Vascular endothelial growth factor receptor 1

Details

Name
Vascular endothelial growth factor receptor 1
Synonyms
  • 2.7.10.1
  • FLT
  • FLT-1
  • Fms-like tyrosine kinase 1
  • FRT
  • Tyrosine-protein kinase FRT
  • Tyrosine-protein kinase receptor FLT
  • Vascular permeability factor receptor
  • VEGFR-1
  • VEGFR1
Gene Name
FLT1
Organism
Humans
Amino acid sequence
>lcl|BSEQ0036938|Vascular endothelial growth factor receptor 1
MVSYWDTGVLLCALLSCLLLTGSSSGSKLKDPELSLKGTQHIMQAGQTLHLQCRGEAAHK
WSLPEMVSKESERLSITKSACGRNGKQFCSTLTLNTAQANHTGFYSCKYLAVPTSKKKET
ESAIYIFISDTGRPFVEMYSEIPEIIHMTEGRELVIPCRVTSPNITVTLKKFPLDTLIPD
GKRIIWDSRKGFIISNATYKEIGLLTCEATVNGHLYKTNYLTHRQTNTIIDVQISTPRPV
KLLRGHTLVLNCTATTPLNTRVQMTWSYPDEKNKRASVRRRIDQSNSHANIFYSVLTIDK
MQNKDKGLYTCRVRSGPSFKSVNTSVHIYDKAFITVKHRKQQVLETVAGKRSYRLSMKVK
AFPSPEVVWLKDGLPATEKSARYLTRGYSLIIKDVTEEDAGNYTILLSIKQSNVFKNLTA
TLIVNVKPQIYEKAVSSFPDPALYPLGSRQILTCTAYGIPQPTIKWFWHPCNHNHSEARC
DFCSNNEESFILDADSNMGNRIESITQRMAIIEGKNKMASTLVVADSRISGIYICIASNK
VGTVGRNISFYITDVPNGFHVNLEKMPTEGEDLKLSCTVNKFLYRDVTWILLRTVNNRTM
HYSISKQKMAITKEHSITLNLTIMNVSLQDSGTYACRARNVYTGEEILQKKEITIRDQEA
PYLLRNLSDHTVAISSSTTLDCHANGVPEPQITWFKNNHKIQQEPGIILGPGSSTLFIER
VTEEDEGVYHCKATNQKGSVESSAYLTVQGTSDKSNLELITLTCTCVAATLFWLLLTLFI
RKMKRSSSEIKTDYLSIIMDPDEVPLDEQCERLPYDASKWEFARERLKLGKSLGRGAFGK
VVQASAFGIKKSPTCRTVAVKMLKEGATASEYKALMTELKILTHIGHHLNVVNLLGACTK
QGGPLMVIVEYCKYGNLSNYLKSKRDLFFLNKDAALHMEPKKEKMEPGLEQGKKPRLDSV
TSSESFASSGFQEDKSLSDVEEEEDSDGFYKEPITMEDLISYSFQVARGMEFLSSRKCIH
RDLAARNILLSENNVVKICDFGLARDIYKNPDYVRKGDTRLPLKWMAPESIFDKIYSTKS
DVWSYGVLLWEIFSLGGSPYPGVQMDEDFCSRLREGMRMRAPEYSTPEIYQIMLDCWHRD
PKERPRFAELVEKLGDLLQANVQQDGKDYIPINAILTGNSGFTYSTPAFSEDFFKESISA
PKFNSGSSDDVRYVNAFKFMSLERIKTFEELLPNATSMFDDYQGDSSTLLASPMLKRFTW
TDSKPKASLKIDLRVTSKSKESGLSDVSRPSFCHSSCGHVSEGKRRFTYDHAELERKIAC
CSPPPDYNSVVLYSTPPI
Number of residues
1338
Molecular Weight
150767.185
Theoretical pI
8.48
GO Classification
Functions
ATP binding / growth factor binding / placental growth factor-activated receptor activity / transmembrane receptor protein tyrosine kinase activity / vascular endothelial growth factor-activated receptor activity / VEGF-A-activated receptor activity / VEGF-B-activated receptor activity
Processes
angiogenesis / blood vessel morphogenesis / cell differentiation / cell migration / cellular response to vascular endothelial growth factor stimulus / embryonic morphogenesis / monocyte chemotaxis / peptidyl-tyrosine phosphorylation / positive regulation of angiogenesis / positive regulation of cell migration / positive regulation of cell proliferation / positive regulation of MAP kinase activity / positive regulation of MAPK cascade / positive regulation of phosphatidylinositol 3-kinase activity / positive regulation of phosphatidylinositol 3-kinase signaling / positive regulation of phospholipase C activity / positive regulation of vascular endothelial growth factor receptor signaling pathway / protein autophosphorylation / transmembrane receptor protein tyrosine kinase signaling pathway / vascular endothelial growth factor receptor signaling pathway / vascular endothelial growth factor receptor-1 signaling pathway / vascular endothelial growth factor signaling pathway
