- 関
- vascular endothelial growth factor receptor、VEGFR
WordNet
- a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
PrepTutorEJDIC
- =sense organ / 受信装置
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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/03/19 09:57:33」(JST)
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| fms-related tyrosine kinase 1 (vascular endothelial growth factor/vascular permeability factor receptor) |
| Identifiers |
| Symbol |
FLT1 |
| Alt. symbols |
FLT |
| Entrez |
2321 |
| HUGO |
3763 |
| OMIM |
165070 |
| RefSeq |
NM_002019 |
| UniProt |
P17948 |
| Other data |
| EC number |
2.7.1.112 |
| Locus |
Chr. 13 q12 |
| kinase insert domain receptor (a type III receptor tyrosine kinase) |
| Identifiers |
| Symbol |
KDR |
| Alt. symbols |
FLK1, VEGFR, VEGFR2, CD309 |
| Entrez |
3791 |
| HUGO |
6307 |
| OMIM |
191306 |
| RefSeq |
NM_002253 |
| UniProt |
P35968 |
| Other data |
| EC number |
2.7.1.112 |
| Locus |
Chr. 4 q11-q12 |
| fms-related tyrosine kinase 4 |
| Identifiers |
| Symbol |
FLT4 |
| Alt. symbols |
VEGFR3, PCL |
| Entrez |
2324 |
| HUGO |
3767 |
| OMIM |
136352 |
| RefSeq |
NM_002020 |
| UniProt |
P35916 |
| Other data |
| EC number |
2.7.1.112 |
| Locus |
Chr. 5 q34-q35 |
|
VEGF receptors are receptors for vascular endothelial growth factor (VEGF).[1][2] There are three main subtypes of VEGFR, numbered 1, 2 and 3. Also, they may be membrane-bound (mbVEGFR) or soluble (sVEGFR), depending on alternative splicing.[3]
Contents
- 1 VEGF
- 2 Receptor biology
- 3 VEGFR antagonists
- 4 References
- 5 External links
VEGF
Main article: Vascular endothelial growth factor
Vascular endothelial growth factor (VEGF) is an important signaling protein involved in both vasculogenesis (the formation of the circulatory system) and angiogenesis (the growth of blood vessels from pre-existing vasculature). As its name implies, VEGF activity is restricted mainly to cells of the vascular endothelium, although it does have effects on a limited number of other cell types (e.g. stimulation monocyte/macrophage migration). In vitro, VEGF has been shown to stimulate endothelial cell mitogenesis and cell migration. VEGF also enhances microvascular permeability and is sometimes referred to as vascular permeability factor.
Receptor biology
Ligands for different VEGF receptors.
[4][5]
All members of the VEGF family stimulate cellular responses by binding to tyrosine kinase receptors (the VEGFRs) on the cell surface, causing them to dimerize and become activated through transphosphorylation. The VEGF receptors have an extracellular portion consisting of 7 immunoglobulin-like domains, a single transmembrane spanning region and an intracellular portion containing a split tyrosine-kinase domain.
VEGF-A binds to VEGFR-1 (Flt-1) and VEGFR-2 (KDR/Flk-1). VEGFR-2 appears to mediate almost all of the known cellular responses to VEGF.[1] The function of VEGFR-1 is less well defined, although it is thought to modulate VEGFR-2 signaling. Another function of VEGFR-1 is to act as a dummy/decoy receptor, sequestering VEGF from VEGFR-2 binding (this appears to be particularly important during vasculogenesis in the embryo). In fact, an alternatively spliced form of VEGFR-1 (sFlt1) is not a membrane bound protein but is secreted and functions primarily as a decoy.[6] A third receptor has been discovered (VEGFR-3), however, VEGF-A is not a ligand for this receptor. VEGFR-3 mediates lymphangiogenesis in response to VEGF-C and VEGF-D.
VEGFR antagonists
Some VEGFR antagonists (inhibitors) (for example lenvatinib, motesanib) are under investigation for treating various cancers. Pazopanib was approved for renal cell carcinoma in 2009. Regorafenib was approved for colorectal cancer in Sept 2012.
References
- ^ a b Holmes K, Roberts OL, Thomas AM, Cross MJ. (Oct 2007). "Vascular endothelial growth factor receptor-2: structure, function, intracellular signalling and therapeutic inhibition.". Cell Signal. 19 (10): 2003–2012. doi:10.1016/j.cellsig.2007.05.013. PMID 17658244.
- ^ Stuttfeld E, Ballmer-Hofer K (September 2009). "Structure and function of VEGF receptors". IUBMB Life 61 (9): 915–22. doi:10.1002/iub.234. PMID 19658168.
- ^ Fujita, N.; Imai, J.; Suzuki, T.; Yamada, M.; Ninomiya, K.; Miyamoto, K.; Iwasaki, R.; Morioka, H.; Matsumoto, M.; Chiba, K.; Watanabe, S.; Suda, T.; Toyama, Y.; Miyamoto, T. (2008). "Vascular endothelial growth factor-A is a survival factor for nucleus pulposus cells in the intervertebral disc". Biochemical and Biophysical Research Communications 372 (2): 367–372. doi:10.1016/j.bbrc.2008.05.044. PMID 18492486.
