Target Information
Target General Infomation | |||||
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Target ID |
T80975
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Former ID |
TTDS00008
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Target Name |
Vascular endothelial growth factor receptor 2
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Gene Name |
KDR
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Synonyms |
VEGFR-2; VEGFR2; Fetal liver kinase 1; FLK-1; Kinase insert domain receptor; Protein-tyrosine kinase receptor flk-1; CD309; FLK1; VEGF-2 receptor; KDR
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Target Type |
Successful
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Disease | Cutaneous Melanoma [ICD10: C43-C44] | ||||
Angiogenesis disorder [ICD10: I00-I99] | |||||
Alzheimer disease [ICD9: 331; ICD10: G30] | |||||
Advanced renal cell carcinoma [ICD9: 189; ICD10: C64] | |||||
Advanced solid tumor [ICD9: 140-199; ICD10: C00-C75, C7A, C7B] | |||||
Advanced malignancies [ICD9: 140-229; ICD10: C00-C96] | |||||
Breast cancer [ICD9: 174, 175; ICD10: C50] | |||||
Breast cancer; Liver cancer [ICD9:174, 175, 140-229, 155, 203.0; ICD10: C50, C22] | |||||
Biliary cancer [ICD10: C22, C24] | |||||
Chronic pain [ICD9: 338.2,780; ICD10: R52.1-R52.2, G89] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Colorectal cancer [ICD9: 153, 154; ICD10: C18-C21] | |||||
Cardiovascular disorder [ICD10: I00-I99] | |||||
Fallopian tube cancer; Ovarian cancer; Peritoneal cavity cancer [ICD9: 140-229, 158, 183, 183.2, 221.0; ICD10: C48.1, C48.2, C56, C57, D28] | |||||
Gastric cancer [ICD9: 151; ICD10: C16] | |||||
Gastric cancer; Renal cell carcinoma; Squamous cell cancer of head and neck [ICD9: 140-229, 151, 189; ICD10: C16, C64] | |||||
Gastrointestinal cancers; Advanced renal cell carcinoma [ICD9:150-159, 189; ICD10: C15-C26, C64] | |||||
Glioma; Solid tumours [ICD9: 140-199, 191; ICD10: C00-C75, C71, C7A, C7B] | |||||
Head and neck cancer [ICD9: 140-149, 140-229; ICD10: C07-C14, C32-C33] | |||||
Hepatocellular carcinoma; NSCLC; Melanoma [ICD9: 155, 162, 172; ICD10: C22.0, C33, C34, C43] | |||||
Metastatic breast cancer [ICD10: C50] | |||||
Melanoma [ICD9: 172; ICD10: 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] | |||||
Metastatic colorectal cancer [ICD9: 153, 154; ICD10: C18-C21] | |||||
Medullary thyroid cancer [ICD9: 193; ICD10: C73] | |||||
Metastatic castration-resistant prostate cancer; Ovarian cancer [ICD9: 140-229, 183, 185; ICD10: C56, C61] | |||||
Non-small cell lung cancer [ICD10: C33-C34] | |||||
Non-small-cell lung cancer; Ovarian cancer; Solid tumours [ICD9: 140-199, 140-229, 162, 183, 210-229; ICD10: C33-C34, C56, D10-D36, D3A] | |||||
Ovarian cancer [ICD9: 183; ICD10: C56] | |||||
Renal cancer [ICD9: 140-229, 189; ICD10: C64] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Thyroid cancer; Renal cell carcinoma [ICD9: 140-229, 189, 193; ICD10: C64, C73] | |||||
Function |
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. 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.
