Target Information
Target General Infomation | |||||
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Target ID |
T59102
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Former ID |
TTDR01217
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Target Name |
Beta platelet-derived growth factor receptor
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Gene Name |
PDGFRB
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Synonyms |
Beta-PDGFR; CD140b antigen; PDGF-R-beta; Platelet-derived growth factor receptor beta; PDGFRB
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Target Type |
Successful
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Disease | Alzheimer disease [ICD9: 331; ICD10: G30] | ||||
Advanced renal cell carcinoma [ICD9: 189; ICD10: C64] | |||||
Brain injury [ICD10: S09.90] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1] | |||||
Hepatocellular carcinoma; NSCLC; Melanoma [ICD9: 155, 162, 172; ICD10: C22.0, C33, C34, C43] | |||||
Myelodysplastic syndrome; AML; Head and neck cancer; Breast cancer; Pancreatic cancer [ICD9: 140-149, 140-229, 157, 183, 205.0; ICD10: C07-C14, C25, C32, C33, C56, C92.0] | |||||
Non-small cell lung cancer [ICD10: C33-C34] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Function |
Tyrosine-protein kinase that acts as cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic development, cell proliferation, survival, differentiation, chemotaxis and migration. Plays an essential role in blood vessel development by promoting proliferation, migration and recruitment of pericytes and smooth muscle cells to endothelial cells. Plays a role in the migration of vascular smooth muscle cells and the formation of neointima at vascular injury sites. Required for normal development of the cardiovascular system. Required for normal recruitment of pericytes (mesangial cells) in the kidney glomerulus, and for normal formation of a branched network of capillaries in kidney glomeruli. Promotes rearrangement of the actin cytoskeleton and the formation of membrane ruffles. Binding of its cognate ligands - homodimeric PDGFB, heterodimers formed by PDGFA and PDGFB or homodimeric PDGFD -leads to the activation of several signaling cascades; the response depends on the nature of the bound ligand and is modulated by the formation of heterodimers between PDGFRA andPDGFRB. Phosphorylates PLCG1, PIK3R1, PTPN11, RASA1/GAP, CBL, SHC1 and NCK1. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5- trisphosphate, mobilization of cytosolic Ca(2+) and the activation of protein kinase C. Phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, leads to the activation of the AKT1signaling pathway. Phosphorylation of SHC1, or of the C-terminus of PTPN11, creates a binding site for GRB2, resulting in the activation of HRAS, RAF1 and down-stream MAP kinases, including MAPK1/ERK2 and/or MAPK3/ERK1. Promotes phosphorylation and activation of SRC family kinases. Promotes phosphorylation of PDCD6IP/ALIX and STAM. Receptor signaling is down-regulated by protein phosphatases thatdephosphorylate the receptor and its down-stream effectors, and by rapid internalization of the activated receptor.
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BioChemical Class |
Kinase
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Target Validation |
