Target General Infomation
Target ID
T80975 (Former ID: TTDS00008)
Target Name
Vascular endothelial growth factor receptor 2 (KDR)
Synonyms
VEGFR2; VEGFR-2; VEGF-2 receptor; Protein-tyrosine kinase receptor flk-1; Kinase insert domain receptor; Fetal liver kinase 1; FLK1; FLK-1; CD309
Gene Name
KDR
Target Type
Successful target
[1]
Disease [+] 8 Target-related Diseases +
1 Breast cancer [ICD-11: 2C60-2C6Y]
2 Colorectal cancer [ICD-11: 2B91]
3 Malignant digestive organ neoplasm [ICD-11: 2C11]
4 Renal cell carcinoma [ICD-11: 2C90]
5 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
6 Stomach cancer [ICD-11: 2B72]
7 Thrombocytopenia [ICD-11: 3B64]
8 Thyroid cancer [ICD-11: 2D10]
Function
Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and embryonic hematopoiesis. Promotes proliferation, survival, migration and differentiation of endothelial cells. Promotes reorganization of the actin cytoskeleton. Isoforms lacking a transmembrane domain, such as isoform 2 and isoform 3, may function as decoy receptors for VEGFA, VEGFC and/or VEGFD. Isoform 2 plays an important role as negative regulator of VEGFA- and VEGFC-mediated lymphangiogenesis by limiting the amount of free VEGFA and/or VEGFC and preventing their binding to FLT4. Modulates FLT1 and FLT4 signaling by forming heterodimers. Binding of vascular growth factors to isoform 1 leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate and the activation of protein kinase C. Mediates activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Mediates phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, reorganization of the actin cytoskeleton and activation of PTK2/FAK1. Required for VEGFA-mediated induction of NOS2 and NOS3, leading to the production of the signaling molecule nitric oxide (NO) by endothelial cells. Phosphorylates PLCG1. Promotes phosphorylation of FYN, NCK1, NOS3, PIK3R1, PTK2/FAK1 and SRC. Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD.
BioChemical Class
Kinase
UniProt ID
VGFR2_HUMAN
EC Number
EC 2.7.10.1
Sequence
MQSKVLLAVALWLCVETRAASVGLPSVSLDLPRLSIQKDILTIKANTTLQITCRGQRDLD
WLWPNNQSGSEQRVEVTECSDGLFCKTLTIPKVIGNDTGAYKCFYRETDLASVIYVYVQD
YRSPFIASVSDQHGVVYITENKNKTVVIPCLGSISNLNVSLCARYPEKRFVPDGNRISWD
SKKGFTIPSYMISYAGMVFCEAKINDESYQSIMYIVVVVGYRIYDVVLSPSHGIELSVGE
KLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRS
DQGLYTCAASSGLMTKKNSTFVRVHEKPFVAFGSGMESLVEATVGERVRIPAKYLGYPPP
EIKWYKNGIPLESNHTIKAGHVLTIMEVSERDTGNYTVILTNPISKEKQSHVVSLVVYVP
PQIGEKSLISPVDSYQYGTTQTLTCTVYAIPPPHHIHWYWQLEEECANEPSQAVSVTNPY
PCEEWRSVEDFQGGNKIEVNKNQFALIEGKNKTVSTLVIQAANVSALYKCEAVNKVGRGE
RVISFHVTRGPEITLQPDMQPTEQESVSLWCTADRSTFENLTWYKLGPQPLPIHVGELPT
PVCKNLDTLWKLNATMFSNSTNDILIMELKNASLQDQGDYVCLAQDRKTKKRHCVVRQLT
VLERVAPTITGNLENQTTSIGESIEVSCTASGNPPPQIMWFKDNETLVEDSGIVLKDGNR
NLTIRRVRKEDEGLYTCQACSVLGCAKVEAFFIIEGAQEKTNLEIIILVGTAVIAMFFWL
LLVIILRTVKRANGGELKTGYLSIVMDPDELPLDEHCERLPYDASKWEFPRDRLKLGKPL
GRGAFGQVIEADAFGIDKTATCRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVN
LLGACTKPGGPLMVIVEFCKFGNLSTYLRSKRNEFVPYKTKGARFRQGKDYVGAIPVDLK
RRLDSITSSQSSASSGFVEEKSLSDVEEEEAPEDLYKDFLTLEHLICYSFQVAKGMEFLA
SRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDARLPLKWMAPETIFDR
VYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTML
DCWHGEPSQRPTFSELVEHLGNLLQANAQQDGKDYIVLPISETLSMEEDSGLSLPTSPVS
CMEEEEVCDPKFHYDNTAGISQYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDNQTDS
GMVLASEELKTLEDRTKLSPSFGGMVPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYS
SEEAELLKLIEIGVQTGSTAQILQPDSGTTLSSPPV
Drugs and Modes of Action
Approved Drug(s) [+] 11 Approved Drugs +
1 Axitinib Drug Info Approved Renal cell carcinoma [2], [3], [4]
2 Cabozantinib Drug Info Approved Thyroid cancer [5], [6]
3 Lenvatinib Drug Info Approved Thyroid cancer [7]
4 Pazopanib HCl Drug Info Approved Renal cell carcinoma [8]
5 Ramucirumab Drug Info Approved Gastric adenocarcinoma [9], [10]
6 Regorafenib Drug Info Approved Metastatic colorectal cancer [11], [3]
7 Romiplostim Drug Info Approved Thrombocytopenia [12], [13]
8 Sorafenib Drug Info Approved Renal cell carcinoma [14], [15]
9 Sunitinib Drug Info Approved Gastrointestinal cancer [16], [17], [18]
10 Vandetanib Drug Info Approved Solid tumour/cancer [19], [20]
11 YN-968D1 Drug Info Approved Breast cancer [21], [22], [23]
Clinical Trial Drug(s) [+] 33 Clinical Trial Drugs +
1 Brivanib Drug Info Phase 3 Liver cancer [24], [25]
2 Cediranib Drug Info Phase 3 Peritoneal cavity cancer [26], [27]
3 E-3810 Drug Info Phase 3 Solid tumour/cancer [28], [29]
4 Fruquintinib Drug Info Phase 3 Solid tumour/cancer [30]
5 HKI-272 Drug Info Phase 3 Breast cancer [31], [32]
6 Rivoceranib Drug Info Phase 3 Gastric adenocarcinoma [32]
7 Rosiglitazone + metformin Drug Info Phase 3 Diabetic complication [33]
8 Tivozanib Drug Info Phase 3 Renal cell carcinoma [34], [35]
9 Alacizumab pegol Drug Info Phase 2 Non-small-cell lung cancer [36]
10 BAY-57-9352 Drug Info Phase 2 Solid tumour/cancer [37]
11 BMS-690514 Drug Info Phase 2 Chronic pain [38]
12 CP-547632 Drug Info Phase 2 Solid tumour/cancer [39], [40]
13 Delphinidin Drug Info Phase 2 Cardiovascular disease [41]
14 Famitinib Drug Info Phase 2 Solid tumour/cancer [42], [43]
15 RAF265 Drug Info Phase 2 Melanoma [44], [45]
16 VATALANIB Drug Info Phase 2 Solid tumour/cancer [46], [47]
17 XL880 Drug Info Phase 2 Squamous head and neck cell carcinom [48], [49]
18 Anti-VEGFR2 CD8 cell therapy Drug Info Phase 1/2 Solid tumour/cancer [50]
19 Elpamotide Drug Info Phase 1/2 Biliary cancer [51]
20 MK-2461 Drug Info Phase 1/2 Alzheimer disease [52]
21 OTSGC-A24 Drug Info Phase 1/2 Colorectal cancer [53]
22 Altiratinib Drug Info Phase 1 Solid tumour/cancer [54]
23 CEP-11981 Drug Info Phase 1 Solid tumour/cancer [55], [56]
24 CYC116 Drug Info Phase 1 Solid tumour/cancer [57]
