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
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 [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 522178ClinicalTrials.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 524749ClinicalTrials.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 525140ClinicalTrials.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 528230Sorafenib (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 530708MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
Ref 532104Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
Ref 532187Anti-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 536297Emerging drugs for diabetic foot ulcers. Expert Opin Emerg Drugs. 2006 Nov;11(4):709-24.
Ref 537114Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
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 544742Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000818)
Ref 544752Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000854)
Ref 546396Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007894)
Ref 546416Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007988)
Ref 546773Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010224)
Ref 525382E-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 525530J 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 525862Biochem 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 526575J 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 526588Tricyclic quinoxalines as potent kinase inhibitors of PDGFR kinase, Flt3 and Kit. Bioorg Med Chem. 2003 May 1;11(9):2007-18.
Ref 526648Selective 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 526865Potent 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 527239Blockade 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 527429Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451. Cancer Res. 2005 Feb 1;65(3):957-66.
Ref 527711J 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 527932J 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 528018Bioorg 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 528107Identification of potent and selective inhibitors of PDGF receptor autophosphorylation. J Med Chem. 2006 Apr 6;49(7):2186-92.
Ref 528122Bioorg 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 528209J 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 528230Sorafenib (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 528527Bioorg 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 528535A 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 528608Bioorg Med Chem. 2007 Mar 1;15(5):2187-97. Epub 2006 Dec 12.Inhibition of FLT3 and PDGFR tyrosine kinase activity by bis(benzo[b]furan-2-yl)methanones.
Ref 529891J Med Chem. 2009 Jan 22;52(2):278-92.Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors.
Ref 530708MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33.
Ref 530858Bioorg Med Chem. 2010 May 15;18(10):3575-87. Epub 2010 Mar 27.Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.
Ref 531635Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36.
Ref 531959The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85.
Ref 532104Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients. Br J Pharmacol. 2013 Apr;168(7):1687-706.
Ref 532187Anti-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 533862J Med Chem. 1994 Jul 8;37(14):2129-37.A new series of PDGF receptor tyrosine kinase inhibitors: 3-substituted quinoline derivatives.
Ref 533872J 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 534808J Med Chem. 1998 Dec 31;41(27):5457-65.Structure-activity relationships for 1-phenylbenzimidazoles as selective ATP site inhibitors of the platelet-derived growth factor receptor.
Ref 543492(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. (Target id: 1804).
Ref 550402National Cancer Institute Drug Dictionary (drug id 452042).
Ref 551331A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation, Bioorg. Med. Chem. Lett. 7(23):2935-2940 (1997).
Ref 551338The 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 553086Biochemical 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.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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