Target Information

Target General Infomation
Target ID
T59102
Former ID
TTDR01217
Target Name
Beta platelet-derived growth factor receptor
Gene Name
PDGFRB
Synonyms
Beta-PDGFR; CD140b antigen; PDGF-R-beta; Platelet-derived growth factor receptor beta; PDGFRB
Target Type
Successful
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.
BioChemical Class
Kinase
Target Validation
T59102
UniProt ID
P09619
EC Number
EC 2.7.10.1
Sequence
MRLPGAMPALALKGELLLLSLLLLLEPQISQGLVVTPPGPELVLNVSSTFVLTCSGSAPV
VWERMSQEPPQEMAKAQDGTFSSVLTLTNLTGLDTGEYFCTHNDSRGLETDERKRLYIFV
PDPTVGFLPNDAEELFIFLTEITEITIPCRVTDPQLVVTLHEKKGDVALPVPYDHQRGFS
GIFEDRSYICKTTIGDREVDSDAYYVYRLQVSSINVSVNAVQTVVRQGENITLMCIVIGN
EVVNFEWTYPRKESGRLVEPVTDFLLDMPYHIRSILHIPSAELEDSGTYTCNVTESVNDH
QDEKAINITVVESGYVRLLGEVGTLQFAELHRSRTLQVVFEAYPPPTVLWFKDNRTLGDS
SAGEIALSTRNVSETRYVSELTLVRVKVAEAGHYTMRAFHEDAEVQLSFQLQINVPVRVL
ELSESHPDSGEQTVRCRGRGMPQPNIIWSACRDLKRCPRELPPTLLGNSSEEESQLETNV
TYWEEEQEFEVVSTLRLQHVDRPLSVRCTLRNAVGQDTQEVIVVPHSLPFKVVVISAILA
LVVLTIISLIILIMLWQKKPRYEIRWKVIESVSSDGHEYIYVDPMQLPYDSTWELPRDQL
VLGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGP
HLNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQHHSDKRRPPSAELYSNAL
PVGLPLPSHVSLTGESDGGYMDMSKDESVDYVPMLDMKGDVKYADIESSNYMAPYDNYVP
SAPERTCRATLINESPVLSYMDLVGFSYQVANGMEFLASKNCVHRDLAARNVLICEGKLV
KICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLG
GTPYPELPMNEQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFEIRPPFSQLVLLLER
LLGEGYKKKYQQVDEEFLRSDHPAILRSQARLPGFHGLRSPLDTSSVLYTAVQPNEGDND
YIIPLPDPKPEVADEGPLEGSPSLASSTLNEVNTSSTISCDSPLEPQDEPEPEPQLELQV
EPEPELEQLPDSGCPAPRAEAEDSFL
Drugs and Mode of Action
Drug(s) Becaplermin Drug Info Approved Diabetes [1]
Sorafenib Drug Info Approved Advanced renal cell carcinoma [2], [3]
E-3810 Drug Info Phase 3 Solid tumours [4], [5]
Sorafenib Drug Info Phase 3 Hepatocellular carcinoma; NSCLC; Melanoma [6], [3]
Famitinib Drug Info Phase 2 Cancer [7], [8]
Sorafenib Drug Info Phase 2 Myelodysplastic syndrome; AML; Head and neck cancer; Breast cancer; Pancreatic cancer [6], [3]
XL-820 Drug Info Phase 2 Solid tumours [9]
MK-2461 Drug Info Phase 1/2 Alzheimer disease [10]
SNN-0031 Drug Info Phase 1/2 Brain injury [11]
TAK-593 Drug Info Phase 1 Cancer [12]
CDP-860 Drug Info Discontinued in Phase 2 Solid tumours [13]
SRI-62-834 Drug Info Discontinued in Phase 2 Solid tumours [14]
CEP-2563 Drug Info Discontinued in Phase 1 Solid tumours [15]
AG1295 Drug Info Terminated Discovery agent [16], [17]
RG-13022 Drug Info Terminated Discovery agent [18]
Inhibitor (1H-indol-2-yl)(5-methoxy-1H-indol-2-yl)methanone Drug Info [19]
(1H-indol-2-yl)(5-phenoxy-1H-indol-2-yl)methanone Drug Info [19]
(1H-indol-2-yl)(6-methoxy-1H-indol-2-yl)methanone Drug Info [19]
(2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamine Drug Info [20]
(5-fluoro-1H-indol-2-yl)-(1H-indol-2-yl)methanone Drug Info [19]
(5-hydroxy-1H-indol-2-yl)(1H-indol-2-yl)methanone Drug Info [19]
(benzo[b]furan-2-yl)-(1H-indol-2-yl)methanone Drug Info [21]
1-Phenyl-1H-benzoimidazol-5-ol Drug Info [22]
1-Phenyl-1H-benzoimidazole Drug Info [22]
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Drug Info [23]
3-((E)-Styryl)-quinoline Drug Info [24]
3-(1H-Indol-3-yl)-6,7-dimethoxy-quinoline Drug Info [24]
3-(1H-Indol-3-yl)-quinoline Drug Info [24]
3-(2-Cyclohexyl-ethyl)-6,7-dimethoxy-quinoline Drug Info [24]