25 E-7050 Drug Info Phase 1 Head and neck cancer [58], [59]
26 KRN633 Drug Info Phase 1 Solid tumour/cancer [60], [61]
27 OSI-930 Drug Info Phase 1 Solid tumour/cancer [62], [63]
28 Pegdinetanib Drug Info Phase 1 Non-small-cell lung cancer [64]
29 PF-00337210 Drug Info Phase 1 Solid tumour/cancer [65]
30 PLX-4720 Drug Info Phase 1 Cutaneous melanoma [66]
31 Sulfatinib Drug Info Phase 1 Solid tumour/cancer [67]
32 TAK-593 Drug Info Phase 1 Solid tumour/cancer [68]
33 XL999 Drug Info Phase 1 Advanced malignancy [18]
Patented Agent(s) [+] 1 Patented Agents +
1 Antibodie derivative 10 Drug Info Patented Neoplasm [69], [70]
Discontinued Drug(s) [+] 4 Discontinued Drugs +
1 Motesanib Drug Info Discontinued in Phase 3 Non-small-cell lung cancer [71], [72]
2 SU-14813 Drug Info Discontinued in Phase 2 Breast cancer [73], [74]
3 IMC-1C11 Drug Info Discontinued in Phase 1 Solid tumour/cancer [75]
4 CEP-5214 Drug Info Terminated Solid tumour/cancer [76]
Mode of Action [+] 4 Modes of Action +
Modulator [+] 17 Modulator drugs +
1 Axitinib Drug Info [3], [4]
2 Ramucirumab Drug Info [10]
3 Regorafenib Drug Info [78]
4 Sorafenib Drug Info [15], [80]
5 Sunitinib Drug Info [17], [81]
6 Brivanib Drug Info [85]
7 Tivozanib Drug Info [90]
8 Delphinidin Drug Info [41]
9 RAF265 Drug Info [94]
10 XL880 Drug Info [85]
11 Anti-VEGFR2 CD8 cell therapy Drug Info [50], [95]
12 E-7050 Drug Info [100]
13 OSI-930 Drug Info [62], [63]
14 Pegdinetanib Drug Info [101]
15 PF-00337210 Drug Info [102]
16 TAK-593 Drug Info [68], [104]
17 EPI-0030 Drug Info [101]
Inhibitor [+] 104 Inhibitor drugs +
1 Cabozantinib Drug Info [6], [77]
2 Lenvatinib Drug Info [1]
3 Pazopanib HCl Drug Info [8]
4 Romiplostim Drug Info [79]
5 Vandetanib Drug Info [82], [83]
6 YN-968D1 Drug Info [84]
7 Cediranib Drug Info [82], [83]
8 E-3810 Drug Info [86]
9 Fruquintinib Drug Info [87]
10 HKI-272 Drug Info [88]
11 Rosiglitazone + metformin Drug Info [82], [89]
12 BAY-57-9352 Drug Info [82]
13 BMS-690514 Drug Info [92]
14 CP-547632 Drug Info [82], [93]
15 Famitinib Drug Info [43]
16 VATALANIB Drug Info [88]
17 MK-2461 Drug Info [52]
18 CEP-11981 Drug Info [82]
19 CYC116 Drug Info [99]
20 KRN633 Drug Info [82]
21 PLX-4720 Drug Info [81]
22 Sulfatinib Drug Info [103]
23 XL999 Drug Info [105]
24 Pyridine derivative 18 Drug Info [106]
25 Pyrimidine derivative 12 Drug Info [69]
26 Pyrimidine derivative 13 Drug Info [69]
27 Pyrimidine derivative 14 Drug Info [69]
28 Pyrimidine derivative 4 Drug Info [69]
29 Quinazoline derivative 15 Drug Info [106]
30 Quinazoline derivative 16 Drug Info [106]
31 Quinoline and quinazoline derivative 1 Drug Info [69]
32 Motesanib Drug Info [107], [108], [109]
33 SU-14813 Drug Info [82], [110], [111]
34 AG1295 Drug Info [113]
35 (2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine Drug Info [115]
36 (3-Phenoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine Drug Info [115]
