Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00165

Target Information
NameCell division protein kinase 4    
Type of targetClinical trial target    
SynonymsCDK4    
Cyclin-dependent kinase 4    
PSK-J3    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1]
Insulin-dependent diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[2]
Squamous cell carcinoma
[ICD9: 199   ICD10: C44]
[2]
Drug(s)LY2835219Phase IICancer
PD-332991Phase IIVarious cancers[3]
Ro 31-7453Phase IIOvarian Cancer; Endometrial Cancer[3]
P276-00Phase I/IIMultiple myeloma, mantle cell lymphoma, head and neck cancers, and cyclin D1-positive melanoma[4]
PD-0332991Phase I/IIBreast Cancer[4]
R547Phase I completedNeoplasms, Advanced solid tumours[4]
LEE011Phase ILymphoma
LEE011Phase ISolid Tumors
P1446A-05Phase IAdvanced refractory malignancies including solid and haematological tumours[4]
PD-0332991Phase ILymphoma, Mantle-Cell[4]
ZK 304709Phase IAdvanced solid tumours[4]
AG-024322Terminated in Phase IAdvanced cancer[4]
Capridine-betaPreclinicalAdvanced Solid Tumors[5]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.37
PathwayBladder cancer
Cell cycle
Chronic myeloid leukemia
Glioma
Melanoma
Non-small cell lung cancer
Pancreatic cancer
Pathways in cancer
Small cell lung cancer
T cell receptor signaling pathway
Tight junction
p53 signaling pathway
UniProt IDP11802
PDB Structure1LD2; 2W96; 2W99; 2W9F; 2W9Z; 3G33.    
FunctionProbably involved in the control of the cell cycle.    
SequenceMATSRYEPVAEIGVGAYGTVYKARDPHSGHFVALKSVRVPNGGGGGGGLPISTVREVALL RRLEAFEHPNVVRLMDVCATSRTDREIKVTLVFEHVDQDLRTYLDKAPPPGLPAETIKDL MRQFLRGLDFLHANCIVHRDLKPENILVTSGGTVKLADFGLARIYSYQMALTPVVVTLWY RAPEVLLQSTYATPVDMWSVGCIFAEMFRRKPLFCGNSEADQLGKIFDLIGLPPEDDWPR DVSLPRGAFPPRGPRPVQSVVPEMEESGAQLLLEMLTFNPHKRISAFRALQHSYLHKDEG NPE
Related US Patent6,630,464
Target ValidationClick to Find Target Validation Information.    
Inhibitor1- (1H-Indazol-6-yl)-3-pyridin-2-yl-urea[6]
1- (7-Hydroxy-naphthalen-1-yl)-3-pyridin-2-yl-urea[6]
1- (9-Oxo-9H-fluoren-4-yl)-3-pyridin-2-yl-urea[6]
1-Pyridin-2-yl-3-quinolin-5-yl-urea[6]
10-hydroxy-18-methoxybetaenone[7]
3,4-di- (4-methoxyphenyl)-1H-pyrrole-2,5-dione[8]
3,4-diphenyl-1H-pyrrole-2,5-dione[8]
3- (4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione[8]
3- (indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione[8]
4-[ (3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol[9]
AG-024322[4]
Capridine-beta[5]
Fascaplysin[1]
Flavopiridol[10]
N- (2-[11]
NU-6102[12]
P1446A-05[4]
P276-00[4]
PD-0332991[4]
PD-332991[3]
PD0183813[1]
PYRAZOLOPYRIDAZINE 1[13]
PYRAZOLOPYRIDAZINE 2[13]
Purvalanol[14]
R547[4]
Ro 31-7453[3]
ZK 304709[4]
MultitargetAG-024322[4]
Capridine-beta[5]
P276-00[4]
PD-0332991[4]
R547[4]
Ro 31-7453[3]
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 2Enhanced malignant tumorigenesis in Cdk4 transgenic mice. Oncogene. 2004 Mar 11;23(10):1863-73. 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 5Agreement signed with Prostagenics to develop prostate cancer treatment. Innovate Oncology, Inc.. 2005 To Reference
Ref 6J Med Chem. 2001 Dec 20;44(26):4615-27.Structure-based generation of a new class of potent Cdk4 inhibitors: new de novo design strategy and library design. To Reference
Ref 7J Nat Prod. 2000 Jun;63(6):739-45.Anthraquinones and betaenone derivatives from the sponge-associated fungus Microsphaeropsis species: novel inhibitors of protein kinases. To Reference
Ref 8J Med Chem. 2006 Feb 23;49(4):1271-81.Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. To Reference
Ref 9J 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 10Zvelebil MJ: Flavopiridol (Hoechst AG). IDrugs. 1998 Jun;1(2):241-6. To Reference
Ref 11Bioorg Med Chem. 2008 Aug 15;16(16):7728-39. Epub 2008 Jul 8.Design, synthesis and biological evaluation of new tryptamine and tetrahydro-beta-carboline-based selective inhibitors of CDK4. To Reference
Ref 12J Med Chem. 2006 Sep 7;49(18):5470-7.Dissecting the determinants of cyclin-dependent kinase 2 and cyclin-dependent kinase 4 inhibitor selectivity. To Reference
Ref 13J Med Chem. 2004 Sep 9;47(19):4716-30.N-Phenyl-4-pyrazolo[1,5-b]pyridazin-3-ylpyrimidin-2-amines as potent and selective inhibitors of glycogen synthase kinase 3 with good cellular efficacy. To Reference
Ref 14Overington 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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