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BioChemical Class |
Kinase
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Target Validation |
T80975
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UniProt ID | |||||
EC Number |
EC 2.7.10.1
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Sequence |
MQSKVLLAVALWLCVETRAASVGLPSVSLDLPRLSIQKDILTIKANTTLQITCRGQRDLD
WLWPNNQSGSEQRVEVTECSDGLFCKTLTIPKVIGNDTGAYKCFYRETDLASVIYVYVQD YRSPFIASVSDQHGVVYITENKNKTVVIPCLGSISNLNVSLCARYPEKRFVPDGNRISWD SKKGFTIPSYMISYAGMVFCEAKINDESYQSIMYIVVVVGYRIYDVVLSPSHGIELSVGE KLVLNCTARTELNVGIDFNWEYPSSKHQHKKLVNRDLKTQSGSEMKKFLSTLTIDGVTRS DQGLYTCAASSGLMTKKNSTFVRVHEKPFVAFGSGMESLVEATVGERVRIPAKYLGYPPP EIKWYKNGIPLESNHTIKAGHVLTIMEVSERDTGNYTVILTNPISKEKQSHVVSLVVYVP PQIGEKSLISPVDSYQYGTTQTLTCTVYAIPPPHHIHWYWQLEEECANEPSQAVSVTNPY PCEEWRSVEDFQGGNKIEVNKNQFALIEGKNKTVSTLVIQAANVSALYKCEAVNKVGRGE RVISFHVTRGPEITLQPDMQPTEQESVSLWCTADRSTFENLTWYKLGPQPLPIHVGELPT PVCKNLDTLWKLNATMFSNSTNDILIMELKNASLQDQGDYVCLAQDRKTKKRHCVVRQLT VLERVAPTITGNLENQTTSIGESIEVSCTASGNPPPQIMWFKDNETLVEDSGIVLKDGNR NLTIRRVRKEDEGLYTCQACSVLGCAKVEAFFIIEGAQEKTNLEIIILVGTAVIAMFFWL LLVIILRTVKRANGGELKTGYLSIVMDPDELPLDEHCERLPYDASKWEFPRDRLKLGKPL GRGAFGQVIEADAFGIDKTATCRTVAVKMLKEGATHSEHRALMSELKILIHIGHHLNVVN LLGACTKPGGPLMVIVEFCKFGNLSTYLRSKRNEFVPYKTKGARFRQGKDYVGAIPVDLK RRLDSITSSQSSASSGFVEEKSLSDVEEEEAPEDLYKDFLTLEHLICYSFQVAKGMEFLA SRKCIHRDLAARNILLSEKNVVKICDFGLARDIYKDPDYVRKGDARLPLKWMAPETIFDR VYTIQSDVWSFGVLLWEIFSLGASPYPGVKIDEEFCRRLKEGTRMRAPDYTTPEMYQTML DCWHGEPSQRPTFSELVEHLGNLLQANAQQDGKDYIVLPISETLSMEEDSGLSLPTSPVS CMEEEEVCDPKFHYDNTAGISQYLQNSKRKSRPVSVKTFEDIPLEEPEVKVIPDDNQTDS GMVLASEELKTLEDRTKLSPSFGGMVPSKSRESVASEGSNQTSGYQSGYHSDDTDTTVYS SEEAELLKLIEIGVQTGSTAQILQPDSGTTLSSPPV |
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Structure |
1VR2; 1Y6A; 1Y6B; 1YWN; 2M59; 2MET; 2MEU; 2OH4; 2P2H; 2P2I; 2QU5; 2QU6; 2RL5; 2X1W; 2X1X; 2XIR; 3B8Q; 3B8R; 3BE2; 3C7Q; 3CJF; 3CJG; 3CP9; 3CPB; 3CPC; 3DTW; 3EFL; 3EWH; 3KVQ; 3S35; 3S36; 3S37; 3U6J; 3V2A; 3V6B; 3VHE; 3VHK; 3VID; 3VNT; 3VO3; 4AG8; 4AGC; 4AGD; 4ASD; 4ASE; 1VR2; 1Y6A; 1Y6B; 1YWN; 2M59; 2MET; 2MEU; 2OH4; 2P2H; 2P2I; 2QU5; 2QU6; 2RL5; 2X1W; 2X1X; 2XIR; 3B8Q; 3B8R; 3BE2; 3C7Q; 3CJF; 3CJG; 3CP9; 3CPB; 3CPC; 3DTW; 3EFL; 3EWH; 3KVQ; 3S35; 3S36;3S37; 3U6J; 3V2A; 3V6B; 3VHE; 3VHK; 3VID; 3VNT; 3VO3; 4AG8; 4AGC; 4AGD; 4ASD; 4ASE
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Drugs and Mode of Action | |||||
Drug(s) | Axitinib | Drug Info | Approved | Advanced renal cell carcinoma | [532210], [532919], [541003] |
Cabozantinib | Drug Info | Approved | Medullary thyroid cancer | [541185], [550636] | |
Pazopanib HCl | Drug Info | Approved | Renal cancer | [530677] | |
Ramucirumab | Drug Info | Approved | Gastric cancer | [533123], [542411] | |
Regorafenib | Drug Info | Approved | Metastatic colorectal cancer | [532210], [541189] | |
Sorafenib | Drug Info | Approved | Advanced renal cell carcinoma | [528230], [541050] | |
Sunitinib | Drug Info | Approved | Gastrointestinal cancers; Advanced renal cell carcinoma | [528715], [537114], [541052] | |
Vandetanib | Drug Info | Approved | Solid tumours | [531783], [541055] | |
YN-968D1 | Drug Info | Approved | Breast cancer | [525168], [542631], [549965] | |
Brivanib | Drug Info | Phase 3 | Breast cancer; Liver cancer | [523016], [541015] | |
Cediranib | Drug Info | Phase 3 | Fallopian tube cancer; Ovarian cancer; Peritoneal cavity cancer | [525194], [541007] | |
E-3810 | Drug Info | Phase 3 | Solid tumours | [524749], [542632] | |
Fruquintinib | Drug Info | Phase 3 | Cancer | [525024] | |
HKI-272 | Drug Info | Phase 3 | Breast cancer | [548009] | |
Sorafenib | Drug Info | Phase 3 | Hepatocellular carcinoma; NSCLC; Melanoma | [537114], [541050] | |
Tivozanib | Drug Info | Phase 3 | Renal cancer | [522960], [541307] | |
Alacizumab pegol | Drug Info | Phase 2 | Non-small cell lung cancer | [521677] | |
BAY-57-9352 | Drug Info | Phase 2 | Solid tumours | [548058] | |
BMS-690514 | Drug Info | Phase 2 | Chronic pain | [528940] | |
Cabozantinib | Drug Info | Phase 2 | Metastatic castration-resistant prostate cancer; Ovarian cancer | [541185], [550636] | |