3-(3,4-Dichloro-phenyl)-6,7-dimethoxy-quinoline Drug Info [24]
3-(3,4-Difluoro-phenyl)-6,7-dimethoxy-quinoline Drug Info [24]
3-(3,4-Dimethoxy-phenyl)-6,7-dimethoxy-quinoline Drug Info [24]
3-(3-Fluoro-phenyl)-6,7-dimethoxy-quinoline Drug Info [24]
3-(4-dimethylamino-benzylidenyl)-2-indolinone Drug Info [25]
3-(4-Fluoro-phenyl)-6,7-dimethoxy-quinoline Drug Info [24]
3-(6,7-Dimethoxy-quinolin-4-yloxy)-phenol Drug Info [26]
3-(6,7-Dimethoxy-quinolin-4-yloxy)-phenylamine Drug Info [26]
3-Benzimidazol-2-ylhydroquinolin-2-one Drug Info [27]
3-Benzyloxy-6,7-dimethoxy-quinoline Drug Info [24]
3-Cyclohexylethynyl-6,7-dimethoxy-quinoline Drug Info [24]
3-Cyclopent-1-enyl-6,7-dimethoxy-quinoline Drug Info [24]
3-Cyclopentyl-6,7-dimethoxy-quinoline Drug Info [24]
3-Pyridin-3-yl-quinoline-6,7-diol Drug Info [24]
3-Pyridin-4-yl-quinolin-7-ol Drug Info [28]
3-Pyridin-4-yl-quinoline Drug Info [28]
3-Pyridin-4-yl-quinoline-5,7-diol Drug Info [28]
3-Thiophen-3-yl-quinoline Drug Info [24]
4-(2,3-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Drug Info [26]
4-(3,4-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Drug Info [26]
4-(3,5-Dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Drug Info [26]
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinazoline Drug Info [26]
4-(3-Bromo-phenoxy)-6,7-dimethoxy-quinoline Drug Info [26]
4-(3-Ethoxy-phenoxy)-6,7-dimethoxy-quinoline Drug Info [26]
4-(3-Ethyl-phenoxy)-6,7-dimethoxy-quinoline Drug Info [26]
4-(3-Fluoro-phenoxy)-6,7-dimethoxy-quinoline Drug Info [26]
4-(5-Methoxy-benzoimidazol-1-yl)-phenylamine Drug Info [29]
4-(6,7-Dimethoxy-quinolin-3-yl)-benzoic acid Drug Info [24]
4-(6,7-Dimethoxy-quinolin-3-yl)-phenol Drug Info [24]
4-Benzoimidazol-1-yl-phenylamine Drug Info [22]
5,6,7-Trimethoxy-3-pyridin-4-yl-quinoline Drug Info [28]
5,7-Dimethoxy-3-pyridin-4-yl-quinoline Drug Info [28]
5,7-Dimethoxy-3-thiophen-3-yl-quinoline Drug Info [24]
5,7-Dimethyl-3-thiophen-3-yl-quinoline Drug Info [24]
5-(6,7-Dimethoxy-quinolin-3-yl)-1H-pyridin-2-one Drug Info [24]
5-Methoxy-1-phenyl-1H-benzoimidazole Drug Info [22]
6,7-Dichloro-3-thiophen-3-yl-quinoline Drug Info [24]
6,7-Difluoro-3-thiophen-3-yl-quinoline Drug Info [24]
6,7-Dimethoxy-3-((E)-styryl)-quinoline Drug Info [24]
6,7-Dimethoxy-3-(3-methoxy-phenyl)-quinoline Drug Info [24]
6,7-Dimethoxy-3-(4-methoxy-phenyl)-quinoline Drug Info [24]
6,7-Dimethoxy-3-(4-nitro-phenyl)-quinoline Drug Info [24]
6,7-Dimethoxy-3-p-tolyl-quinoline Drug Info [24]
6,7-Dimethoxy-3-phenyl-quinoline Drug Info [24]
6,7-Dimethoxy-3-phenylethynyl-quinoline Drug Info [24]
6,7-Dimethoxy-3-pyridin-3-yl-quinoline Drug Info [24]
6,7-Dimethoxy-3-pyridin-4-yl-quinoline Drug Info [28]
6,7-Dimethoxy-3-thiophen-2-yl-quinoline Drug Info [24]
6,7-Dimethoxy-4-(2-methoxy-phenoxy)-quinoline Drug Info [26]
6,7-Dimethoxy-4-(3-methoxy-phenoxy)-quinoline Drug Info [26]
6,7-Dimethoxy-4-(3-nitro-phenoxy)-quinoline Drug Info [26]
6,7-Dimethoxy-4-(4-methoxy-phenoxy)-quinoline Drug Info [26]
6,7-Dimethoxy-4-m-tolyloxy-quinoline Drug Info [26]
6,7-Dimethoxy-4-phenoxy-quinoline Drug Info [26]
6-Methoxy-3-pyridin-4-yl-quinoline Drug Info [28]
6-Methoxy-3-thiophen-3-yl-quinoline Drug Info [24]
7-Chloro-3-pyridin-4-yl-quinoline Drug Info [28]
7-Fluoro-3-thiophen-3-yl-quinoline Drug Info [24]
7-Methoxy-3-pyridin-4-yl-quinoline Drug Info [28]
7-Methoxy-3-thiophen-3-yl-quinoline Drug Info [24]