Components
endosome / extracellular space / focal adhesion / integral component of plasma membrane / plasma membrane / receptor complex
General Function
Vegf-b-activated receptor activity
Specific Function
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell survival, cell migration, macrophage function, chemotaxis, and cancer cell invasion. May play an essential role as a negative regulator of embryonic angiogenesis by inhibiting excessive proliferation of endothelial cells. Can promote endothelial cell proliferation, survival and angiogenesis in adulthood. Its function in promoting cell proliferation seems to be cell-type specific. Promotes PGF-mediated proliferation of endothelial cells, proliferation of some types of cancer cells, but does not promote proliferation of normal fibroblasts (in vitro). Has very high affinity for VEGFA and relatively low protein kinase activity; may function as a negative regulator of VEGFA signaling by limiting the amount of free VEGFA and preventing its binding to KDR. Likewise, isoforms lacking a transmembrane domain, such as isoform 2, isoform 3 and isoform 4, may function as decoy receptors for VEGFA. Modulates KDR signaling by forming heterodimers with KDR. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate and the activation of protein kinase C. Mediates phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, leading to activation of phosphatidylinositol kinase and the downstream signaling pathway. Mediates activation of MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Phosphorylates SRC and YES1, and may also phosphorylate CBL. Isoform 1 phosphorylates PLCG. Promotes phosphorylation of AKT1 at 'Ser-473'. Promotes phosphorylation of PTK2/FAK1. Isoform 7 has a truncated kinase domain; it increases phosphorylation of SRC at 'Tyr-418' by unknown means and promotes tumor cell invasion.
Pfam Domain Function
Transmembrane Regions
759-780
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0010136|Vascular endothelial growth factor receptor 1 (FLT1)
ATGGTCAGCTACTGGGACACCGGGGTCCTGCTGTGCGCGCTGCTCAGCTGTCTGCTTCTC
ACAGGATCTAGTTCAGGTTCAAAATTAAAAGATCCTGAACTGAGTTTAAAAGGCACCCAG
CACATCATGCAAGCAGGCCAGACACTGCATCTCCAATGCAGGGGGGAAGCAGCCCATAAA
TGGTCTTTGCCTGAAATGGTGAGTAAGGAAAGCGAAAGGCTGAGCATAACTAAATCTGCC
TGTGGAAGAAATGGCAAACAATTCTGCAGTACTTTAACCTTGAACACAGCTCAAGCAAAC
CACACTGGCTTCTACAGCTGCAAATATCTAGCTGTACCTACTTCAAAGAAGAAGGAAACA
GAATCTGCAATCTATATATTTATTAGTGATACAGGTAGACCTTTCGTAGAGATGTACAGT
GAAATCCCCGAAATTATACACATGACTGAAGGAAGGGAGCTCGTCATTCCCTGCCGGGTT
ACGTCACCTAACATCACTGTTACTTTAAAAAAGTTTCCACTTGACACTTTGATCCCTGAT
GGAAAACGCATAATCTGGGACAGTAGAAAGGGCTTCATCATATCAAATGCAACGTACAAA
GAAATAGGGCTTCTGACCTGTGAAGCAACAGTCAATGGGCATTTGTATAAGACAAACTAT
CTCACACATCGACAAACCAATACAATCATAGATGTCCAAATAAGCACACCACGCCCAGTC
