Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00261

Target Information
NamePlatelet-derived growth factor receptor    
Type of targetSuccessful target    
SynonymsPDGF-R    
PDGFR kinase    
Platelet-derived growth factor receptor tyrosine kinase    
DiseaseCancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[1]
Chronic myelomonocytic leukemia
[ICD9: 208.9   ICD10: C91-C95]
[2]
Glioblastoma multiforme
[ICD9: 191   ICD10: C71]
[2]
Drug(s)BecaplerminApprovedDiabetes mellitus[3]
Pazopanib HClApprovedRenal cell carcinoma[4]
CT-102LaunchedDiabetic foot ulcers[5]
ImatinibLaunchedChronic myelogenous leukemia [6]
SunitinibLaunchedAdvanced renal cell carcinoma[7][8][6][9]
Sunitinib malatePhase IVMetastatic Renal Cell Carcinoma; Gastrointestinal Stromal Tumors[10][11][6]
AxitinibPhase IIIRenal Cell Carcinoma[6][10][12]
ImatinibPhase IIIIntestinal cancer & myeloid leukemia[6]
MotesanibPhase IIINon-small cell lung cancer[13][14][15]
NilotinibPhase IIILeukemia[6]
NintedanibPhase IIINon-small cell lung cancer (NSCLC)
NintedanibPhase IIIOvarian cancer
PazopanibPhase IIIAdvanced / metastatic renal cancer[6][16][17]
PazopanibPhase II completedSolid tumours, NSCLC[6][16][17]
AxitinibPhase IILung Cancer; Thyroid Cancer[6][10][12]
ImatinibPhase IIGlioma, lung, prostate, solid tumours[6]
MotesanibPhase IIBreast cancer[13][14][15]
NilotinibPhase IIALL, CML, GIST[6]
SunitinibPhase IIAdvanced renal cell carcinoma[7][8][6][9]
Sunitinib malatePhase IISoft Tissue Sarcoma[10][11][6]
TKI258Phase I/IIAdvanced/ Metastatic Renal Cell Cancer[6]
BAY-57-9352Phase IVarious cancers[6]
MP470Phase ISolid Tumors[18]
Motesanib diphosphatePhase IProgressive non-small cell lung cancer[19][14]
X-82Phase IAdvanced solid tumors
CP-868596Discontinued in Phase IVarious Cancers[6]
SU-6668DiscontinuedAdvanced solid tumours[6][20]
BioChemical ClassTransferases transferring phosphorus-containing groups    
EC NumberEC 2.7.1.112
PathwayCalcium signaling pathway
Colorectal cancer
Cytokine-cytokine receptor interaction
Focal adhesion
Gap junction
Glioma
MAPK signaling pathway
Melanoma
Pathways in cancer
Prostate cancer
Regulation of actin cytoskeleton
Related US Patent6,566,075
6,642,232
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
InhibitorAxitinib[6][10][12]
BAY-57-9352[6]
Becaplermin[3]
CP-868596[6]
Imatinib[6]
MP470[18]
Motesanib[13][14][15]
Motesanib diphosphate[19][14]
Nilotinib[6]
Pazopanib[6][16][17]
Pazopanib HCl[4]
SU-6668[6][20]
Sunitinib[7][8][6][9]
Sunitinib malate[10][11][6]
TKI258[6]
Trapidil[21]
ActivatorCT-102[5]
PDGF gene therapy[5]
BinderAlkaloid staurosporin
MultitargetAxitinib[6][10][12]
BAY-57-9352[6]
Imatinib[6]
MP470[18]
Motesanib[13][14][15]
Motesanib diphosphate[19][14]
Nilotinib[6]
Pazopanib[6][16][17]
Pazopanib HCl[4]
SU-6668[6][20]
Sunitinib[7][8][6][9]
Sunitinib malate[10][11][6]
TKI258[6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Growth factor receptors as therapeutic targets: strategies to inhibit the insulin-like growth factor I receptor. Oncogene. 2003 Sep 29;22(42):6589-97. To Reference
Ref 2Targeting PDGF receptors in cancer--rationales and proof of concept clinical trials. Adv Exp Med Biol. 2003;532:141-51. To Reference
Ref 3Drugs and their molecular targets: an updated overview. Fundam Clin Pharmacol. 2008 Feb;22(1):1-18. To Reference
Ref 4Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. To Reference
Ref 5Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24. To Reference
Ref 6A 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 7FLT3 inhibition and mechanisms of drug resistance in mutant FLT3-positive AML. Drug Resist Updat. 2009 Jun;12(3):81-9. Epub 2009 May 20. To Reference
Ref 8FMS-like tyrosine kinase 3-internal tandem duplication tyrosine kinase inhibitors display a nonoverlapping profile of resistance mutations in vitro. Cancer Res. 2009 Apr 1;69(7):3032-41. Epub 2009 Mar 24. To Reference
Ref 9Multi-target therapeutics: when the whole is greater than the sum of the parts. Drug Discov Today. 2007 Jan;12(1-2):34-42. Epub 2006 Nov 28. To Reference
Ref 10Pfizer. Product Development Pipeline. March 31 2009. To Reference
Ref 11Sunitinib (Sutent, SU11248), a small-molecule receptor tyrosine kinase inhibitor, blocks function of the ATP-binding cassette (ABC) transporters P-glycoprotein (ABCB1) and ABCG2. Drug Metab Dispos. 2009 Feb;37(2):359-65. Epub 2008 Oct 29. To Reference
Ref 12Pfizer. Report of Pfizer. July 28 2008. To Reference
Ref 13Amgen. Product Development Pipeline. February 6 2009. To Reference
Ref 14Phase II study of safety and efficacy of motesanib in patients with progressive or symptomatic, advanced or metastatic medullary thyroid cancer. J Clin Oncol. 2009 Aug 10;27(23):3794-801. Epub 2009 Jun 29. To Reference
Ref 15Amgen. Report of Amgen. 2009. To Reference
Ref 16GSK. Product Development Pipeline. February 2009. To Reference
Ref 17Pazopanib, a VEGF receptor tyrosine kinase inhibitor for cancer therapy. Curr Opin Investig Drugs. 2008 Dec;9(12):1324-35. To Reference
Ref 18MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer. BMC Cancer. 2009 May 11;9:142. To Reference
Ref 19Takeda. Product Development Pipeline. July 31 2009. To Reference
Ref 20Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies. Clin Cancer Res. 2005 Sep 1;11(17):6240-6. To Reference
Ref 21Osteitis fibrosa is mediated by Platelet-Derived Growth Factor-A via a phosphoinositide 3-kinase-dependent signaling pathway in a rat model for chronic hyperparathyroidism. Endocrinology. 2008 Nov;149(11):5735-46. Epub 2008 Jul 17. To Reference



 

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