CP-547632 | Drug Info | Phase 2 | Non-small-cell lung cancer; Ovarian cancer; Solid tumours | [521618], [542806] | |
Delphinidin | Drug Info | Phase 2 | Cardiovascular disorder | [527896] | |
Famitinib | Drug Info | Phase 2 | Cancer | [532104], [542811] | |
RAF265 | Drug Info | Phase 2 | Melanoma | [521813], [541017] | |
Sorafenib | Drug Info | Phase 2 | Myelodysplastic syndrome; AML; Head and neck cancer; Breast cancer; Pancreatic cancer | [537114], [541050] | |
VATALANIB | Drug Info | Phase 2 | Solid tumours | [521851], [541046] | |
XL880 | Drug Info | Phase 2 | Gastric cancer; Renal cell carcinoma; Squamous cell cancer of head and neck | [541022], [550637] | |
Anti-VEGFR2 CD8 cell therapy | Drug Info | Phase 1/2 | Cancer | [523207] | |
Elpamotide | Drug Info | Phase 1/2 | Biliary cancer | [522286] | |
MK-2461 | Drug Info | Phase 1/2 | Alzheimer disease | [530708] | |
OTSGC-A24 | Drug Info | Phase 1/2 | Colorectal cancer | [523227] | |
Cabozantinib | Drug Info | Phase 1b | Thyroid cancer; Renal cell carcinoma | [541185], [550636] | |
Altiratinib | Drug Info | Phase 1 | Solid tumours | [549538] | |
CEP-11981 | Drug Info | Phase 1 | Solid tumours | [522626], [542989] | |
CYC116 | Drug Info | Phase 1 | Solid tumours | [522163] | |
E 7080 | Drug Info | Phase 1 | Ovarian cancer | [536839] | |
E-7050 | Drug Info | Phase 1 | Head and neck cancer | [525301], [542872] | |
KRN633 | Drug Info | Phase 1 | Glioma; Solid tumours | [541306], [547568] | |
OSI-930 | Drug Info | Phase 1 | Solid tumours | [531624], [531955] | |
Pegdinetanib | Drug Info | Phase 1 | Non-small cell lung cancer | [523078] | |
PF-00337210 | Drug Info | Phase 1 | Solid tumours | [523008] | |
SU-6668 | Drug Info | Phase 1 | Advanced solid tumor | [527156], [542760] | |
Sulfatinib | Drug Info | Phase 1 | Cancer | [524745] | |
TAK-593 | Drug Info | Phase 1 | Cancer | [532187] | |
XL880 | Drug Info | Phase 1 | Solid tumours | [541022], [550637] | |
XL999 | Drug Info | Phase 1 | Advanced malignancies | [537114] | |
Motesanib | Drug Info | Discontinued in Phase 3 | Non-small cell lung cancer | [541005], [546905] | |
SU-14813 | Drug Info | Discontinued in Phase 2 | Metastatic breast cancer | [541051], [548093] | |
IMC-1C11 | Drug Info | Discontinued in Phase 1 | Cancer | [547109] | |
AG1295 | Drug Info | Terminated | Discovery agent | [541205], [546396] | |
CEP-5214 | Drug Info | Terminated | Solid tumours | [547462] | |
Inhibitor | (2-Methoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine | Drug Info | [527458] | ||
(3-Phenoxy-phenyl)-(5-phenyl-oxazol-2-yl)-amine | Drug Info | [527458] | |||
(4-Phenoxy-phenyl)-quinazolin-4-yl-amine | Drug Info | [525876] | |||
(5-Phenyl-oxazol-2-yl)-m-tolyl-amine | Drug Info | [527458] | |||
2-(1H-indazol-3-yl)-1H-benzo[d]imidazole | Drug Info | [528122] | |||
2-(5-Phenyl-oxazol-2-ylamino)-benzonitrile | Drug Info | [527458] | |||
2-(p-toluidino)-4-phenylpyrimidine-5-carbonitrile | Drug Info | [528821] | |||
2-(pyrimidin-4-ylamino)thiazole-5-carbonitrile | Drug Info | [527935] | |||
3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione | Drug Info | [528032] | |||
3,4-diphenyl-1H-pyrrole-2,5-dione | Drug Info | [528032] | |||
3,6-Di-pyridin-4-yl-pyrazolo[1,5-a]pyrimidine | Drug Info | [526462] | |||
3-((3-bromothiophen-2-yl)methylene)indolin-2-one | Drug Info | [528681] | |||
3-(1H-Indol-2-yl)-1H-quinolin-2-one | Drug Info | [526914] | |||
3-(4-aminophenyl)thieno[3,2-c]pyridin-4-amine | Drug Info | [528593] | |||
3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione | Drug Info | [528032] | |||
3-(5-Phenyl-oxazol-2-ylamino)-benzonitrile | Drug Info | [527458] | |||
3-(5-Thiophen-3-yl-pyridin-3-yl)-1H-indole | Drug Info | [526703] | |||
3-Benzimidazol-2-ylhydroquinolin-2-one | Drug Info | [529891] | |||
3-methyl-1H-thieno[2,3-c]pyrazole-5-carboxamide | Drug Info | [527793] | |||
3-phenyl-1,4-dihydroindeno[1,2-c]pyrazole | Drug Info | [528227] | |||
4-(4-aminophenyl)-1H-indazol-3yl-amine | Drug Info | [528716] | |||
4-(4-m-Tolylamino-phthalazin-1-yl)-benzamide | Drug Info | [527725] | |||
4-(4-p-Tolylamino-phthalazin-1-yl)-benzamide | Drug Info | [527725] | |||
4-(5-Phenyl-oxazol-2-ylamino)-benzenesulfonamide | Drug Info | [527458] | |||