AAATTACTTAGAGGCCATACTCTTGTCCTCAATTGTACTGCTACCACTCCCTTGAACACG
AGAGTTCAAATGACCTGGAGTTACCCTGATGAAAAAAATAAGAGAGCTTCCGTAAGGCGA
CGAATTGACCAAAGCAATTCCCATGCCAACATATTCTACAGTGTTCTTACTATTGACAAA
ATGCAGAACAAAGACAAAGGACTTTATACTTGTCGTGTAAGGAGTGGACCATCATTCAAA
TCTGTTAACACCTCAGTGCATATATATGATAAAGCATTCATCACTGTGAAACATCGAAAA
CAGCAGGTGCTTGAAACCGTAGCTGGCAAGCGGTCTTACCGGCTCTCTATGAAAGTGAAG
GCATTTCCCTCGCCGGAAGTTGTATGGTTAAAAGATGGGTTACCTGCGACTGAGAAATCT
GCTCGCTATTTGACTCGTGGCTACTCGTTAATTATCAAGGACGTAACTGAAGAGGATGCA
GGGAATTATACAATCTTGCTGAGCATAAAACAGTCAAATGTGTTTAAAAACCTCACTGCC
ACTCTAATTGTCAATGTGAAACCCCAGATTTACGAAAAGGCCGTGTCATCGTTTCCAGAC
CCGGCTCTCTACCCACTGGGCAGCAGACAAATCCTGACTTGTACCGCATATGGTATCCCT
CAACCTACAATCAAGTGGTTCTGGCACCCCTGTAACCATAATCATTCCGAAGCAAGGTGT
GACTTTTGTTCCAATAATGAAGAGTCCTTTATCCTGGATGCTGACAGCAACATGGGAAAC
AGAATTGAGAGCATCACTCAGCGCATGGCAATAATAGAAGGAAAGAATAAGATGGCTAGC
ACCTTGGTTGTGGCTGACTCTAGAATTTCTGGAATCTACATTTGCATAGCTTCCAATAAA
GTTGGGACTGTGGGAAGAAACATAAGCTTTTATATCACAGATGTGCCAAATGGGTTTCAT
GTTAACTTGGAAAAAATGCCGACGGAAGGAGAGGACCTGAAACTGTCTTGCACAGTTAAC
AAGTTCTTATACAGAGACGTTACTTGGATTTTACTGCGGACAGTTAATAACAGAACAATG
CACTACAGTATTAGCAAGCAAAAAATGGCCATCACTAAGGAGCACTCCATCACTCTTAAT
CTTACCATCATGAATGTTTCCCTGCAAGATTCAGGCACCTATGCCTGCAGAGCCAGGAAT
GTATACACAGGGGAAGAAATCCTCCAGAAGAAAGAAATTACAATCAGAGGTGAGCACTGC
AACAAAAAGGCTGTTTTCTCTCGGATCTCCAAATTTAAAAGCACAAGGAATGATTGTACC
ACACAAAGTAATGTAAAACATTAA
Chromosome Location
13
Locus
13q12
External Identifiers
ResourceLink
UniProtKB IDP17948
UniProtKB Entry NameVGFR1_HUMAN
GenBank Protein ID31432
GenBank Gene IDX51602
GenAtlas IDFLT1
HGNC IDHGNC:3763
General References
  1. Shibuya M, Yamaguchi S, Yamane A, Ikeda T, Tojo A, Matsushime H, Sato M: Nucleotide sequence and expression of a novel human receptor-type tyrosine kinase gene (flt) closely related to the fms family. Oncogene. 1990 Apr;5(4):519-24. [Article]
  2. Kendall RL, Thomas KA: Inhibition of vascular endothelial cell growth factor activity by an endogenously encoded soluble receptor. Proc Natl Acad Sci U S A. 1993 Nov 15;90(22):10705-9. [Article]
  3. Herley MT, Yu Y, Whitney RG, Sato JD: Characterization of the VEGF binding site on the Flt-1 receptor. Biochem Biophys Res Commun. 1999 Sep 7;262(3):731-8. [Article]
  4. Jin P, Zhang J, Sumariwalla PF, Ni I, Jorgensen B, Crawford D, Phillips S, Feldmann M, Shepard HM, Paleolog EM: Novel splice variants derived from the receptor tyrosine kinase superfamily are potential therapeutics for rheumatoid arthritis. Arthritis Res Ther. 2008;10(4):R73. doi: 10.1186/ar2447. Epub 2008 Jul 1. [Article]
  5. Sela S, Itin A, Natanson-Yaron S, Greenfield C, Goldman-Wohl D, Yagel S, Keshet E: A novel human-specific soluble vascular endothelial growth factor receptor 1: cell-type-specific splicing and implications to vascular endothelial growth factor homeostasis and preeclampsia. Circ Res. 2008 Jun 20;102(12):1566-74. doi: 10.1161/CIRCRESAHA.108.171504. Epub 2008 May 30. [Article]
