Therapeutic Targets Database
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TTD Target ID: TTDC00166

Target Information
NameCell division control protein 2 homolog    
Type of targetClinical trial target    
SynonymsCDK1    
Cyclin-dependent kinase 1    
P34 protein kinase    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1]
Malaria
[ICD9: 084   ICD10: B50-B54]
[2]
Drug(s)Ro 31-7453Phase IIOvarian Cancer; Endometrial Cancer[3]
SCH 727965Phase IIAdvanced breast cancer, NSCLC, acute leukaemia and lymphoma[4]
P276-00Phase I/IIMultiple myeloma, mantle cell lymphoma, head and neck cancers, and cyclin D1-positive melanoma[4]
R547Phase I completedNeoplasms, Advanced solid tumours[4]
SCH 727965Phase IAdvanced solid tumours, NHL, multiple myeloma and CLL[4]
TerameprocolPhase ILeukaemia, refractory solid tumours and lymphoma[4]
ZK 304709Phase IAdvanced solid tumours[4]
AG-024322Terminated in Phase IAdvanced cancer[4]
R-roscovitineTerminated in Phase IINon-Small Cell Lung Cancer (NSCLC)[4]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.-
EC 2.7.1.37
UniProt IDP06493
Q6LFL1
PDB Structure1LC9.    
FunctionPlays a key role in the control of the eukaryotic cell cycle. It is required in higher cells for entry into s-phase and mitosis. P34 is a component of the kinase complex that phosphorylates the repetitive carboxyl-terminus of rna polymerase ii.    
SequenceMESGVYFSLYEDFFKDAKIFLNTIESKNKILDVSNSSTTSSSISSDEVDDISSNNDTEKY DDNYNSTGRYLDYYLNMENNKAICYNNIEESNTISHNNNNHNNHFSNILYNGSSKILLCY KNNYNICFSYKPYNENIYHDVPNINYSLSIFRKKGSLNTTSHIKGKRQIEPNWTKQQIRE ALDLEKGIKRRTRSREIYDNNYNDDNNYSDDNNYNDDNNYSDDNYYNDDNYYNEDNYYND NKSVGGGIVKYLNIFSKLPFFYLFYPSSYKKKKRKKKFYHNQVRNDLNSSIFYSKHFKNE IKKKSDNSDFKKSAQKKNKKNEENILYNDKKDNIHINENNIYKNMKKQNHMLTKKEMYKS TSVNNLDIDTKKTEEDYFLKKKRKKENNKKGISYEYLLKPSKHDYDAFCLFNPRFKQGKH HTVMYLQSYNVSIIPFVKAKKLKERVNQLFSEINPWIHKSLTLSKLRNLKIDLFNLINNI PEIDISTISCAWVFFERLVMKGYVHKYNRKLYAATCLILSFKFYQHDDIQILEKLLIHIQ KLDKKENLTPSLIFSVEFLVYRLLEFSLQHTYENIRPHIHQYLESKELKFEDVYGTSEEI YLYSNKS
Target ValidationClick to Find Target Validation Information.    
Inhibitor (2,6-Diamino-pyridin-3-yl)-phenyl-methanone[5]
(R)-roscovitine[6]
2- (p-toluidino)-4-phenylpyrimidine-5-carbonitrile[7]
3,4-bis (indol-3-yl)maleimide derivative[8]
3,4-di- (4-methoxyphenyl)-1H-pyrrole-2,5-dione[9]
3,4-diphenyl-1H-pyrrole-2,5-dione[9]
3- (4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione[9]
3- (indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione[9]
4- (Quinolin-3-yl)-N-p-tolylpyrimidin-2-amine[10]
4- (Quinolin-4-yl)-N-p-tolylpyrimidin-2-amine[10]
4-phenyl-2- (phenylamino)pyrimidine-5-carbonitrile[7]
AG-024322[4]
AZAKENPAULLONE[11]
Alsterpaullone[12]
Alsterpaullone[13]
CGP-60474[14]
Flavopiridol[15]
GF-109203[8]
Hymenialdisine[13]
Indirubin-5-Sulphonate[16]
JNJ-7706621[17]
KENPAULLONE[18]
Microxine[19]
P276-00[4]
PF-228[20]
PHA-767491[21]
Purvalanol[16]
Purvalanol A[12]
R-roscovitine[4]
R547[4]
RO-316233[8]
Ro 31-7453[3]
SCH 727965[4]
Terameprocol[4]
Thieno analogue of kenpaullone[11]
ZK 304709[4]
Binder10Z-Hymenialdisine[22]
IN1535[23]
Indirubin-3'-Monoxime[13]
Indirubin-3'-monoxime[24]
Indirubin-5-sulfonate[25]
Olomoucine[26]
Olomoucine[16]
Purvalanol B[12]
SU9516[27]
SU9516[13]
MultitargetAG-024322[4]
P276-00[4]
R-roscovitine[4]
R547[4]
Ro 31-7453[3]
SCH 727965[4]
Terameprocol[4]
ZK 304709[4]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Pharmacological inhibitors of cyclin-dependent kinases. Trends Pharmacol Sci. 2002 Sep;23(9):417-25. To Reference
Ref 2Can mosquitoes be bitten? A new hope for anti-malarial drug design. Structure. 2003 Nov;11(11):1309-10. To Reference