4-(isoquinolin-5-yl)-N-m-tolylphthalazin-1-amine | Drug Info | [527948] | |||
4-(isoquinolin-5-yl)-N-o-tolylphthalazin-1-amine | Drug Info | [527948] | |||
4-Chloro-N-(2-chloro-benzoyl)-benzenesulfonamide | Drug Info | [527245] | |||
4-Chloro-N-(2-methyl-benzoyl)-benzenesulfonamide | Drug Info | [527245] | |||
4-Chloro-N-(3-chloro-benzoyl)-benzenesulfonamide | Drug Info | [527245] | |||
4-Chloro-N-(4-chloro-benzoyl)-benzenesulfonamide | Drug Info | [527245] | |||
4-Chloro-N-(4-nitro-benzoyl)-benzenesulfonamide | Drug Info | [527245] | |||
4-phenyl-2-(phenylamino)pyrimidine-5-carbonitrile | Drug Info | [528821] | |||
5-(4-Methoxy-phenyl)-1-phenyl-1H-benzoimidazole | Drug Info | [526669] | |||
6-(1H-Benzoimidazol-2-yl)-benzocyclohepten-7-one | Drug Info | [526914] | |||
6-o-tolylquinazolin-2-amine | Drug Info | [528429] | |||
8-methyl-4H,7H-indolo[6,5,4-cd]indol-5-one | Drug Info | [528681] | |||
AAL-993 | Drug Info | [526484] | |||
AG-E-85378 | Drug Info | [529047] | |||
AG1295 | Drug Info | [530377] | |||
AMG-429 | Drug Info | [543499] | |||
AST-487 | Drug Info | [528954] | |||
BAY-57-9352 | Drug Info | [536474] | |||
BIBF-1202 | Drug Info | [531679] | |||
BMS-536924 | Drug Info | [527711] | |||
BMS-645737 | Drug Info | [529409] | |||
BMS-690514 | Drug Info | [530732] | |||
BX-795 | Drug Info | [527484] | |||
BX-912 | Drug Info | [527484] | |||
Cabozantinib | Drug Info | [550636] | |||
CB-676475 | Drug Info | [527794] | |||
Cediranib | Drug Info | [536474], [550288] | |||
CEP-11981 | Drug Info | [536474] | |||
CEP-5104 | Drug Info | [529647] | |||
compound 13a | Drug Info | [532338] | |||
compound 8h | Drug Info | [531959] | |||
CP-547632 | Drug Info | [536201], [536474] | |||
CYC116 | Drug Info | [550374] | |||
E 7080 | Drug Info | [536839] | |||
E-3810 | Drug Info | [525382] | |||
Famitinib | Drug Info | [532104] | |||
Fruquintinib | Drug Info | [533061] | |||
HKI-272 | Drug Info | [528774] | |||
IM-023911 | Drug Info | [527725] | |||
IM-094261 | Drug Info | [527725] | |||
IM-094882 | Drug Info | [527948] | |||
Indolin-2-one deriv. 4b | Drug Info | [525828] | |||
Isoindolinone Urea derivative | Drug Info | [527209] | |||
JNJ-38158471 | Drug Info | [543499] | |||
K-252a analogue | Drug Info | [527569] | |||
Ki-20227 | Drug Info | [528535] | |||
KRN633 | Drug Info | [536474] | |||
L000021649 | Drug Info | [526462] | |||
MG-516 | Drug Info | [543499] | |||
MK-2461 | Drug Info | [530708] | |||
Motesanib | Drug Info | [537551], [550250], [551087] | |||
N-(2,4-Dichloro-benzoyl)-benzenesulfonamide | Drug Info | [527245] | |||
N-(3-Bromo-benzoyl)-4-chloro-benzenesulfonamide | Drug Info | [527245] | |||
Pazopanib HCl | Drug Info | [530677] | |||
Phenyl-(5-phenyl-oxazol-2-yl)-amine | Drug Info | [527458] | |||
PLX-4720 | Drug Info | [526516] | |||
PP121 | Drug Info | [529744] | |||
Pyrazolo[1,5-a]pyrimidine 3G | Drug Info | [526462] | |||
Ro-4396686 | Drug Info | [528018] | |||
SEMAXINIB | Drug Info | [526484] | |||
SU-11652 | Drug Info | [526575] | |||
SU-14813 | Drug Info | [536260], [536474], [549974] | |||
SU-6668 | Drug Info | [536137], [536474] | |||
Sulfatinib | Drug Info | [550989] | |||
TG-100435 | Drug Info | [528527] | |||
Vandetanib | Drug Info | [536474], [550288] | |||
VATALANIB | Drug Info | [528774] | |||
VEGF receptor 2 kinase inhibitor I | Drug Info | [534662] | |||
WHI-P180 | Drug Info | [528681] | |||
XL999 | Drug Info | [536402] | |||
YN-968D1 | Drug Info | [531412] | |||
[3-(5-Phenyl-oxazol-2-ylamino)-phenyl]-methanol | Drug Info | [527458] | |||
Antagonist | Altiratinib | Drug Info | [550598] | ||
CEP-5214 | Drug Info | [528142] | |||
Modulator | Anti-VEGFR2 CD8 cell therapy | Drug Info | [523207], [532072] | ||
Axitinib | Drug Info | [532210], [532919] | |||
Brivanib | Drug Info | [1572591] | |||
Delphinidin | Drug Info | [527896] | |||
E-7050 | Drug Info | [530452] | |||
EPI-0030 | Drug Info | [543499] | |||
OSI-930 | Drug Info | [531624], [531955] | |||
Pegdinetanib | Drug Info | [543499] | |||
PF-00337210 | Drug Info | [544325] | |||
RAF265 | Drug Info | [531962] | |||
Ramucirumab | Drug Info | [533123] | |||
Regorafenib | Drug Info | [551871] | |||