  6. Mezquita B, Mezquita J, Pau M, Mezquita C: A novel intracellular isoform of VEGFR-1 activates Src and promotes cell invasion in MDA-MB-231 breast cancer cells. J Cell Biochem. 2010 Jun 1;110(3):732-42. doi: 10.1002/jcb.22584. [Article]
  7. Ota T, Suzuki Y, Nishikawa T, Otsuki T, Sugiyama T, Irie R, Wakamatsu A, Hayashi K, Sato H, Nagai K, Kimura K, Makita H, Sekine M, Obayashi M, Nishi T, Shibahara T, Tanaka T, Ishii S, Yamamoto J, Saito K, Kawai Y, Isono Y, Nakamura Y, Nagahari K, Murakami K, Yasuda T, Iwayanagi T, Wagatsuma M, Shiratori A, Sudo H, Hosoiri T, Kaku Y, Kodaira H, Kondo H, Sugawara M, Takahashi M, Kanda K, Yokoi T, Furuya T, Kikkawa E, Omura Y, Abe K, Kamihara K, Katsuta N, Sato K, Tanikawa M, Yamazaki M, Ninomiya K, Ishibashi T, Yamashita H, Murakawa K, Fujimori K, Tanai H, Kimata M, Watanabe M, Hiraoka S, Chiba Y, Ishida S, Ono Y, Takiguchi S, Watanabe S, Yosida M, Hotuta T, Kusano J, Kanehori K, Takahashi-Fujii A, Hara H, Tanase TO, Nomura Y, Togiya S, Komai F, Hara R, Takeuchi K, Arita M, Imose N, Musashino K, Yuuki H, Oshima A, Sasaki N, Aotsuka S, Yoshikawa Y, Matsunawa H, Ichihara T, Shiohata N, Sano S, Moriya S, Momiyama H, Satoh N, Takami S, Terashima Y, Suzuki O, Nakagawa S, Senoh A, Mizoguchi H, Goto Y, Shimizu F, Wakebe H, Hishigaki H, Watanabe T, Sugiyama A, Takemoto M, Kawakami B, Yamazaki M, Watanabe K, Kumagai A, Itakura S, Fukuzumi Y, Fujimori Y, Komiyama M, Tashiro H, Tanigami A, Fujiwara T, Ono T, Yamada K, Fujii Y, Ozaki K, Hirao M, Ohmori Y, Kawabata A, Hikiji T, Kobatake N, Inagaki H, Ikema Y, Okamoto S, Okitani R, Kawakami T, Noguchi S, Itoh T, Shigeta K, Senba T, Matsumura K, Nakajima Y, Mizuno T, Morinaga M, Sasaki M, Togashi T, Oyama M, Hata H, Watanabe M, Komatsu T, Mizushima-Sugano J, Satoh T, Shirai Y, Takahashi Y, Nakagawa K, Okumura K, Nagase T, Nomura N, Kikuchi H, Masuho Y, Yamashita R, Nakai K, Yada T, Nakamura Y, Ohara O, Isogai T, Sugano S: Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat Genet. 2004 Jan;36(1):40-5. Epub 2003 Dec 21. [Article]
  8. Dunham A, Matthews LH, Burton J, Ashurst JL, Howe KL, Ashcroft KJ, Beare DM, Burford DC, Hunt SE, Griffiths-Jones S, Jones MC, Keenan SJ, Oliver K, Scott CE, Ainscough R, Almeida JP, Ambrose KD, Andrews DT, Ashwell RI, Babbage AK, Bagguley CL, Bailey J, Bannerjee R, Barlow KF, Bates K, Beasley H, Bird CP, Bray-Allen S, Brown AJ, Brown JY, Burrill W, Carder C, Carter NP, Chapman JC, Clamp ME, Clark SY, Clarke G, Clee CM, Clegg SC, Cobley V, Collins JE, Corby N, Coville GJ, Deloukas P, Dhami P, Dunham I, Dunn M, Earthrowl ME, Ellington AG, Faulkner L, Frankish AG, Frankland J, French L, Garner P, Garnett J, Gilbert JG, Gilson CJ, Ghori J, Grafham DV, Gribble SM, Griffiths C, Hall RE, Hammond S, Harley JL, Hart EA, Heath PD, Howden PJ, Huckle EJ, Hunt PJ, Hunt AR, Johnson C, Johnson D, Kay M, Kimberley AM, King A, Laird GK, Langford CJ, Lawlor S, Leongamornlert DA, Lloyd DM, Lloyd C, Loveland JE, Lovell J, Martin S, Mashreghi-Mohammadi M, McLaren SJ, McMurray A, Milne S, Moore MJ, Nickerson T, Palmer SA, Pearce AV, Peck AI, Pelan S, Phillimore B, Porter KM, Rice CM, Searle S, Sehra HK, Shownkeen R, Skuce CD, Smith M, Steward CA, Sycamore N, Tester J, Thomas DW, Tracey A, Tromans A, Tubby B, Wall M, Wallis JM, West AP, Whitehead SL, Willey DL, Wilming L, Wray PW, Wright MW, Young L, Coulson A, Durbin R, Hubbard T, Sulston JE, Beck S, Bentley DR, Rogers J, Ross MT: The DNA sequence and analysis of human chromosome 13. Nature. 2004 Apr 1;428(6982):522-8. [Article]