37 (4-Phenoxy-phenyl)-quinazolin-4-yl-amine Drug Info [116]
38 (5-Phenyl-oxazol-2-yl)-m-tolyl-amine Drug Info [115]
39 2-(1H-indazol-3-yl)-1H-benzo[d]imidazole Drug Info [117]
40 2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Drug Info [115]
41 2-(p-toluidino)-4-phenylpyrimidine-5-carbonitrile Drug Info [118]
42 2-(pyrimidin-4-ylamino)thiazole-5-carbonitrile Drug Info [119]
43 3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Drug Info [120]
44 3,4-diphenyl-1H-pyrrole-2,5-dione Drug Info [120]
45 3,6-Di-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine Drug Info [121]
46 3-((3-bromothiophen-2-yl)methylene)indolin-2-one Drug Info [122]
47 3-(1H-Indol-2-yl)-1H-quinolin-2-one Drug Info [123]
48 3-(4-aminophenyl)thieno[3,2-c]pyridin-4-amine Drug Info [124]
49 3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Drug Info [120]
50 3-(5-Phenyl-oxazol-2-ylamino)-benzonitrile Drug Info [115]
51 3-(5-Thiophen-3-yl-pyridin-3-yl)-1H-indole Drug Info [125]
52 3-Benzimidazol-2-ylhydroquinolin-2-one Drug Info [126]
53 3-methyl-1H-thieno[2,3-c]pyrazole-5-carboxamide Drug Info [127]
54 3-phenyl-1,4-dihydroindeno[1,2-c]pyrazole Drug Info [128]
55 4-(4-aminophenyl)-1H-indazol-3yl-amine Drug Info [129]
56 4-(4-m-Tolylamino-phthalazin-1-yl)-benzamide Drug Info [130]
57 4-(4-p-Tolylamino-phthalazin-1-yl)-benzamide Drug Info [130]
58 4-(5-Phenyl-oxazol-2-ylamino)-benzenesulfonamide Drug Info [115]
59 4-(isoquinolin-5-yl)-N-m-tolylphthalazin-1-amine Drug Info [131]
60 4-(isoquinolin-5-yl)-N-o-tolylphthalazin-1-amine Drug Info [131]
61 4-Chloro-N-(2-chloro-benzoyl)-benzenesulfonamide Drug Info [132]
62 4-Chloro-N-(2-methyl-benzoyl)-benzenesulfonamide Drug Info [132]
63 4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide Drug Info [132]
64 4-Chloro-N-(4-chloro-benzoyl)-benzenesulfonamide Drug Info [132]
65 4-Chloro-N-(4-nitro-benzoyl)-benzenesulfonamide Drug Info [132]
66 4-phenyl-2-(phenylamino)pyrimidine-5-carbonitrile Drug Info [118]
67 4-[3-Hydroxyanilino]-6,7-Dimethoxyquinazoline Drug Info [122]
68 5-(4-Methoxy-phenyl)-1-phenyl-1H-benzoimidazole Drug Info [133]
69 6-(1H-Benzoimidazol-2-yl)-benzocyclohepten-7-one Drug Info [123]
70 6-o-tolylquinazolin-2-amine Drug Info [134]
71 8-methyl-4H,7H-indolo[6,5,4-cd]indol-5-one Drug Info [122]
72 AAL-993 Drug Info [79]
73 AG-E-85378 Drug Info [135]
74 AMG-429 Drug Info [101]
75 AST-487 Drug Info [136]
76 BIBF-1202 Drug Info [137]
77 BMS-536924 Drug Info [138]
78 BMS-645737 Drug Info [139]
79 BX-795 Drug Info [140]
80 BX-912 Drug Info [140]
81 CB-676475 Drug Info [141]
82 CEP-5104 Drug Info [142]
83 IM-023911 Drug Info [130]
84 IM-094261 Drug Info [130]
85 IM-094882 Drug Info [131]
86 Indolin-2-one deriv. 4b Drug Info [143]
87 Isoindolinone Urea derivative Drug Info [144]
88 JNJ-38158471 Drug Info [101]
89 K-252a analogue Drug Info [145]
90 Ki-20227 Drug Info [146]
