno analogue of kenpaullone		[7]
Cross References	3D Structure Related Literature On-Line Medical Dictionary
Ref 1	Cdk5, a therapeutic target for Alzheimer's disease? Biochim Biophys Acta. 2004 Mar 11;1697(1-2):137-42. To Reference
Ref 2	Pharmacological inhibitors of cyclin-dependent kinases. Trends Pharmacol Sci. 2002 Sep;23(9):417-25. To Reference
Ref 3	Association of overexpressed proline-directed protein kinase F(A) with chemoresistance, invasion, and recurrence in patients with bladder carcinoma. Cancer. 2002 Aug 15;95(4):775-83. To Reference
Ref 4	Bioorg Med Chem. 2007 Oct 15;15(20):6574-95. Epub 2007 Jul 25.Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors. To Reference
Ref 5	Bioorg Med Chem Lett. 2007 Oct 1;17(19):5384-9. Epub 2007 Aug 6.Design and synthesis of quinolin-2(1H)-one derivatives as potent CDK5 inhibitors. To Reference
Ref 6	Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 7	Bioorg Med Chem Lett. 2004 Jan 19;14(2):413-6.1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3 beta. To Reference
Ref 8	Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. To Reference
Ref 9	Zvelebil MJ: Flavopiridol (Hoechst AG). IDrugs. 1998 Jun;1(2):241-6. To Reference
Ref 10	J Nat Prod. 2007 Sep;70(9):1397-405. Epub 2007 Aug 21.Glycogen synthase kinase-3 (GSK-3) inhibitory activity and structure-activity relationship (SAR) studies of the manzamine alkaloids. Potential for Alzheimer's disease. To Reference
Ref 11	Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference

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