7-Thiophen-3-yl-[1,3]dioxolo[4,5-g]quinoline Drug Info [24]
AG1295 Drug Info [21]
AGL 2043 Drug Info [30]
Benzyl-(6,7-dimethoxy-quinolin-3-yl)-amine Drug Info [24]
Bis(5-acetoxybenzo[b]furan-2-yl)methanone Drug Info [21]
Bis(5-aminobenzo[b]furan-2-yl)methanone Drug Info [21]
Bis(5-hydroxybenzo[b]furan-2-yl)methanone Drug Info [21]
Bis(5-methoxybenzo[b]furan-2-yl)methanone Drug Info [21]
Bis(6-hydroxybenzo[b]furan-2-yl)methanone Drug Info [21]
Bis(benzo[b]furan-2-yl)methanone Drug Info [21]
Bis-(5-hydroxy-1H-indol-2-yl)-methanone Drug Info [19]
BMS-536924 Drug Info [31]
CEP-2563 Drug Info [32]
compound 8h Drug Info [33]
CP-673451 Drug Info [34]
Di(1H-indol-2-yl)methanone Drug Info [19]
E-3810 Drug Info [35]
Famitinib Drug Info [7]
Flt-3 inhibitor II Drug Info [19]
GTP-14564 Drug Info [36]
JNJ-10198409 Drug Info [20]
Ki-11502 Drug Info [37]
Ki-20227 Drug Info [38]
MK-2461 Drug Info [10]
PD-0166326 Drug Info [39]
PD-0173952 Drug Info [39]
PD-0173955 Drug Info [39]
PD-0173956 Drug Info [39]
PD-0173958 Drug Info [39]
PD-0179483 Drug Info [39]
PD-0180970 Drug Info [39]
PDGF receptor tyrosine kinase inhibitor III Drug Info [40]
RG-13022 Drug Info [24]
Ro-4396686 Drug Info [41]
RPR-101511 Drug Info [24]
RPR-108514A Drug Info [42]
SEMAXINIB Drug Info [43]
SRI-62-834 Drug Info [32]
SU-11652 Drug Info [43]
TG-100435 Drug Info [44]
XL-820 Drug Info [45]
Modulator Becaplermin Drug Info [46]
CDP-860 Drug Info [47]
SNN-0031 Drug Info
Sorafenib Drug Info [2]
TAK-593 Drug Info [12], [48]
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
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REF 28J Med Chem. 1994 Aug 19;37(17):2627-9.5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase.
REF 29J 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 30Tricyclic quinoxalines as potent kinase inhibitors of PDGFR kinase, Flt3 and Kit. Bioorg Med Chem. 2003 May 1;11(9):2007-18.
REF 31J 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.
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REF 34Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer Res. 2005 Feb 1;65(3):957-66.
REF 35E-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.
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REF 37Identification of potent and selective inhibitors of PDGF receptor autophosphorylation. J Med Chem. 2006 Apr 6;49(7):2186-92.
REF 38A 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.
REF 39Biochem 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 40Potent 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 41Bioorg 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 42The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4-d]pyrimidines, inhibitors of CSF-1R tyrosine kinase activity, Bioorg. Med. Chem. Lett. 7(4):421-424 (1997).
REF 43J 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 44Bioorg 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 45National Cancer Institute Drug Dictionary (drug id 452042).
REF 46Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 47Blockade 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 48Biochemical characterization of TAK-593, a novel VEGFR/PDGFR inhibitor with a two-step slow binding mechanism. Biochemistry. 2011 Feb 8;50(5):738-51. doi: 10.1021/bi101777f. Epub 2011 Jan 10.

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