Sorafenib | Drug Info | [528230] | |||
Sunitinib | Drug Info | [526516], [528715] | |||
TAK-593 | Drug Info | [532187], [553086] | |||
Tivozanib | Drug Info | [550325] | |||
XL880 | Drug Info | [1572591] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Ras signaling pathway | ||||
Rap1 signaling pathway | |||||
Cytokine-cytokine receptor interaction | |||||
Endocytosis | |||||
PI3K-Akt signaling pathway | |||||
VEGF signaling pathway | |||||
Focal adhesion | |||||
Proteoglycans in cancer | |||||
NetPath Pathway | IL2 Signaling Pathway | ||||
PANTHER Pathway | Angiogenesis | ||||
VEGF signaling pathway | |||||
Pathway Interaction Database | HIF-2-alpha transcription factor network | ||||
Beta3 integrin cell surface interactions | |||||
Signaling events mediated by TCPTP | |||||
SHP2 signaling | |||||
S1P1 pathway | |||||
VEGF and VEGFR signaling network | |||||
Integrins in angiogenesis | |||||
Signaling events mediated by VEGFR1 and VEGFR2 | |||||
Notch-mediated HES/HEY network | |||||
Reactome | Neurophilin interactions with VEGF and VEGFR | ||||
VEGF binds to VEGFR leading to receptor dimerization | |||||
Integrin cell surface interactions | |||||
EPHA-mediated growth cone collapse | |||||
VEGFA-VEGFR2 Pathway | |||||
VEGFR2 mediated cell proliferation | |||||
WikiPathways | Focal Adhesion | ||||
Nifedipine Activity | |||||
Cardiac Progenitor Differentiation | |||||
Signaling by VEGF | |||||
Angiogenesis | |||||
References | |||||
Ref 521618 | 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 521677 | ClinicalTrials.gov (NCT00152477) A Study of Paclitaxel/Carboplatin With or Without CDP791 in Patients With Lung Cancer. U.S. National Institutes of Health. | ||||
Ref 521813 | 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 521851 | ClinicalTrials.gov (NCT00348790) Vatalanib in Treating Patients With Recurrent or Progressive Meningioma. U.S. National Institutes of Health. | ||||
Ref 522163 | ClinicalTrials.gov (NCT00560716) A Phase I Pharmacologic Study of CYC116, an Oral Aurora Kinase Inhibitor, in Patients With Advanced Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 522286 | ClinicalTrials.gov (NCT00655785) Antiangiogenic Peptide Vaccine Therapy With Gemcitabine in Treating Patient With Pancreatic Cancer (Phase1/2). U.S. National Institutes of Health. | ||||
Ref 522626 | ClinicalTrials.gov (NCT00875264) Open-Label Study to Determine the Maximum Tolerated Oral Dose of the Kinase Inhibitor CEP-11981 in Patients With Advanced Cancer. U.S. National Institutes of Health. | ||||
Ref 522960 | 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 523008 | ClinicalTrials.gov (NCT01105533) A Dose Finding Study Of A New Medication, PF-00337210 That Will Possibly Decrease Blood Supply To Tumors. U.S. National Institutes of Health. | ||||
Ref 523016 | 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 523078 | ClinicalTrials.gov (NCT01146171) Japanese Phase 1 Study of BMS-844203 (CT322). U.S. National Institutes of Health. | ||||
Ref 523207 | ClinicalTrials.gov (NCT01218867) CAR T Cell Receptor Immunotherapy Targeting VEGFR2 for Patients With Metastatic Cancer. U.S. National Institutes of Health. | ||||
Ref 523227 | ClinicalTrials.gov (NCT01227772) Study of OTSGC-A24 Vaccine in Advanced Gastric Cancer. U.S. National Institutes of Health. | ||||
Ref 524745 | ClinicalTrials.gov (NCT02133157) Phase I Study of Sulfatinib(HMPL-012) in Patients With Advanced Solid Tumors. 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 525024 | 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 525168 | ClinicalTrials.gov (NCT02426034) Study of Apatinib Tablets in the Treatment of Advanced or Metastatic Gastric Cancer. U.S. National Institutes of Health. | ||||
Ref 525194 | 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 525301 | ClinicalTrials.gov (NCT02533102) Pharmacokinetics and Food Effect of Single Oral Dose of E7050 in Healthy Volunteers. | ||||
Ref 527156 | A phase I surrogate endpoint study of SU6668 in patients with solid tumors. Invest New Drugs. 2004 Nov;22(4):459-66. | ||||
Ref 527896 | Delphinidin, a dietary anthocyanidin, inhibits vascular endothelial growth factor receptor-2 phosphorylation. Carcinogenesis. 2006 May;27(5):989-96. Epub 2005 Nov 23. | ||||