91 L000021649 Drug Info [121]
92 MG-516 Drug Info [101]
93 N-(2,4-Dichloro-benzoyl)-benzenesulfonamide Drug Info [132]
94 N-(3-Bromo-benzoyl)-4-chloro-benzenesulfonamide Drug Info [132]
95 Phenyl-(5-phenyl-oxazol-2-yl)-amine Drug Info [115]
96 PMID22765894C8h Drug Info [147]
97 PMID23639540C13a Drug Info [148]
98 PP121 Drug Info [149]
99 Pyrazolo[1,5-a]pyrimidine 3G Drug Info [121]
100 Ro-4396686 Drug Info [150]
101 SU-11652 Drug Info [151]
102 TG-100435 Drug Info [152]
103 VEGF receptor 2 kinase inhibitor I Drug Info [153]
104 [3-(5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol Drug Info [115]
Antagonist [+] 3 Antagonist drugs +
1 Altiratinib Drug Info [98]
2 Rivoceranib Drug Info [32]
3 CEP-5214 Drug Info [114]
Binder [+] 1 Binder drugs +
1 Antibodie derivative 6 Drug Info [69]
Target Regulators
Target-regulating microRNAs
Target-interacting Proteins
Target Profiles in Patients
Target Expression
 Profile (TEP)
Target Affiliated Biological Pathways
KEGG Pathway [+] 8 KEGG Pathways +
1 Ras signaling pathway
2 Rap1 signaling pathway
3 Cytokine-cytokine receptor interaction
4 Endocytosis
5 PI3K-Akt signaling pathway
6 VEGF signaling pathway
7 Focal adhesion
8 Proteoglycans in cancer
NetPath Pathway [+] 1 NetPath Pathways +
1 IL2 Signaling Pathway
Panther Pathway [+] 2 Panther Pathways +
1 Angiogenesis
2 VEGF signaling pathway
PID Pathway [+] 9 PID Pathways +
1 HIF-2-alpha transcription factor network
2 Beta3 integrin cell surface interactions
3 Signaling events mediated by TCPTP
4 SHP2 signaling
5 S1P1 pathway
6 VEGF and VEGFR signaling network
7 Integrins in angiogenesis
8 Signaling events mediated by VEGFR1 and VEGFR2
9 Notch-mediated HES/HEY network
Reactome [+] 6 Reactome Pathways +
1 Neurophilin interactions with VEGF and VEGFR
2 VEGF binds to VEGFR leading to receptor dimerization
3 Integrin cell surface interactions
4 EPHA-mediated growth cone collapse
5 VEGFA-VEGFR2 Pathway
6 VEGFR2 mediated cell proliferation
WikiPathways [+] 5 WikiPathways +
1 Focal Adhesion
2 Nifedipine Activity
3 Cardiac Progenitor Differentiation
4 Signaling by VEGF
5 Angiogenesis
Target-Related Models and Studies
Target Validation
Target QSAR Model
References
REF 1 Emerging drugs for ovarian cancer. Expert Opin Emerg Drugs. 2008 Sep;13(3):523-36.
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: 5659).
REF 3 Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
REF 4 Axitinib: VEGF inhibition in advanced thyroid cancer. Lancet Oncol. 2014 Jul;15(8):e310.
REF 5 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: 5887).
REF 6 Clinical pipeline report, company report or official report of Exelixis (2011).
REF 7 FDA Approved Drug Products from FDA Official Website. 2018. Application Number: (ANDA) 208627.
REF 8 Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
REF 9 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: 7390).