T59102
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UniProt ID | |||||
EC Number |
EC 2.7.10.1
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Sequence |
MRLPGAMPALALKGELLLLSLLLLLEPQISQGLVVTPPGPELVLNVSSTFVLTCSGSAPV
VWERMSQEPPQEMAKAQDGTFSSVLTLTNLTGLDTGEYFCTHNDSRGLETDERKRLYIFV PDPTVGFLPNDAEELFIFLTEITEITIPCRVTDPQLVVTLHEKKGDVALPVPYDHQRGFS GIFEDRSYICKTTIGDREVDSDAYYVYRLQVSSINVSVNAVQTVVRQGENITLMCIVIGN EVVNFEWTYPRKESGRLVEPVTDFLLDMPYHIRSILHIPSAELEDSGTYTCNVTESVNDH QDEKAINITVVESGYVRLLGEVGTLQFAELHRSRTLQVVFEAYPPPTVLWFKDNRTLGDS SAGEIALSTRNVSETRYVSELTLVRVKVAEAGHYTMRAFHEDAEVQLSFQLQINVPVRVL ELSESHPDSGEQTVRCRGRGMPQPNIIWSACRDLKRCPRELPPTLLGNSSEEESQLETNV TYWEEEQEFEVVSTLRLQHVDRPLSVRCTLRNAVGQDTQEVIVVPHSLPFKVVVISAILA LVVLTIISLIILIMLWQKKPRYEIRWKVIESVSSDGHEYIYVDPMQLPYDSTWELPRDQL VLGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGP HLNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQHHSDKRRPPSAELYSNAL PVGLPLPSHVSLTGESDGGYMDMSKDESVDYVPMLDMKGDVKYADIESSNYMAPYDNYVP SAPERTCRATLINESPVLSYMDLVGFSYQVANGMEFLASKNCVHRDLAARNVLICEGKLV KICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLG GTPYPELPMNEQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFEIRPPFSQLVLLLER LLGEGYKKKYQQVDEEFLRSDHPAILRSQARLPGFHGLRSPLDTSSVLYTAVQPNEGDND YIIPLPDPKPEVADEGPLEGSPSLASSTLNEVNTSSTISCDSPLEPQDEPEPEPQLELQV EPEPELEQLPDSGCPAPRAEAEDSFL |
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Drugs and Mode of Action | |||||
Drug(s) | Becaplermin | Drug Info | Approved | Diabetes | [536297] |
Sorafenib | Drug Info | Approved | Advanced renal cell carcinoma | [528230], [541050] | |
E-3810 | Drug Info | Phase 3 | Solid tumours | [524749], [542632] | |
Sorafenib | Drug Info | Phase 3 | Hepatocellular carcinoma; NSCLC; Melanoma | [537114], [541050] | |
Famitinib | Drug Info | Phase 2 | Cancer | [532104], [542811] | |
Sorafenib | Drug Info | Phase 2 | Myelodysplastic syndrome; AML; Head and neck cancer; Breast cancer; Pancreatic cancer | [537114], [541050] | |
XL-820 | Drug Info | Phase 2 | Solid tumours | [522178] | |
MK-2461 | Drug Info | Phase 1/2 | Alzheimer disease | [530708] | |
SNN-0031 | Drug Info | Phase 1/2 | Brain injury | [525140] | |
TAK-593 | Drug Info | Phase 1 | Cancer | [532187] | |
CDP-860 | Drug Info | Discontinued in Phase 2 | Solid tumours | [546773] | |
SRI-62-834 | Drug Info | Discontinued in Phase 2 | Solid tumours | [544742] | |
CEP-2563 | Drug Info | Discontinued in Phase 1 | Solid tumours | [546416] | |
AG1295 | Drug Info | Terminated | Discovery agent | [541205], [546396] | |
RG-13022 | Drug Info | Terminated | Discovery agent | [544752] | |
Inhibitor | (1H-indol-2-yl)(5-methoxy-1H-indol-2-yl)methanone | Drug Info | [528209] | ||
(1H-indol-2-yl)(5-phenoxy-1H-indol-2-yl)methanone | Drug Info | [528209] | |||
(1H-indol-2-yl)(6-methoxy-1H-indol-2-yl)methanone | Drug Info | [528209] | |||
(2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine | Drug Info | [527932] | |||
(5-fluoro-1H-indol-2-yl)-(1H-indol-2-yl)methanone | Drug Info | [528209] | |||
(5-hydroxy-1H-indol-2-yl)(1H-indol-2-yl)methanone | Drug Info | [528209] | |||
(benzo[b]furan-2-yl)-(1H-indol-2-yl)methanone | Drug Info | [528608] | |||
1-Phenyl-1H-benzoimidazol-5-ol | Drug Info | [534808] | |||
1-Phenyl-1H-benzoimidazole | Drug Info | [534808] | |||