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 528940 | 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 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 531624 | Inhibition of c-Kit, VEGFR-2 (KDR), and ABCG2 by analogues of OSI-930. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6495-9. | ||||
Ref 531955 | OSI-930 analogues as novel reversal agents for ABCG2-mediated multidrug resistance. Biochem Pharmacol. 2012 Sep 15;84(6):766-74. | ||||
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 541003 | (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 541005 | (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 541007 | (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 541015 | (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 541017 | (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 541022 | (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 541046 | (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 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 541051 | (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: 5712). | ||||
Ref 541052 | (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 541055 | (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 541185 | (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 541189 | (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 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 541306 | (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: 6057). | ||||
Ref 541307 | (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 542411 | (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 542631 | (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 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 542760 | (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: 7816). | ||||
Ref 542806 | (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 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 542872 | (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: 7956). | ||||
Ref 542989 | (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: 8189). | ||||
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 546905 | 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 547109 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013121) | ||||
Ref 547462 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016567) | ||||
Ref 547568 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017407) | ||||
Ref 548009 | 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 548058 | 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 548093 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800021861) | ||||
Ref 523207 | ClinicalTrials.gov (NCT01218867) CAR T Cell Receptor Immunotherapy Targeting VEGFR2 for Patients With Metastatic Cancer. U.S. National Institutes of Health. | ||||
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 525828 | Identification of substituted 3-[(4,5,6, 7-tetrahydro-1H-indol-2-yl)methylene]-1,3-dihydroindol-2-ones as growth factor receptor inhibitors for VEGF-R2 (Flk-1/KDR), FGF-R1, and PDGF-Rbeta tyrosine kinases. J Med Chem. 2000 Jul 13;43(14):2655-63. | ||||
Ref 525876 | Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70.Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. | ||||
Ref 526462 | Bioorg Med Chem Lett. 2002 Dec 16;12(24):3537-41.Optimization of a pyrazolo[1,5-a]pyrimidine class of KDR kinase inhibitors: improvements in physical properties enhance cellular activity and pharmacokinetics. | ||||
Ref 526484 | J Med Chem. 2002 Dec 19;45(26):5687-93.Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. | ||||
Ref 526516 | In vivo antitumor activity of SU11248, a novel tyrosine kinase inhibitor targeting vascular endothelial growth factor and platelet-derived growth factor receptors: determination of a pharmacokinetic/pharmacodynamic relationship. Clin Cancer Res. 2003 Jan;9(1):327-37. | ||||
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 526669 | Bioorg Med Chem Lett. 2003 Aug 4;13(15):2485-8.Design and synthesis of 1,5-diarylbenzimidazoles as inhibitors of the VEGF-receptor KDR. | ||||