REF 10 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
REF 11 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: 5891).
REF 12 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: 6974).
REF 13 2008 FDA drug approvals. Nat Rev Drug Discov. 2009 Feb;8(2):93-6.
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: 5711).
REF 15 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 16 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: 5713).
REF 17 2006 drug approvals: finding the niche. Nat Rev Drug Discov. 2007 Feb;6(2):99-101.
REF 18 Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
REF 19 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: 5717).
REF 20 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4.
REF 21 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: 7648).
REF 22 Clinical pipeline report, company report or official report of LSK BioPharma.
REF 23 ClinicalTrials.gov (NCT02426034) Study of Apatinib Tablets in the Treatment of Advanced or Metastatic Gastric Cancer. U.S. National Institutes of Health.
REF 24 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: 5671).
REF 25 ClinicalTrials.gov (NCT01108705) Comparison of Brivanib and Best Supportive Care (BSC) With Placebo and BSC for Treatment of Liver Cancer in Asian Patients Who Have Failed Sorafenib Treatment. U.S. National Institutes of Health.
REF 26 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: 5664).
REF 27 ClinicalTrials.gov (NCT02446600) Olaparib or Cediranib Maleate and Olaparib Compared With Standard Platinum-Based Chemotherapy in Treating Patients With Recurrent Platinum-Sensitive Ovarian, Fallopian Tube, or Primary Peritoneal Cancer. U.S. National Institutes of Health.
REF 28 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: 7649).
REF 29 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 30 ClinicalTrials.gov (NCT02314819) A Phase III Trial Evaluating Fruquintinib Efficacy and Safety in 3+ Line Colorectal Cancer Patients RESCO). U.S. National Institutes of Health.
REF 31 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021154)
REF 32 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
REF 33 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 34 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: 6058).
REF 35 ClinicalTrials.gov (NCT01076010) An Extension Treatment Protocol for Subjects Who Have Participated in a Phase 3 Study of Tivozanib Versus Sorafenib in Renal Cell Carcinoma (Protocol AV-951-09-301). U.S. National Institutes of Health.
REF 36 ClinicalTrials.gov (NCT00152477) A Study of Paclitaxel/Carboplatin With or Without CDP791 in Patients With Lung Cancer. U.S. National Institutes of Health.
REF 37 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 38 A novel epidermal growth factor receptor inhibitor promotes apoptosis in non-small cell lung cancer cells resistant to erlotinib. Cancer Res. 2007 Jul 1;67(13):6253-62.
REF 39 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: 7881).
REF 40 ClinicalTrials.gov (NCT00096239) CP-547,632 in Treating Patients With Recurrent or Persistent Ovarian Cancer, Primary Peritoneal Cancer, or Fallopian Tube Cancer. U.S. National Institutes of Health.
REF 41 Delphinidin, a dietary anthocyanidin, inhibits vascular endothelial growth factor receptor-2 phosphorylation. Carcinogenesis. 2006 May;27(5):989-96.
REF 42 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: 7886).
REF 43 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 44 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: 5674).
REF 45 ClinicalTrials.gov (NCT00304525) A Study to Evaluate RAF265, an Oral Drug Administered to Subjects With Locally Advanced or Metastatic Melanoma. U.S. National Institutes of Health.
REF 46 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: 5705).
REF 47 ClinicalTrials.gov (NCT00348790) Vatalanib in Treating Patients With Recurrent or Progressive Meningioma. U.S. National Institutes of Health.
REF 48 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: 5679).
REF 49 Clinical pipeline report, company report or official report of Exelixis (2011).
REF 50 ClinicalTrials.gov (NCT01218867) CAR T Cell Receptor Immunotherapy Targeting VEGFR2 for Patients With Metastatic Cancer. U.S. National Institutes of Health.
REF 51 ClinicalTrials.gov (NCT00655785) Antiangiogenic Peptide Vaccine Therapy With Gemcitabine in Treating Patient With Pancreatic Cancer (Phase1/2). U.S. National Institutes of Health.
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