  9. Gerhard DS, Wagner L, Feingold EA, Shenmen CM, Grouse LH, Schuler G, Klein SL, Old S, Rasooly R, Good P, Guyer M, Peck AM, Derge JG, Lipman D, Collins FS, Jang W, Sherry S, Feolo M, Misquitta L, Lee E, Rotmistrovsky K, Greenhut SF, Schaefer CF, Buetow K, Bonner TI, Haussler D, Kent J, Kiekhaus M, Furey T, Brent M, Prange C, Schreiber K, Shapiro N, Bhat NK, Hopkins RF, Hsie F, Driscoll T, Soares MB, Casavant TL, Scheetz TE, Brown-stein MJ, Usdin TB, Toshiyuki S, Carninci P, Piao Y, Dudekula DB, Ko MS, Kawakami K, Suzuki Y, Sugano S, Gruber CE, Smith MR, Simmons B, Moore T, Waterman R, Johnson SL, Ruan Y, Wei CL, Mathavan S, Gunaratne PH, Wu J, Garcia AM, Hulyk SW, Fuh E, Yuan Y, Sneed A, Kowis C, Hodgson A, Muzny DM, McPherson J, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madari A, Young AC, Wetherby KD, Granite SJ, Kwong PN, Brinkley CP, Pearson RL, Bouffard GG, Blakesly RW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Griffith M, Griffith OL, Krzywinski MI, Liao N, Morin R, Palmquist D, Petrescu AS, Skalska U, Smailus DE, Stott JM, Schnerch A, Schein JE, Jones SJ, Holt RA, Baross A, Marra MA, Clifton S, Makowski KA, Bosak S, Malek J: The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. 2004 Oct;14(10B):2121-7. [Article]
  10. Matsushime H, Yoshida MC, Sasaki M, Shibuya M: A possible new member of tyrosine kinase family, human frt sequence, is highly conserved in vertebrates and located on human chromosome 13. Jpn J Cancer Res. 1987 Jul;78(7):655-61. [Article]
  11. Ito N, Wernstedt C, Engstrom U, Claesson-Welsh L: Identification of vascular endothelial growth factor receptor-1 tyrosine phosphorylation sites and binding of SH2 domain-containing molecules. J Biol Chem. 1998 Sep 4;273(36):23410-8. [Article]
  12. Seetharam L, Gotoh N, Maru Y, Neufeld G, Yamaguchi S, Shibuya M: A unique signal transduction from FLT tyrosine kinase, a receptor for vascular endothelial growth factor VEGF. Oncogene. 1995 Jan 5;10(1):135-47. [Article]
  13. Barleon B, Sozzani S, Zhou D, Weich HA, Mantovani A, Marme D: Migration of human monocytes in response to vascular endothelial growth factor (VEGF) is mediated via the VEGF receptor flt-1. Blood. 1996 Apr 15;87(8):3336-43. [Article]
  14. Sawano A, Takahashi T, Yamaguchi S, Shibuya M: The phosphorylated 1169-tyrosine containing region of flt-1 kinase (VEGFR-1) is a major binding site for PLCgamma. Biochem Biophys Res Commun. 1997 Sep 18;238(2):487-91. [Article]