Ref 526703 | Bioorg Med Chem Lett. 2003 Sep 15;13(18):2973-6.Discovery and evaluation of 3-(5-thien-3-ylpyridin-3-yl)-1H-indoles as a novel class of KDR kinase inhibitors. | ||||
Ref 526914 | Bioorg Med Chem Lett. 2004 Jan 19;14(2):351-5.Optimization of the indolyl quinolinone class of KDR (VEGFR-2) kinase inhibitors: effects of 5-amido- and 5-sulphonamido-indolyl groups on pharmacokinetics and hERG binding. | ||||
Ref 527209 | Bioorg Med Chem Lett. 2004 Sep 6;14(17):4505-9.Isoindolinone ureas: a novel class of KDR kinase inhibitors. | ||||
Ref 527245 | J Med Chem. 2004 Oct 21;47(22):5367-80.Acyl sulfonamide anti-proliferatives: benzene substituent structure-activity relationships for a novel class of antitumor agents. | ||||
Ref 527458 | J Med Chem. 2005 Mar 10;48(5):1610-9.Discovery and evaluation of 2-anilino-5-aryloxazoles as a novel class of VEGFR2 kinase inhibitors. | ||||
Ref 527484 | Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J Biol Chem. 2005 May 20;280(20):19867-74. Epub 2005 Mar 16. | ||||
Ref 527569 | J Med Chem. 2005 Jun 2;48(11):3776-83.Synthesis, modeling, and in vitro activity of (3'S)-epi-K-252a analogues. Elucidating the stereochemical requirements of the 3'-sugar alcohol on trkA tyrosine kinase activity. | ||||
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 527725 | Bioorg Med Chem Lett. 2005 Nov 1;15(21):4696-8.Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase. | ||||
Ref 527793 | Bioorg Med Chem Lett. 2006 Jan 1;16(1):96-9. Epub 2005 Oct 10.Scaffold oriented synthesis. Part 1: Design, preparation, and biological evaluation of thienopyrazoles as kinase inhibitors. | ||||
Ref 527794 | Bioorg Med Chem Lett. 2006 Jan 1;16(1):129-33. Epub 2005 Oct 10.Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases. | ||||
Ref 527896 | Delphinidin, a dietary anthocyanidin, inhibits vascular endothelial growth factor receptor-2 phosphorylation. Carcinogenesis. 2006 May;27(5):989-96. Epub 2005 Nov 23. | ||||
Ref 527935 | Bioorg Med Chem Lett. 2006 Mar 1;16(5):1146-50. Epub 2005 Dec 20.Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase. | ||||
Ref 527948 | Bioorg Med Chem Lett. 2006 Mar 15;16(6):1579-81. Epub 2005 Dec 28.Arylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II. | ||||
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 528032 | J Med Chem. 2006 Feb 23;49(4):1271-81.Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. | ||||
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 528142 | Neuropilin-2 interacts with VEGFR-2 and VEGFR-3 and promotes human endothelial cell survival and migration. Blood. 2006 Aug 15;108(4):1243-50. Epub 2006 Apr 18. | ||||
Ref 528227 | Bioorg Med Chem Lett. 2006 Aug 15;16(16):4371-5. Epub 2006 Jun 5.Hit-to-lead optimization of 1,4-dihydroindeno[1,2-c]pyrazoles as a novel class of KDR kinase inhibitors. | ||||
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 528429 | J Med Chem. 2006 Sep 21;49(19):5671-86.Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity. | ||||
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. | ||||
Ref 528593 | Bioorg Med Chem Lett. 2007 Mar 1;17(5):1246-9. Epub 2006 Dec 9.Thienopyridine urea inhibitors of KDR kinase. | ||||
Ref 528681 | Bioorg Med Chem Lett. 2007 Apr 15;17(8):2126-33. Epub 2007 Feb 2.Pharmacophore modeling and in silico screening for new KDR kinase inhibitors. | ||||
Ref 528716 | J Med Chem. 2007 Apr 5;50(7):1584-97. Epub 2007 Mar 8.Discovery of N-(4-(3-amino-1H-indazol-4-yl)phenyl)-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), a 3-aminoindazole-based orally active multitargeted receptor tyrosine kinase inhibitor. | ||||
Ref 528774 | Bioorg Med Chem. 2007 Jun 1;15(11):3635-48. Epub 2007 Mar 23.Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2. | ||||
Ref 528821 | Bioorg Med Chem Lett. 2007 Jun 15;17(12):3266-70. Epub 2007 Apr 10.4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation. | ||||
Ref 528954 | The RET kinase inhibitor NVP-AST487 blocks growth and calcitonin gene expression through distinct mechanisms in medullary thyroid cancer cells. Cancer Res. 2007 Jul 15;67(14):6956-64. | ||||