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole | Drug Info | [528122] | |||
3-((E)-Styryl)-quinoline | Drug Info | [533862] | |||
3-(1H-Indol-3-yl)-6,7-dimethoxy-quinoline | Drug Info | [533862] | |||
3-(1H-Indol-3-yl)-quinoline | Drug Info | [533862] | |||
3-(2-Cyclohexyl-ethyl)-6,7-dimethoxy-quinoline | Drug Info | [533862] | |||
3-(3,4-Dichloro-phenyl)-6,7-dimethoxy-quinoline | Drug Info | [533862] | |||
3-(3,4-Difluoro-phenyl)-6,7-dimethoxy-quinoline | Drug Info | [533862] | |||
3-(3,4-Dimethoxy-phenyl)-6,7-dimethoxy-quinoline | Drug Info | [533862] | |||
3-(3-Fluoro-phenyl)-6,7-dimethoxy-quinoline | Drug Info | [533862] | |||
3-(4-dimethylamino-benzylidenyl)-2-indolinone | Drug Info | [530858] | |||
3-(4-Fluoro-phenyl)-6,7-dimethoxy-quinoline | Drug Info | [533862] | |||
3-(6,7-Dimethoxy-quinolin-4-yloxy)-phenol | Drug Info | [551331] | |||
3-(6,7-Dimethoxy-quinolin-4-yloxy)-phenylamine | Drug Info | [551331] | |||
3-Benzimidazol-2-ylhydroquinolin-2-one | Drug Info | [529891] | |||
3-Benzyloxy-6,7-dimethoxy-quinoline | Drug Info | [533862] | |||
3-Cyclohexylethynyl-6,7-dimethoxy-quinoline | Drug Info | [533862] | |||
3-Cyclopent-1-enyl-6,7-dimethoxy-quinoline | Drug Info | [533862] | |||
3-Cyclopentyl-6,7-dimethoxy-quinoline | Drug Info | [533862] | |||
3-Pyridin-3-yl-quinoline-6,7-diol | Drug Info | [533862] | |||
3-Pyridin-4-yl-quinolin-7-ol | Drug Info | [533872] | |||
3-Pyridin-4-yl-quinoline | Drug Info | [533872] | |||
3-Pyridin-4-yl-quinoline-5,7-diol | Drug Info | [533872] | |||
3-Thiophen-3-yl-quinoline | Drug Info | [533862] | |||
4-(2,3-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline | Drug Info | [551331] | |||
4-(3,4-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline | Drug Info | [551331] | |||
4-(3,5-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline | Drug Info | [551331] | |||
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline | Drug Info | [551331] | |||
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline | Drug Info | [551331] | |||
4-(3-Ethoxy-phenoxy)-6,7-dimethoxy-quinoline | Drug Info | [551331] | |||
4-(3-Ethyl-phenoxy)-6,7-dimethoxy-quinoline | Drug Info | [551331] | |||
4-(3-Fluoro-phenoxy)-6,7-dimethoxy-quinoline | Drug Info | [551331] | |||
4-(5-Methoxy-benzoimidazol-1-yl)-phenylamine | Drug Info | [525530] | |||
4-(6,7-Dimethoxy-quinolin-3-yl)-benzoic acid | Drug Info | [533862] | |||
4-(6,7-Dimethoxy-quinolin-3-yl)-phenol | Drug Info | [533862] | |||
4-Benzoimidazol-1-yl-phenylamine | Drug Info | [534808] | |||
5,6,7-Trimethoxy-3-pyridin-4-yl-quinoline | Drug Info | [533872] | |||
5,7-Dimethoxy-3-pyridin-4-yl-quinoline | Drug Info | [533872] | |||
5,7-Dimethoxy-3-thiophen-3-yl-quinoline | Drug Info | [533862] | |||
5,7-Dimethyl-3-thiophen-3-yl-quinoline | Drug Info | [533862] | |||
5-(6,7-Dimethoxy-quinolin-3-yl)-1H-pyridin-2-one | Drug Info | [533862] | |||
5-Methoxy-1-phenyl-1H-benzoimidazole | Drug Info | [534808] | |||
6,7-Dichloro-3-thiophen-3-yl-quinoline | Drug Info | [533862] | |||
6,7-Difluoro-3-thiophen-3-yl-quinoline | Drug Info | [533862] | |||
6,7-Dimethoxy-3-((E)-styryl)-quinoline | Drug Info | [533862] | |||
6,7-Dimethoxy-3-(3-methoxy-phenyl)-quinoline | Drug Info | [533862] | |||
6,7-Dimethoxy-3-(4-methoxy-phenyl)-quinoline | Drug Info | [533862] | |||
