Target Information
| Target General Information | Top | |||||
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| Target ID |
T52624
(Former ID: TTDS00261)
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| Target Name |
Platelet-derived growth factor receptor (PDGFR)
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| Synonyms |
Platelet-derived growth factor receptor tyrosine kinase; PDGFR kinase; PDGF-R
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| Gene Name |
NO-GeName
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 8 Target-related Diseases | + | ||||
| 1 | Colorectal cancer [ICD-11: 2B91] | |||||
| 2 | Diabetic foot ulcer [ICD-11: BD54] | |||||
| 3 | Idiopathic interstitial pneumonitis [ICD-11: CB03] | |||||
| 4 | Mature B-cell lymphoma [ICD-11: 2A85] | |||||
| 5 | Myeloproliferative neoplasm [ICD-11: 2A20] | |||||
| 6 | Renal cell carcinoma [ICD-11: 2C90] | |||||
| 7 | Coronary atherosclerosis [ICD-11: BA80] | |||||
| 8 | Myocardial infarction [ICD-11: BA41-BA43] | |||||
| UniProt ID | ||||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Approved Drug(s) | [+] 2 Approved Drugs | + | ||||
| 1 | Intedanib | Drug Info | Approved | Colorectal cancer | [5] | |
| 2 | Pazopanib HCl | Drug Info | Approved | Renal cell carcinoma | [6] | |
| Clinical Trial Drug(s) | [+] 4 Clinical Trial Drugs | + | ||||
| 1 | Rosiglitazone + metformin | Drug Info | Phase 3 | Diabetic complication | [8] | |
| 2 | TKI258 | Drug Info | Phase 3 | Renal cell carcinoma | [9] | |
| 3 | BAY-57-9352 | Drug Info | Phase 2 | Solid tumour/cancer | [11] | |
| 4 | X-82 | Drug Info | Phase 2 | Age-related macular degeneration | [12] | |
| Patented Agent(s) | [+] 1 Patented Agents | + | ||||
| 1 | PMID25623274-Compound-WO2014132220C2 | Drug Info | Patented | Pulmonary arterial hypertension | [13] | |
| Discontinued Drug(s) | [+] 2 Discontinued Drugs | + | ||||
| 1 | Motesanib | Drug Info | Discontinued in Phase 3 | Non-small-cell lung cancer | [14], [15] | |
| 2 | CGP-53716 | Drug Info | Terminated | Solid tumour/cancer | [16] | |
| Mode of Action | [+] 3 Modes of Action | + | ||||
| Modulator | [+] 3 Modulator drugs | + | ||||
| 1 | Intedanib | Drug Info | [5] | |||
| 2 | X-82 | Drug Info | [18] | |||
| 3 | CGP-53716 | Drug Info | [22], [23], [24] | |||
| Inhibitor | [+] 6 Inhibitor drugs | + | ||||
| 1 | Pazopanib HCl | Drug Info | [6] | |||
| 2 | Rosiglitazone + metformin | Drug Info | [1], [17] | |||
| 3 | TKI258 | Drug Info | [1] | |||
| 4 | BAY-57-9352 | Drug Info | [1] | |||
| 5 | PMID25623274-Compound-WO2014132220C2 | Drug Info | [13] | |||
| 6 | Motesanib | Drug Info | [19], [20], [21] | |||
| Activator | [+] 1 Activator drugs | + | ||||
| 1 | PDGF gene therapy | Drug Info | [4] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Co-Targets | Top | |||||
|---|---|---|---|---|---|---|
| Co-Targets | ||||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| Target QSAR Model | ||||||
| References | Top | |||||
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| REF 1 | A 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. | |||||
| REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5687). | |||||
| REF 3 | Emerging treatments for pulmonary arterial hypertension. Expert Opin Emerg Drugs. 2006 Nov;11(4):609-19. | |||||
| REF 4 | Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24. | |||||
| REF 5 | 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81. | |||||
| REF 6 | Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. | |||||
| REF 7 | ClinicalTrials.gov (NCT00914420) Optical Coherence Tomography (OCT) Evaluation of Re-endothelization: A Comparison of the Intrepide Stent Versus Taxus . U.S. National Institutes of Health. | |||||
| REF 8 | ClinicalTrials.gov (NCT00499707) Efficacy and Safety Study of Rosiglitazone/Metformin Therapy vs Rosiglitazone and Metformin in Type 2 Diabetes Subjects. U.S. National Institutes of Health. | |||||
| REF 9 | ClinicalTrials.gov (NCT01223027) Study of Dovitinib Versus Sorafenib in Patients With Metastatic Renal Cell Carcinoma. U.S. National Institutes of Health. | |||||
| REF 10 | ClinicalTrials.gov (NCT03848611) CM082 and JS001 in Patients With Advanced Non-Small Cell Lung Cancer (NSCLC).. U.S. National Institutes of Health. | |||||
| REF 11 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021605) | |||||
| REF 12 | ClinicalTrials.gov (NCT02348359) X-82 to Treat Age-related Macular Degeneration. U.S. National Institutes of Health. | |||||
| REF 13 | Evaluation of WO-2014132220, selective PDGFR inhibitors for the treatment of pulmonary arterial hypertension.Expert Opin Ther Pat. 2015 Apr;25(4):493-9. | |||||
| REF 14 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5660). | |||||
| REF 15 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011016) | |||||
| REF 16 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005535) | |||||
| REF 17 | Dose-finding study of the multitargeted tyrosine kinase inhibitor SU6668 in patients with advanced malignancies. Clin Cancer Res. 2005 Sep 1;11(17):6240-6. | |||||
| REF 18 | National Cancer Institute Drug Dictionary (drug id 695817). | |||||
| REF 19 | Clinical pipeline report, company report or official report of Amgen (2009). | |||||
| REF 20 | Phase 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. | |||||
| REF 21 | Axitinib for renal cell carcinoma. Expert Opin Investig Drugs. 2008 May;17(5):741-8. | |||||
| REF 22 | Inhibition of cell growth: effects of the tyrosine kinase inhibitor CGP 53716. J Pharmacol Exp Ther. 1997 Oct;283(1):402-10. | |||||
| REF 23 | Inhibition of platelet-derived growth factor receptor tyrosine kinase inhibits vascular smooth muscle cell migration and proliferation. FASEB J. 1997 Nov;11(13):1119-26. | |||||
| REF 24 | Role of platelet-derived growth factor in obliterative bronchiolitis (chronic rejection) in the rat. Am J Respir Crit Care Med. 1999 Oct;160(4):1324-32. | |||||
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