Ref 529047 | Discovery of N-phenyl nicotinamides as potent inhibitors of Kdr. Bioorg Med Chem Lett. 2007 Nov 1;17(21):6003-8. Epub 2007 Aug 22. | ||||
Ref 529196 | Phase I evaluation of CDP791, a PEGylated di-Fab' conjugate that binds vascular endothelial growth factor receptor 2. Clin Cancer Res. 2007 Dec 1;13(23):7113-8. | ||||
Ref 529409 | Bioorg Med Chem Lett. 2008 May 1;18(9):2985-9. Epub 2008 Mar 22.Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor. | ||||
Ref 529647 | J Med Chem. 2008 Sep 25;51(18):5680-9. Epub 2008 Aug 21.Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models. | ||||
Ref 529744 | Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. Nat Chem Biol. 2008 Nov;4(11):691-9. | ||||
Ref 529891 | J 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 530377 | Bioorg Med Chem. 2009 Oct 15;17(20):7324-36. Epub 2009 Aug 22.Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors. | ||||
Ref 530452 | E7050: a dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer Sci. 2010 Jan;101(1):210-5. | ||||
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 530732 | Preclinical pharmacokinetics and in vitro metabolism of BMS-690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci. 2010 Aug;99(8):3579-93. | ||||
Ref 531412 | YN968D1 is a novel and selective inhibitor of vascular endothelial growth factor receptor-2 tyrosine kinase with potent activity in vitro and in vivo. Cancer Sci. 2011 Jul;102(7):1374-80. | ||||
Ref 531624 | Inhibition of c-Kit, VEGFR-2 (KDR), and ABCG2 by analogues of OSI-930. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6495-9. | ||||
Ref 531679 | Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol. 2011 Oct 30;29(11):1046-51. | ||||
Ref 531955 | OSI-930 analogues as novel reversal agents for ABCG2-mediated multidrug resistance. Biochem Pharmacol. 2012 Sep 15;84(6):766-74. | ||||
Ref 531959 | The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett. 2012 Aug 1;22(15):4979-85. | ||||
Ref 531962 | RAF265, a dual BRAF and VEGFR2 inhibitor, prevents osteoclast formation and resorption. Therapeutic implications. Invest New Drugs. 2013 Feb;31(1):200-5. | ||||
Ref 532029 | Clinical phase I study of elpamotide, a peptide vaccine for vascular endothelial growth factor receptor 2, in patients with advanced solid tumors. Cancer Sci. 2012 Dec;103(12):2135-8. | ||||
Ref 532072 | Vascular normalizing doses of antiangiogenic treatment reprogram the immunosuppressive tumor microenvironment and enhance immunotherapy. Proc Natl Acad Sci U S A. 2012 Oct 23;109(43):17561-6. | ||||
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 532338 | Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3248-52. | ||||
Ref 533061 | Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther. 2014;15(12):1635-45. | ||||
Ref 534662 | Synthesis and biological evaluations of 3-substituted indolin-2-ones: a novel class of tyrosine kinase inhibitors that exhibit selectivity toward particular receptor tyrosine kinases. J Med Chem. 1998 Jul 2;41(14):2588-603. | ||||
Ref 535250 | Technology evaluation: IMC-1C11, ImClone Systems. Curr Opin Mol Ther. 2001 Aug;3(4):418-24. | ||||
Ref 536137 | 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 536201 | YM-359445, an orally bioavailable vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor, has highly potent antitumor activity against established tumors. Clin Cancer Res. 2006 Mar 1;12(5):1630-8. | ||||
Ref 536260 | SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther. 2006 Jul;5(7):1774-82. | ||||
Ref 536474 | 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 537551 | 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. Epub 2009 Jun 29. | ||||
Ref 543499 | (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: 1813). | ||||
Ref 544325 | Inhibition of VEGFR-2 Reverses Type 1 Diabetes in NOD Mice by Abrogating Insulitis and Restoring Islet Function. Diabetes. 2013 August; 62(8): 2870-2878. | ||||
Ref 551871 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
Ref 553086 | Biochemical 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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