- ^ cancerpublications.com.
- ^ Interactions of VEGF ligands and VEGF receptors ResearchVEGF.com, retrieved on November 13, 2009
- ^ Zygmunt T, Gay CM, Blondelle J, Singh MK, Flaherty KM, Means PC, Herwig L, Krudewig A, Belting HG, Affolter M, Epstein JA, Torres-Vázquez J. (August 2011). "Semaphorin-PlexinD1 Signaling Limits Angiogenic Potential via the VEGF Decoy Receptor sFlt1". Dev Cell. 21 (2): 301–314. doi:10.1016/j.devcel.2011.06.033. PMC 3156278. PMID 21802375.
External links
- VEGF Receptors at the US National Library of Medicine Medical Subject Headings (MeSH)
- Proteopedia Vascular_Endothelial_Growth_Factor_Receptor - the Vascular Endothelial Growth Factor Receptor Structure in Interactive 3D
|
Receptors: growth factor receptors
|
|
| Type I cytokine receptor |
- Nerve growth factors: Ciliary neurotrophic factor
- Erythropoietin
|
|
| Receptor protein serine/threonine kinase |
- TGF pathway: TGF-beta
- Activin
- Bone morphogenetic protein
|
|
| Receptor tyrosine kinase |
|
|
|
- Nerve growth factors: high affinity Trk
|
|
|
|
|
- Somatomedin
- Insulin-like growth factor 1
|
|
- ErbB/Epidermal growth factor
|
|
|
|
|
|
| Tumor necrosis factor receptor |
- Nerve growth factors: Low affinity/p75
|
|
| Ig superfamily |
- Platelet-derived growth factor
- Stem cell factor
|
|
| Other/ungrouped |
- Somatomedin
- Insulin-like growth factor 2
|
|
|
Protein kinases: tyrosine kinases (EC 2.7.10)
|
|
|
Receptor tyrosine kinases (EC 2.7.10.1)
|
|
| Growth factor receptors |
| EGF receptor family |
|
|
| Insulin receptor family |
|
|
| PDGF receptor family |
- CSF1R
- FLT3
- KIT
- PDGFR (PDGFRA
- PDGFRB)
|
|
| FGF receptor family |
|
|
| VEGF receptors family |
|
|
| HGF receptor family |
|
|
| Trk receptor family |
|
|
|
| EPH receptor family |
- EPHA1
- EPHA2
- EPHA3
- EPHA4
- EPHA5
- EPHA6
- EPHA7
- EPHA8
- EPHB1
- EPHB2
- EPHB3
- EPHB4
- EPHB5
- EPHB6
- EPHX
|
|
| LTK receptor family |
|
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| TIE receptor family |
|
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| ROR receptor family |
|
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| DDR receptor family |
|
|
| PTK7 receptor family |
|
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| RYK receptor family |
|
|
| MuSK receptor family |
|
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| ROS receptor family |
|
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| AATYK receptor family |
|
|
| AXL receptor family |
|
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| RET receptor family |
|
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| uncatagorised |
|
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Non-receptor tyrosine kinases (EC 2.7.10.2)
|
|
| ABL family |
|
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| ACK family |
|
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| CSK family |
|
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| FAK family |
|
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| FES family |
|
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| FRK family |
|
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| JAK family |
|
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| SRC-A family |
|
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| SRC-B family |
|
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| TEC family |
|
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| SYK family |
|
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Proteins: enzymes
|
|
| Activity |
- Active site
- Binding site
- Catalytic triad
- Oxyanion hole
- Enzyme promiscuity
- Catalytically perfect enzyme
- Coenzyme
- Cofactor
- Enzyme catalysis
- Enzyme kinetics
- Lineweaver–Burk plot
- Michaelis–Menten kinetics
|
|
| Regulation |
- Allosteric regulation
- Cooperativity
- Enzyme inhibitor
|
|
| Classification |
- EC number
- Enzyme superfamily
- Enzyme family
- List of enzymes
|
|
| Types |
- EC1 Oxidoreductases(list)
- EC2 Transferases(list)
- EC3 Hydrolases(list)
- EC4 Lyases(list)
- EC5 Isomerases(list)
- EC6 Ligases(list)
|
|
UpToDate Contents
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English Journal
- Dopamine is a safe antiangiogenic drug which can also prevent 5-fluorouracil induced neutropenia.
- Sarkar C1, Chakroborty D1, Dasgupta PS2, Basu S1,3.
- International journal of cancer. Journal international du cancer.Int J Cancer.2015 Aug 1;137(3):744-9. doi: 10.1002/ijc.29414. Epub 2015 Jan 7.
- The role of vascular endothelial growth factor A (VEGFA) in tumor angiogenesis is well established and accordingly, molecules targeting VEGFA or its receptors are being presently used in the clinics for treatment of several types of cancer. However, these antiangiogenic agents are expensive and have
- PMID 25556636
- Safety profile of combined therapy inhibiting EFGR and VEGF pathways in patients with advanced non-small-cell lung cancer: A meta-analysis of 15 phase II/III randomized trials.