  15. Igarashi K, Isohara T, Kato T, Shigeta K, Yamano T, Uno I: Tyrosine 1213 of Flt-1 is a major binding site of Nck and SHP-2. Biochem Biophys Res Commun. 1998 May 8;246(1):95-9. [Article]
  16. Dunk C, Ahmed A: Vascular endothelial growth factor receptor-2-mediated mitogenesis is negatively regulated by vascular endothelial growth factor receptor-1 in tumor epithelial cells. Am J Pathol. 2001 Jan;158(1):265-73. [Article]
  17. Yu Y, Hulmes JD, Herley MT, Whitney RG, Crabb JW, Sato JD: Direct identification of a major autophosphorylation site on vascular endothelial growth factor receptor Flt-1 that mediates phosphatidylinositol 3'-kinase binding. Biochem J. 2001 Sep 1;358(Pt 2):465-72. [Article]
  18. Angelucci C, Lama G, Iacopino F, Maglione D, Sica G: Effect of placenta growth factor-1 on proliferation and release of nitric oxide, cyclic AMP and cyclic GMP in human epithelial cells expressing the FLT-1 receptor. Growth Factors. 2001;19(3):193-206. [Article]
  19. Huang K, Andersson C, Roomans GM, Ito N, Claesson-Welsh L: Signaling properties of VEGF receptor-1 and -2 homo- and heterodimers. Int J Biochem Cell Biol. 2001 Apr;33(4):315-24. [Article]
  20. Cai J, Ahmad S, Jiang WG, Huang J, Kontos CD, Boulton M, Ahmed A: Activation of vascular endothelial growth factor receptor-1 sustains angiogenesis and Bcl-2 expression via the phosphatidylinositol 3-kinase pathway in endothelial cells. Diabetes. 2003 Dec;52(12):2959-68. [Article]
  21. Autiero M, Waltenberger J, Communi D, Kranz A, Moons L, Lambrechts D, Kroll J, Plaisance S, De Mol M, Bono F, Kliche S, Fellbrich G, Ballmer-Hofer K, Maglione D, Mayr-Beyrle U, Dewerchin M, Dombrowski S, Stanimirovic D, Van Hummelen P, Dehio C, Hicklin DJ, Persico G, Herbert JM, Communi D, Shibuya M, Collen D, Conway EM, Carmeliet P: Role of PlGF in the intra- and intermolecular cross talk between the VEGF receptors Flt1 and Flk1. Nat Med. 2003 Jul;9(7):936-43. [Article]
  22. Kobayashi S, Sawano A, Nojima Y, Shibuya M, Maru Y: The c-Cbl/CD2AP complex regulates VEGF-induced endocytosis and degradation of Flt-1 (VEGFR-1). FASEB J. 2004 May;18(7):929-31. Epub 2004 Mar 4. [Article]
  23. Fan F, Wey JS, McCarty MF, Belcheva A, Liu W, Bauer TW, Somcio RJ, Wu Y, Hooper A, Hicklin DJ, Ellis LM: Expression and function of vascular endothelial growth factor receptor-1 on human colorectal cancer cells. Oncogene. 2005 Apr 14;24(16):2647-53. [Article]
  24. Lesslie DP, Summy JM, Parikh NU, Fan F, Trevino JG, Sawyer TK, Metcalf CA, Shakespeare WC, Hicklin DJ, Ellis LM, Gallick GE: Vascular endothelial growth factor receptor-1 mediates migration of human colorectal carcinoma cells by activation of Src family kinases. Br J Cancer. 2006 Jun 5;94(11):1710-7. [Article]
  25. Meyer RD, Mohammadi M, Rahimi N: A single amino acid substitution in the activation loop defines the decoy characteristic of VEGFR-1/FLT-1. J Biol Chem. 2006 Jan 13;281(2):867-75. Epub 2005 Nov 14. [Article]
  26. Tchaikovski V, Fellbrich G, Waltenberger J: The molecular basis of VEGFR-1 signal transduction pathways in primary human monocytes. Arterioscler Thromb Vasc Biol. 2008 Feb;28(2):322-8. Epub 2007 Dec 13. [Article]
