血管内皮増殖因子受容体2

関: vascular endothelial growth factor receptor-2

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/06/30 13:58:16」(JST)

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Kinase insert domain receptor (KDR, a type III receptor tyrosine kinase) also known as vascular endothelial growth factor receptor 2 (VEGFR-2) is a VEGF receptor. KDR is the human gene encoding it. KDR has also been designated as CD309 (cluster of differentiation 309). KDR is also known as Flk1 (Fetal Liver Kinase 1).

Interactions

Kinase insert domain receptor has been shown to interact with SHC2,^[1] Annexin A5^[2] and SHC1.^[3]^[4]

References

^ Warner, A J; Lopez-Dee J; Knight E L; Feramisco J R; Prigent S A (April 2000). "The Shc-related adaptor protein, Sck, forms a complex with the vascular-endothelial-growth-factor receptor KDR in transfected cells". Biochem. J. (England) 347 (Pt 2): 501–9. doi:10.1042/0264-6021:3470501. ISSN 0264-6021. PMC 1220983. PMID 10749680.
^ Wen, Y; Edelman J L; Kang T; Sachs G (May 1999). "Lipocortin V may function as a signaling protein for vascular endothelial growth factor receptor-2/Flk-1". Biochem. Biophys. Res. Commun. (UNITED STATES) 258 (3): 713–21. doi:10.1006/bbrc.1999.0678. ISSN 0006-291X. PMID 10329451.
^ Zanetti, Adriana; Lampugnani Maria Grazia; Balconi Giovanna; Breviario Ferruccio; Corada Monica; Lanfrancone Luisa; Dejana Elisabetta (April 2002). "Vascular endothelial growth factor induces SHC association with vascular endothelial cadherin: a potential feedback mechanism to control vascular endothelial growth factor receptor-2 signaling". Arterioscler. Thromb. Vasc. Biol. (United States) 22 (4): 617–22. doi:10.1161/01.ATV.0000012268.84961.AD. PMID 11950700.
^ D'Angelo, G; Martini J F; Iiri T; Fantl W J; Martial J; Weiner R I (May 1999). "16K human prolactin inhibits vascular endothelial growth factor-induced activation of Ras in capillary endothelial cells". Mol. Endocrinol. (UNITED STATES) 13 (5): 692–704. doi:10.1210/mend.13.5.0280. ISSN 0888-8809. PMID 10319320.

External links

Kinase insert domain receptor at the US National Library of Medicine Medical Subject Headings (MeSH)

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.

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Japanese Journal

Immunohistochemical detection of a potential molecular therapeutic target for canine hemangiosarcoma

Journal of Veterinary Medical Science 78(4), 649-656, 2016-04
NAID 120005766748

注目の新薬ラムシルマブ(ramucirumab) : 血管新生を抑制する抗VEGFR-2抗体

国際医薬品情報 (1030), 17-19, 2015-03-23
NAID 40020402502

Ramucirumab

腫瘍内科 = Clinical oncology 15(2), 213-217, 2015-02
NAID 40020372081

「ソラフェニブ」

KDR
Available structures
PDB	Ortholog search: PDBe RCSB
List of PDB id codes
	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, 3VHE, 3VHK, 3VID, 3VNT, 3VO3, 3WZD, 3WZE, 4AG8, 4AGC, 4AGD, 4ASD, 4ASE, 5EW3
Identifiers
Aliases	KDR, CD309, FLK1, VEGFR, VEGFR2, Kinase insert domain receptor
External IDs	MGI: 96683 HomoloGene: 55639 GeneCards: 3791
Gene ontology
Molecular function	• vascular endothelial growth factor-activated receptor activity; • transferase activity; • Hsp90 protein binding; • nucleotide binding; • protein kinase activity; • receptor signaling protein tyrosine kinase activity; • growth factor binding; • vascular endothelial growth factor binding; • kinase activity; • integrin binding; • protein binding; • transmembrane receptor protein tyrosine kinase activity; • protein tyrosine kinase activity; • ATP binding;
Cellular component	• cytoplasm; • integral component of membrane; • endosome; • Golgi apparatus; • membrane; • plasma membrane; • integral component of plasma membrane; • cytoplasmic, membrane-bounded vesicle; • extracellular region; • cell junction; • early endosome; • endoplasmic reticulum; • membrane raft; • sorting endosome; • cytoplasmic vesicle; • nucleus;
Biological process	• negative regulation of endothelial cell apoptotic process; • cell differentiation; • positive regulation of protein phosphorylation; • positive regulation of mitochondrial fission; • positive regulation of endothelial cell proliferation; • signal transduction by protein phosphorylation; • phosphorylation; • transmembrane receptor protein tyrosine kinase signaling pathway; • positive regulation of cell migration; • extracellular matrix organization; • negative regulation of apoptotic process; • positive regulation of nitric-oxide synthase biosynthetic process; • cell migration involved in sprouting angiogenesis; • positive regulation of angiogenesis; • vasculogenesis; • positive regulation of endothelial cell migration; • multicellular organism development; • protein phosphorylation; • positive regulation of macroautophagy; • vascular endothelial growth factor receptor signaling pathway; • positive regulation of mitochondrial depolarization; • positive regulation of vasculogenesis; • angiogenesis; • positive regulation of cell proliferation; • embryonic hemopoiesis; • endothelium development; • regulation of cell shape; • positive regulation of endothelial cell chemotaxis by VEGF-activated vascular endothelial growth factor receptor signaling pathway; • positive regulation of ERK1 and ERK2 cascade; • peptidyl-tyrosine autophosphorylation; • protein autophosphorylation; • positive regulation of focal adhesion assembly; • positive regulation of phosphatidylinositol 3-kinase signaling; • peptidyl-tyrosine phosphorylation; • cellular response to vascular endothelial growth factor stimulus; • viral process; • calcium-mediated signaling using intracellular calcium source; • positive regulation of MAPK cascade; • positive regulation of positive chemotaxis;
	Sources:Amigo / QuickGO
RNA expression pattern
	More reference expression data
Orthologs
	3791
	16542
	ENSG00000128052
	ENSMUSG00000062960
	P35968
	P35918
	NM_002253
	NM_010612
	NP_002244.1
	n/a
	Wikidata
View/Edit Human	View/Edit Mouse