6,7-Dimethoxy-3-(4-nitro-phenyl)-quinoline | Drug Info | [533862] | |||
6,7-Dimethoxy-3-p-tolyl-quinoline | Drug Info | [533862] | |||
6,7-Dimethoxy-3-phenyl-quinoline | Drug Info | [533862] | |||
6,7-Dimethoxy-3-phenylethynyl-quinoline | Drug Info | [533862] | |||
6,7-Dimethoxy-3-pyridin-3-yl-quinoline | Drug Info | [533862] | |||
6,7-Dimethoxy-3-pyridin-4-yl-quinoline | Drug Info | [533872] | |||
6,7-Dimethoxy-3-thiophen-2-yl-quinoline | Drug Info | [533862] | |||
6,7-Dimethoxy-4-(2-methoxy-phenoxy)-quinoline | Drug Info | [551331] | |||
6,7-Dimethoxy-4-(3-methoxy-phenoxy)-quinoline | Drug Info | [551331] | |||
6,7-Dimethoxy-4-(3-nitro-phenoxy)-quinoline | Drug Info | [551331] | |||
6,7-Dimethoxy-4-(4-methoxy-phenoxy)-quinoline | Drug Info | [551331] | |||
6,7-Dimethoxy-4-m-tolyloxy-quinoline | Drug Info | [551331] | |||
6,7-Dimethoxy-4-phenoxy-quinoline | Drug Info | [551331] | |||
6-Methoxy-3-pyridin-4-yl-quinoline | Drug Info | [533872] | |||
6-Methoxy-3-thiophen-3-yl-quinoline | Drug Info | [533862] | |||
7-Chloro-3-pyridin-4-yl-quinoline | Drug Info | [533872] | |||
7-Fluoro-3-thiophen-3-yl-quinoline | Drug Info | [533862] | |||
7-Methoxy-3-pyridin-4-yl-quinoline | Drug Info | [533872] | |||
7-Methoxy-3-thiophen-3-yl-quinoline | Drug Info | [533862] | |||
7-Thiophen-3-yl-[1,3]dioxolo[4,5-g]quinoline | Drug Info | [533862] | |||
AG1295 | Drug Info | [528608] | |||
AGL 2043 | Drug Info | [526588] | |||
Benzyl-(6,7-dimethoxy-quinolin-3-yl)-amine | Drug Info | [533862] | |||
Bis(5-acetoxybenzo[b]furan-2-yl)methanone | Drug Info | [528608] | |||
Bis(5-aminobenzo[b]furan-2-yl)methanone | Drug Info | [528608] | |||
Bis(5-hydroxybenzo[b]furan-2-yl)methanone | Drug Info | [528608] | |||
Bis(5-methoxybenzo[b]furan-2-yl)methanone | Drug Info | [528608] | |||
Bis(6-hydroxybenzo[b]furan-2-yl)methanone | Drug Info | [528608] | |||
Bis(benzo[b]furan-2-yl)methanone | Drug Info | [528608] | |||
Bis-(5-hydroxy-1H-indol-2-yl)-methanone | Drug Info | [528209] | |||
BMS-536924 | Drug Info | [527711] | |||
CEP-2563 | Drug Info | [531635] | |||
compound 8h | Drug Info | [531959] | |||
CP-673451 | Drug Info | [527429] | |||
Di(1H-indol-2-yl)methanone | Drug Info | [528209] | |||
E-3810 | Drug Info | [525382] | |||
Famitinib | Drug Info | [532104] | |||
Flt-3 inhibitor II | Drug Info | [528209] | |||
GTP-14564 | Drug Info | [526648] | |||
JNJ-10198409 | Drug Info | [527932] | |||
Ki-11502 | Drug Info | [528107] | |||
Ki-20227 | Drug Info | [528535] | |||
MK-2461 | Drug Info | [530708] | |||
PD-0166326 | Drug Info | [525862] | |||
PD-0173952 | Drug Info | [525862] | |||
PD-0173955 | Drug Info | [525862] | |||
PD-0173956 | Drug Info | [525862] | |||
PD-0173958 | Drug Info | [525862] | |||
PD-0179483 | Drug Info | [525862] | |||
PD-0180970 | Drug Info | [525862] | |||
PDGF receptor tyrosine kinase inhibitor III | Drug Info | [526865] | |||
RG-13022 | Drug Info | [533862] | |||
Ro-4396686 | Drug Info | [528018] | |||
RPR-101511 | Drug Info | [533862] | |||
RPR-108514A | Drug Info | [551338] | |||
SEMAXINIB | Drug Info | [526575] | |||
SRI-62-834 | Drug Info | [531635] | |||
SU-11652 | Drug Info | [526575] | |||
TG-100435 | Drug Info | [528527] | |||
XL-820 | Drug Info | [550402] | |||
Modulator | Becaplermin | Drug Info | [556264] | ||
CDP-860 | Drug Info | [527239] | |||
SNN-0031 | Drug Info | ||||