Ref 3A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. To Reference
Ref 4Nat Rev Drug Discov. 2009 Jul;8(7):547-66.Cell cycle kinases as therapeutic targets for cancer. To Reference
Ref 5Bioorg Med Chem Lett. 2005 May 2;15(9):2221-4.3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation. To Reference
Ref 6Hormone-induced cortical maturation ensures the slow block to polyspermy and does not couple with meiotic maturation in starfish. Dev Biol. 2008 Jun 1;318(1):194-202. Epub 2008 Mar 28. To Reference
Ref 7Bioorg Med Chem Lett. 2007 Jun 15;17(12):3266-70. Epub 2007 Apr 10.4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation. To Reference
Ref 8Bioorg Med Chem Lett. 1998 May 5;8(9):1019-22.Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure. To Reference
Ref 9J Med Chem. 2006 Feb 23;49(4):1271-81.Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. To Reference
Ref 10Eur J Med Chem. 2010 Jan;45(1):379-86. Epub 2009 Oct 13.Synthesis and cytotoxic activity of 2-methylimidazo[1,2-a]pyridine- and quinoline-substituted 2-aminopyrimidine derivatives. To Reference
Ref 11Bioorg 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 12Down-regulation of survivin in nitric oxide-induced cell growth inhibition and apoptosis of the human lung carcinoma cells. J Biol Chem. 2004 May 7;279(19):20267-76. Epub 2004 Feb 26. To Reference
Ref 13Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. To Reference
Ref 14J Med Chem. 2005 Mar 24;48(6):1886-900.Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors. To Reference
Ref 15Zvelebil MJ: Flavopiridol (Hoechst AG). IDrugs. 1998 Jun;1(2):241-6. To Reference
Ref 16Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 17Bioorg Med Chem Lett. 2006 Jul 15;16(14):3639-41. Epub 2006 May 6.Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621. To Reference
Ref 18Eur J Med Chem. 2010 Sep;45(9):4316-30. Epub 2010 Jun 30.Discovery of novel CDK1 inhibitors by combining pharmacophore modeling, QSAR analysis and in silico screening followed by in vitro bioassay. To Reference
Ref 19Microxine, a new cdc2 kinase inhibitor from the Australian marine sponge Microxina species. J Nat Prod. 2001 Apr;64(4):525-6. To Reference
Ref 20J Biol Chem. 2007 May 18;282(20):14845-52. Epub 2007 Mar 28.Cellular characterization of a novel focal adhesion kinase inhibitor. To Reference
Ref 21J 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 22DrugBank: a knowledgebase for drugs, drug actions and drug targets. Nucleic Acids Res. 2008 Jan;36(Database issue):D901-6. Epub 2007 Nov 29. To Reference
Ref 23M-phase regulation of the recruitment of mRNAs onto polysomes using the CDK1/cyclin B inhibitor aminopurvalanol. Biochem Biophys Res Commun. 2003 Jul 11;306(4):880-6. To Reference
Ref 24The kinase inhibitor indirubin-3'-oxime prevents germinal vesicle breakdown and reduces parthenogenetic development of pig oocytes. Theriogenology. 2006 Mar 1;65(4):744-56. Epub 2005 Aug 18. To Reference
Ref 25Binding of the potential antitumour agent indirubin-5-sulphonate at the inhibitor site of rabbit muscle glycogen phosphorylase b. Comparison with ligand binding to pCDK2-cyclin A complex. Eur J Biochem. 2004 Jun;271(11):2280-90. To Reference
Ref 26Antiproliferative activity of olomoucine II, a novel 2,6,9-trisubstituted purine cyclin-dependent kinase inhibitor. Cell Mol Life Sci. 2005 Aug;62(15):1763-71. To Reference
Ref 27SU9516: biochemical analysis of cdk inhibition and crystal structure in complex with cdk2. Biochem Biophys Res Commun. 2003 Oct 24;310(3):1026-31. To Reference



 

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