  27. Nishi J, Minamino T, Miyauchi H, Nojima A, Tateno K, Okada S, Orimo M, Moriya J, Fong GH, Sunagawa K, Shibuya M, Komuro I: Vascular endothelial growth factor receptor-1 regulates postnatal angiogenesis through inhibition of the excessive activation of Akt. Circ Res. 2008 Aug 1;103(3):261-8. doi: 10.1161/CIRCRESAHA.108.174128. Epub 2008 Jun 26. [Article]
  28. Taylor AP, Leon E, Goldenberg DM: Placental growth factor (PlGF) enhances breast cancer cell motility by mobilising ERK1/2 phosphorylation and cytoskeletal rearrangement. Br J Cancer. 2010 Jun 29;103(1):82-9. doi: 10.1038/sj.bjc.6605746. Epub 2010 Jun 15. [Article]
  29. Wang F, Yamauchi M, Muramatsu M, Osawa T, Tsuchida R, Shibuya M: RACK1 regulates VEGF/Flt1-mediated cell migration via activation of a PI3K/Akt pathway. J Biol Chem. 2011 Mar 18;286(11):9097-106. doi: 10.1074/jbc.M110.165605. Epub 2011 Jan 6. [Article]
  30. Cai J, Chen Z, Ruan Q, Han S, Liu L, Qi X, Boye SL, Hauswirth WW, Grant MB, Boulton ME: gamma-Secretase and presenilin mediate cleavage and phosphorylation of vascular endothelial growth factor receptor-1. J Biol Chem. 2011 Dec 9;286(49):42514-23. doi: 10.1074/jbc.M111.296590. Epub 2011 Oct 20. [Article]
  31. Ahmad S, Hewett PW, Al-Ani B, Sissaoui S, Fujisawa T, Cudmore MJ, Ahmed A: Autocrine activity of soluble Flt-1 controls endothelial cell function and angiogenesis. Vasc Cell. 2011 Jul 13;3(1):15. doi: 10.1186/2045-824X-3-15. [Article]
  32. Shibuya M: Differential roles of vascular endothelial growth factor receptor-1 and receptor-2 in angiogenesis. J Biochem Mol Biol. 2006 Sep 30;39(5):469-78. [Article]
  33. Roskoski R Jr: VEGF receptor protein-tyrosine kinases: structure and regulation. Biochem Biophys Res Commun. 2008 Oct 24;375(3):287-91. doi: 10.1016/j.bbrc.2008.07.121. Epub 2008 Aug 3. [Article]
  34. Lohela M, Bry M, Tammela T, Alitalo K: VEGFs and receptors involved in angiogenesis versus lymphangiogenesis. Curr Opin Cell Biol. 2009 Apr;21(2):154-65. doi: 10.1016/j.ceb.2008.12.012. Epub 2009 Feb 21. [Article]
  35. Grunewald FS, Prota AE, Giese A, Ballmer-Hofer K: Structure-function analysis of VEGF receptor activation and the role of coreceptors in angiogenic signaling. Biochim Biophys Acta. 2010 Mar;1804(3):567-80. doi: 10.1016/j.bbapap.2009.09.002. Epub 2009 Sep 15. [Article]
  36. Schwartz JD, Rowinsky EK, Youssoufian H, Pytowski B, Wu Y: Vascular endothelial growth factor receptor-1 in human cancer: concise review and rationale for development of IMC-18F1 (Human antibody targeting vascular endothelial growth factor receptor-1). Cancer. 2010 Feb 15;116(4 Suppl):1027-32. doi: 10.1002/cncr.24789. [Article]
  37. Koch S, Tugues S, Li X, Gualandi L, Claesson-Welsh L: Signal transduction by vascular endothelial growth factor receptors. Biochem J. 2011 Jul 15;437(2):169-83. doi: 10.1042/BJ20110301. [Article]