Sorafenib | Drug Info | [528230] | |||
TAK-593 | Drug Info | [532187], [553086] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | MAPK signaling pathway | ||||
Ras signaling pathway | |||||
Rap1 signaling pathway | |||||
Calcium signaling pathway | |||||
Cytokine-cytokine receptor interaction | |||||
PI3K-Akt signaling pathway | |||||
Focal adhesion | |||||
Gap junction | |||||
Regulation of actin cytoskeleton | |||||
HTLV-I infection | |||||
Pathways in cancer | |||||
MicroRNAs in cancer | |||||
Glioma | |||||
Prostate cancer | |||||
Melanoma | |||||
Central carbon metabolism in cancer | |||||
Choline metabolism in cancer | |||||
PANTHER Pathway | Angiogenesis | ||||
PDGF signaling pathway | |||||
Pathway Interaction Database | Signaling events mediated by PTP1B | ||||
Beta3 integrin cell surface interactions | |||||
S1P3 pathway | |||||
Nectin adhesion pathway | |||||
Signaling events mediated by TCPTP | |||||
SHP2 signaling | |||||
S1P1 pathway | |||||
Urokinase-type plasminogen activator (uPA) and uPAR-mediated signaling | |||||
PDGFR-beta signaling pathway | |||||
Validated targets of C-MYC transcriptional repression | |||||
PDGF receptor signaling network | |||||
Reactome | PIP3 activates AKT signaling | ||||
Constitutive Signaling by Aberrant PI3K in Cancer | |||||
RAF/MAP kinase cascade | |||||
WikiPathways | Regulation of Actin Cytoskeleton | ||||
MAPK Signaling Pathway | |||||
Osteoblast Signaling | |||||
Focal Adhesion | |||||
PIP3 activates AKT signaling | |||||
PDGF Pathway | |||||
Signaling Pathways in Glioblastoma | |||||
Signaling by PDGF | |||||
References | |||||
Ref 522178 | ClinicalTrials.gov (NCT00570635) A Phase 2 Study of XL820 in Adults With Advanced GIST Resistant to Imatinib and/or Sunitinib. U.S. National Institutes of Health. | ||||
Ref 524749 | ClinicalTrials.gov (NCT02135107) A Double-blind Comparative Study of the Efficacy and Safety of E3810 10mg Once and Twice Daily in Maintenance Therapy for PPI Resistant Gastroesophageal Reflux Disease Patients. U.S. National Institutes of Health. | ||||
Ref 525140 | ClinicalTrials.gov (NCT02408562) Study on Tolerability of Repeat i.c.v. Administration of sNN0031 Infusion Solution in Patients With PD. U.S. National Institutes of Health. | ||||
Ref 528230 | Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol. 2006;407:597-612. | ||||
Ref 530708 | MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33. | ||||
Ref 532104 | Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706. | ||||
Ref 532187 | Anti-angiogenic and anti-tumor effects of TAK-593, a potent and selective inhibitor of vascular endothelial growth factor and platelet-derived growth factor receptor tyrosine kinase. Cancer Sci. 2013Apr;104(4):486-94. | ||||
Ref 541050 | (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: 5711). | ||||
Ref 541205 | (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: 5914). | ||||
Ref 542632 | (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: 7649). | ||||
Ref 542811 | (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: 7886). | ||||
Ref 544742 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000818) | ||||
Ref 544752 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000854) | ||||
Ref 546396 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007894) | ||||