- Ma W1, Xu M2, Liu Y3, Liu H4, Huang J2, Zhu Y2, Ji LJ5, Qi X1,2.
- International journal of cancer. Journal international du cancer.Int J Cancer.2015 Jul 15;137(2):409-19. doi: 10.1002/ijc.29377. Epub 2014 Dec 12.
- The efficacy of combined vascular endothelial growth factor (VEGF) and epidermal growth factor receptor (EGFR) inhibition in patients with advanced non-small-cell lung cancer (NSCLC) was well studied. However, few studies focused on the risk and adverse events (AEs) of combined targeted therapy. The
- PMID 25471638
- Functional interaction between CTGF and FPRL1 regulates VEGF-A-induced angiogenesis.
- Lee MS1, Ghim J1, Kim SJ1, Yun YS1, Yoo SA2, Suh PG1, Kim WU3, Ryu SH4.
- Cellular signalling.Cell Signal.2015 Jul;27(7):1439-48. doi: 10.1016/j.cellsig.2015.04.001. Epub 2015 Apr 9.
- Vascular endothelial growth factor-A (VEGF-A) is a master regulator of angiogenesis that controls several angiogenic processes in endothelial cells. However, the detailed mechanisms of VEGF-A responsible for pleiotropic functions and crosstalk with other signaling pathways have not been fully unders
- PMID 25862954
Japanese Journal
- Identification of Tumor Endothelial Cells with High Aldehyde Dehydrogenase Activity and a Highly Angiogenic Phenotype
- Ohmura-Kakutani Hitomi,Akiyama Kosuke,Maishi Nako,Ohga Noritaka,Hida Yasuhiro,Kawamoto Taisuke,Iida Junichiro,Shindoh Masanobu,Tsuchiya Kunihiko,Shinohara Nobuo,Hida Kyoko
- PLOS one 9(12), e113910, 2014-12-01
- … TECs show higher proliferative and migratory abilities than those NECs, together with upregulation of vascular endothelial growth factor (VEGF) and VEGF receptor 2 (VEGFR2). …
- NAID 120005540289
- イマチニブによる血管周皮細胞を標的としたリンパ腫の治療 (特集 血管生物学の進歩と血液内科)
- Selenoprotein P as a diabetes-associated hepatokine that impairs angiogenesis by inducing VEGF resistance in vascular endothelial cells
- Ishikura Kazuhide,Misu Hirofumi,Kumazaki Masafumi,Takayama Hiroaki,Matsuzawa-Nagata Naoto,Tajima Natsumi,Chikamoto Keita,Lan Fei,Ando Hitoshi,Ota Tsuguhito,Sakurai Masaru,Takeshita Yumie,Kato Kenichiro,Fujimura Akio,Miyamoto Ken-ichi,Saito Yoshiro,Kameo Satomi,Okamoto Yasuo,Takuwa Yoh,Takahashi Kazuhiko,Kidoya Hiroyasu,Takakura Nobuyuki,Kaneko Shuichi,Takamaura Toshinari
- Diabetologia 57(9), 1968-1976, 2014-09
- … Aims/hypothesis Impaired angiogenesis induced by vascular endothelial growth factor (VEGF) resistance is a hallmark of vascular complications in type 2 diabetes; … Here, we investigated the effects of SeP on VEGF signalling and angiogenesis. … We examined the actions of SeP on VEGF signalling and VEGF-induced angiogenesis in HUVECs. …
- NAID 120005463349
Related Links
- 血管内皮細胞増殖因子受容体（けっかんないひさいぼうぞうしょくいんしじゅようたい、英: Vascular Endothelial Growth Factor Receptor、VEGFR）とは受容体型チロシン キナーゼの一種であり、リガンドである血管内皮増殖因子（VEGF）は血管内皮細胞の 増殖・ ...
- VEGF receptors are receptors for vascular endothelial growth factor (VEGF). There are three main subtypes of VEGFR, numbered 1, 2 and 3. Also, they may be membrane-bound (mbVEGFR) or soluble (sVEGFR), depending on alternative ...
★リンクテーブル★
[★]
- 英
- vascular endothelial growth factor receptor、VEGF receptor、VEGFR
- 関
- 血管内皮増殖因子レセプター、VEGF受容体、VEGFレセプター
[★]
- 英
- vascular endothelial growth factor receptor、VEGF receptor
- 関
- 血管内皮増殖因子受容体、VEGF受容体、VEGFレセプター
[★]
- 英
- VEGF receptor
- 関
- 血管内皮増殖因子受容体、血管内皮増殖因子レセプター、VEGFレセプター
[★]
- 英
- VEGF receptor
- 関
- 血管内皮増殖因子受容体、血管内皮増殖因子レセプター、VEGF受容体
[★]
血管内皮増殖因子受容体、血管内皮増殖因子レセプター
- 関
- VEGF receptor、VEGFR
[★]
血管内皮増殖因子 vascular endothelial growth factor