  38. Shibuya M: Involvement of Flt-1 (VEGF receptor-1) in cancer and preeclampsia. Proc Jpn Acad Ser B Phys Biol Sci. 2011;87(4):167-78. [Article]
  39. Wiesmann C, Fuh G, Christinger HW, Eigenbrot C, Wells JA, de Vos AM: Crystal structure at 1.7 A resolution of VEGF in complex with domain 2 of the Flt-1 receptor. Cell. 1997 Nov 28;91(5):695-704. [Article]
  40. Starovasnik MA, Christinger HW, Wiesmann C, Champe MA, de Vos AM, Skelton NJ: Solution structure of the VEGF-binding domain of Flt-1: comparison of its free and bound states. J Mol Biol. 1999 Oct 29;293(3):531-44. [Article]
  41. Christinger HW, Fuh G, de Vos AM, Wiesmann C: The crystal structure of placental growth factor in complex with domain 2 of vascular endothelial growth factor receptor-1. J Biol Chem. 2004 Mar 12;279(11):10382-8. Epub 2003 Dec 18. [Article]
  42. Iyer S, Darley PI, Acharya KR: Structural insights into the binding of vascular endothelial growth factor-B by VEGFR-1(D2): recognition and specificity. J Biol Chem. 2010 Jul 30;285(31):23779-89. doi: 10.1074/jbc.M110.130658. Epub 2010 May 25. [Article]
  43. Greenman C, Stephens P, Smith R, Dalgliesh GL, Hunter C, Bignell G, Davies H, Teague J, Butler A, Stevens C, Edkins S, O'Meara S, Vastrik I, Schmidt EE, Avis T, Barthorpe S, Bhamra G, Buck G, Choudhury B, Clements J, Cole J, Dicks E, Forbes S, Gray K, Halliday K, Harrison R, Hills K, Hinton J, Jenkinson A, Jones D, Menzies A, Mironenko T, Perry J, Raine K, Richardson D, Shepherd R, Small A, Tofts C, Varian J, Webb T, West S, Widaa S, Yates A, Cahill DP, Louis DN, Goldstraw P, Nicholson AG, Brasseur F, Looijenga L, Weber BL, Chiew YE, DeFazio A, Greaves MF, Green AR, Campbell P, Birney E, Easton DF, Chenevix-Trench G, Tan MH, Khoo SK, Teh BT, Yuen ST, Leung SY, Wooster R, Futreal PA, Stratton MR: Patterns of somatic mutation in human cancer genomes. Nature. 2007 Mar 8;446(7132):153-8. [Article]

Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB01268Sunitinibapproved, investigationalyesinhibitorDetails
DB04879VatalanibinvestigationalunknownDetails
DB05075TG-100801investigationalunknownDetails
DB06080LinifanibinvestigationalunknownDetails
DB05913OSI-930investigationalunknownDetails
DB06101IMC-1C11investigationalunknownDetails
DB05932DenibulininvestigationalunknownDetails
DB06589PazopanibapprovedyesinhibitorDetails
DB06626Axitinibapproved, investigationalyesinhibitorDetails
DB07288N-(4-chlorophenyl)-2-[(pyridin-4-ylmethyl)amino]benzamideexperimentalunknownDetails
DB08896RegorafenibapprovedyesinhibitorDetails
DB00398Sorafenibapproved, investigationalyesinhibitorDetails
DB09078Lenvatinibapproved, investigationalyesinhibitorDetails
DB09079NintedanibapprovedyesinhibitorDetails
DB09221PolaprezincexperimentalunknownagonistDetails
DB10770Foreskin fibroblast (neonatal)approvedyesagonistDetails
DB12010Fostamatinibapproved, investigationalunknowninhibitorDetails
DB15685Selpercatinibapproved, investigationalunknowninhibitorDetails
DB11800Tivozanibapproved, investigationalyesinhibitorDetails