Ref 525382 | E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405. doi: 10.1158/0008-5472.CAN-10-2700. Epub 2011 Jan 6. | ||||
Ref 525530 | J Med Chem. 1999 Jul 1;42(13):2373-82.Structure-activity relationships for 5-substituted 1-phenylbenzimidazoles as selective inhibitors of the platelet-derived growth factor receptor. | ||||
Ref 525862 | Biochem Pharmacol. 2000 Oct 1;60(7):885-98.Biochemical and cellular effects of c-Src kinase-selective pyrido[2, 3-d]pyrimidine tyrosine kinase inhibitors. | ||||
Ref 526575 | J Med Chem. 2003 Mar 27;46(7):1116-9.Discovery of 5-[5-fluoro-2-oxo-1,2- dihydroindol-(3Z)-ylidenemethyl]-2,4- dimethyl-1H-pyrrole-3-carboxylic acid (2-diethylaminoethyl)amide, a novel tyrosine kinase inhibitor targeting vascular endothelial and platelet-derived growth factor receptor tyrosine kinase. | ||||
Ref 526588 | Tricyclic quinoxalines as potent kinase inhibitors of PDGFR kinase, Flt3 and Kit. Bioorg Med Chem. 2003 May 1;11(9):2007-18. | ||||
Ref 526648 | Selective cytotoxic mechanism of GTP-14564, a novel tyrosine kinase inhibitor in leukemia cells expressing a constitutively active Fms-like tyrosine kinase 3 (FLT3). J Biol Chem. 2003 Aug 29;278(35):32892-8. Epub 2003 Jun 18. | ||||
Ref 526865 | Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. 3. Replacement of quinazoline moiety and improvement of metabolic polymorphism of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives. J Med Chem. 2003 Nov 6;46(23):4910-25. | ||||
Ref 527239 | Blockade of platelet-derived growth factor receptor-beta by CDP860, a humanized, PEGylated di-Fab', leads to fluid accumulation and is associated with increased tumor vascularized volume. J Clin Oncol. 2005 Feb 10;23(5):973-81. Epub 2004 Oct 4. | ||||
Ref 527429 | Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer Res. 2005 Feb 1;65(3):957-66. | ||||
Ref 527711 | J Med Chem. 2005 Sep 8;48(18):5639-43.Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity. | ||||
Ref 527932 | J Med Chem. 2005 Dec 29;48(26):8163-73.(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells. | ||||
Ref 528018 | Bioorg Med Chem Lett. 2006 Apr 1;16(7):1950-3. Epub 2006 Feb 3.Biological evaluation of a multi-targeted small molecule inhibitor of tumor-induced angiogenesis. | ||||
Ref 528107 | Identification of potent and selective inhibitors of PDGF receptor autophosphorylation. J Med Chem. 2006 Apr 6;49(7):2186-92. | ||||
Ref 528122 | Bioorg Med Chem Lett. 2006 Jul 1;16(13):3595-9. Epub 2006 Apr 5.Design and structure-activity relationship of 3-benzimidazol-2-yl-1H-indazoles as inhibitors of receptor tyrosine kinases. | ||||
Ref 528209 | J Med Chem. 2006 Jun 1;49(11):3101-15.Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. | ||||
Ref 528230 | Sorafenib (BAY 43-9006, Nexavar), a dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases VEGFR/PDGFR in tumor vasculature. Methods Enzymol. 2006;407:597-612. | ||||
Ref 528527 | Bioorg Med Chem Lett. 2007 Feb 1;17(3):602-8. Epub 2006 Nov 7.Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays. | ||||
Ref 528535 | A c-fms tyrosine kinase inhibitor, Ki20227, suppresses osteoclast differentiation and osteolytic bone destruction in a bone metastasis model. Mol Cancer Ther. 2006 Nov;5(11):2634-43. | ||||
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