　　[★]

英: sorafenib
商: ネクサバール
関: その他の腫瘍用薬。上皮成長因子受容体阻害薬

もともとC-RAFを阻害するように設計されたが、B-RAFに対する阻害作用も認められた。
さらにVEGFR-2やPDFDR-βのチロシンキナーゼ活性も阻害することが示されている

効能又は効果／用法及び用量

根治切除不能又は転移性の腎細胞癌，切除不能な肝細胞癌

作用機序

(1)

1. B-Rafのキナーゼ活性やc-KIT受容体のチロシンキナーゼ活性などを阻害することで腫瘍進行を阻止
2. 血管内皮増殖因子受容体（VEGFR）や血小板由来成長因子受容体（PDGFR）のチロシンキナーゼ活性を阻害し腫瘍血管形成に対抗する

参考

1. wikipedia ja

http://ja.wikipedia.org/wiki/%E3%82%BD%E3%83%A9%E3%83%95%E3%82%A7%E3%83%8B%E3%83%96

添付文書

ネクサバール錠200mg

http://www.info.pmda.go.jp/go/pack/4291017F1025_1_12/4291017F1025_1_12?view=body

「サイラムザ」

　　[★]

商品名

サイラムザ

会社名

日本イーライリリー

成分

ラムシルマブ

薬効分類

抗悪性腫瘍剤, ヒト型抗VEGFR-2モノクローナル抗体

薬効

治癒切除不能な進行・再発の胃癌を効能・効果とする新有効成分含有医薬品

【優先審査】

「血管内皮増殖因子受容体2」

　　[★]

英: vascular endothelial growth factor receptor-2、VEGFR-2
関: 血管内皮増殖因子受容体-2

「vascular endothelial growth factor receptor-2」

　　[★]

血管内皮増殖因子受容体2

関: VEGFR-2

「VEGFR」

　　[★]

血管内皮増殖因子受容体

関: vascular endothelial growth factor receptor、VEGF receptor

「VEGF」

　　[★] 血管内皮増殖因子 vascular endothelial growth factor

[pmid10749680-1] Warner, A J; Lopez-Dee J; Knight E L; Feramisco J R; Prigent S A (April 2000). "The Shc-related adaptor protein, Sck, forms a complex with the vascular-endothelial-growth-factor receptor KDR in transfected cells". Biochem. J. (England) 347 (Pt 2): 501–9. doi:10.1042/0264-6021:3470501. ISSN 0264-6021. PMC 1220983. PMID 10749680.

[pmid10329451-2] Wen, Y; Edelman J L; Kang T; Sachs G (May 1999). "Lipocortin V may function as a signaling protein for vascular endothelial growth factor receptor-2/Flk-1". Biochem. Biophys. Res. Commun. (UNITED STATES) 258 (3): 713–21. doi:10.1006/bbrc.1999.0678. ISSN 0006-291X. PMID 10329451.

[pmid11950700-3] Zanetti, Adriana; Lampugnani Maria Grazia; Balconi Giovanna; Breviario Ferruccio; Corada Monica; Lanfrancone Luisa; Dejana Elisabetta (April 2002). "Vascular endothelial growth factor induces SHC association with vascular endothelial cadherin: a potential feedback mechanism to control vascular endothelial growth factor receptor-2 signaling". Arterioscler. Thromb. Vasc. Biol. (United States) 22 (4): 617–22. doi:10.1161/01.ATV.0000012268.84961.AD. PMID 11950700.

[pmid10319320-4] D'Angelo, G; Martini J F; Iiri T; Fantl W J; Martial J; Weiner R I (May 1999). "16K human prolactin inhibits vascular endothelial growth factor-induced activation of Ras in capillary endothelial cells". Mol. Endocrinol. (UNITED STATES) 13 (5): 692–704. doi:10.1210/mend.13.5.0280. ISSN 0888-8809. PMID 10319320.

リンク元	「ソラフェニブ」「サイラムザ」「血管内皮増殖因子受容体2」「vascular endothelial growth factor receptor-2」
関連記事	「VEGFR」「VEGF」

匿名

検索

案内

案内

VEGFR-2