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fms related receptor tyrosine kinase 1

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Target id: 1812

Nomenclature: fms related receptor tyrosine kinase 1

Abbreviated Name: VEGFR-1

Family: Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1338 13q12.3 FLT1 fms related receptor tyrosine kinase 1
Mouse 1 1333 5 87.01 cM Flt1 FMS-like tyrosine kinase 1
Rat 1 1336 12p11 Flt1 Fms related receptor tyrosine kinase 1
Previous and Unofficial Names Click here for help
fms related tyrosine kinase 1 | FMS-related tyrosine kinase 1 | fms-related tyrosine kinase 1 | vascular endothelial growth factor receptor 1
Database Links Click here for help
Alphafold P17948 (Hs), P35969 (Mm), P53767 (Rn)
BRENDA 2.7.10.1
CATH/Gene3D 2.60.40.10
ChEMBL Target CHEMBL1868 (Hs), CHEMBL3516 (Mm)
DrugBank Target P17948 (Hs)
Ensembl Gene ENSG00000102755 (Hs), ENSMUSG00000029648 (Mm), ENSRNOG00000000940 (Rn)
Entrez Gene 2321 (Hs), 14254 (Mm), 54251 (Rn)
Human Protein Atlas ENSG00000102755 (Hs)
KEGG Enzyme 2.7.10.1
KEGG Gene hsa:2321 (Hs), mmu:14254 (Mm), rno:54251 (Rn)
OMIM 165070 (Hs)
Pharos P17948 (Hs)
RefSeq Nucleotide NM_001159920 (Hs), NM_010228 (Mm), NM_019306 (Rn)
RefSeq Protein NP_001153392 (Hs), NP_034358 (Mm), NP_062179 (Rn)
UniProtKB P17948 (Hs), P35969 (Mm), P53767 (Rn)
Wikipedia FLT1 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of VEGFR1 (FLT1) in complex with N-(4-Chlorophenyl)-2-((pyridin-4-ylmethyl)amino)benzamide.
PDB Id:  3HNG
Resolution:  2.7Å
Species:  Human
References: 
Enzyme Reaction Click here for help
EC Number: 2.7.10.1
Natural/Endogenous Ligands Click here for help
VEGFA {Sp: Human}
VEGFB {Sp: Human}

Download all structure-activity data for this target as a CSV file go icon to follow link

Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
RG-1530 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pKd 29
⤷ pKd 8.1 (Kd 9x10-9 M) [29]
compound 25 [PMID: 17935989] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pKi 27
⤷ pKi 6.4 (Ki 4.4x10-7 M) [27]
tivozanib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.7 pIC50 21
⤷ pIC50 9.7 (IC50 2.1x10-10 M) [21]
foretinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.1 pIC50 21
⤷ pIC50 9.1 (IC50 8x10-10 M) [21]
VEGF receptor tyrosine kinase inhibitor III Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.0 pIC50 9
⤷ pIC50 9.0 (IC50 1x10-9 M) [9]
ilorasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.0 pIC50 12
⤷ pIC50 9.0 (IC50 1x10-9 M) [12]
Description: Measuring inhibition of kinase activity in a biochemical assay.
motesanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pIC50 21
⤷ pIC50 8.7 (IC50 2x10-9 M) [21]
SU-14813 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.7 pIC50 24
⤷ pIC50 8.7 (IC50 2x10-9 M) [24]
tinengotinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.6 pIC50 33
⤷ pIC50 8.6 (IC50 2.4x10-9 M) [33]
linifanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.5 pIC50 1
⤷ pIC50 8.5 (IC50 3x10-9 M) [1]
CEP-11981 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.5 pIC50 16
⤷ pIC50 8.5 (IC50 3x10-9 M) [16]
catequentinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 8.4 pIC50 7
⤷ pIC50 8.4 (IC50 4x10-9 M) [7]
Description: In vitro activity
cediranib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.3 pIC50 31
⤷ pIC50 8.3 (IC50 5x10-9 M) [31]
dovitinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 – 8.5 pIC50 25,30
⤷ pIC50 8.0 – 8.5 (IC50 1x10-8 – 3x10-9 M) [25,30]
sitravatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.2 pIC50 23
⤷ pIC50 8.2 (IC50 6x10-9 M) [23]
Description: In a biochemical enzyme activity assay.
compound 8h [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 17
⤷ pIC50 8.1 (IC50 7.2x10-9 M) [17]
semaxanib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.1 pIC50 6
⤷ pIC50 8.1 (IC50 8x10-9 M) [6]
OSI-930 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 11
⤷ pIC50 8.1 (IC50 8x10-9 M) [11]
ibcasertib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 36
⤷ pIC50 8.1 (IC50 8x10-9 M) [36]
Description: Inhibition in a biochemical assay.
pazopanib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.0 pIC50 13
⤷ pIC50 8.0 (IC50 1x10-8 M) [13]
MK-2461 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.0 pIC50 22
⤷ pIC50 8.0 (IC50 1x10-8 M) [22]
dorsomorphin Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.0 pIC50 20
⤷ pIC50 8.0 (IC50 1.1x10-8 M) [20]
Description: Assayed using AMPK heterotrimeric complex containing α2, β1, γ1 subunits
lucitanib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.9 pIC50 35
⤷ pIC50 7.9 (IC50 1.2x10-8 M) [35]
compound 8i [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.5 – 7.7 pIC50 17,34
⤷ pIC50 7.7 (IC50 2x10-8 M) [17]
pIC50 7.5 (IC50 2.9x10-8 M) [34]
nintedanib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 15
⤷ pIC50 7.5 (IC50 3.1x10-8 M) [15]
Cdk1/2 inhibitor III Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 19
⤷ pIC50 7.5 (IC50 3.2x10-8 M) [19]
fruquintinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 7.5 pIC50 26
⤷ pIC50 7.5 (IC50 3.3x10-8 M) [26]
Description: Evaluated in a [32]p-ATP incorporation assay
pexmetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.3 pIC50 4
⤷ pIC50 7.3 (IC50 4.7x10-8 M) [4]
vatalanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.8 pIC50 18
⤷ pIC50 6.8 (IC50 1.4x10-7 M) [18]
brivanib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.4 pIC50 5
⤷ pIC50 6.4 (IC50 3.8x10-7 M) [5]
ZM-306416 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 5.7 – 6.5 pIC50 3,14
⤷ pIC50 5.7 – 6.5 (IC50 2x10-6 – 3.3x10-7 M) [3,14]
pexidartinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.1 pIC50 28
⤷ pIC50 6.1 (IC50 8.8x10-7 M) [28]
Inhibitor Comments
Note that pazopanib is a multi-target kinase inhibitor. See for [13] futher affinity data.
Compound 25 [PMID 17935989] is a CHK1 inhibitor and interacts with VEGFR1 as an off-target. Inhibiton of CHK1 is >100 times more potent than inhibition of VEGFR1 [...].
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 8,32
Key to terms and symbols Click column headers to sort
Target used in screen: FLT1
Ligand Sp. Type Action Value Parameter
cediranib Small molecule or natural product Hs Inhibitor Inhibition 9.1 pKd
sunitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
SU-14813 Small molecule or natural product Hs Inhibitor Inhibition 8.3 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.2 pKd
linifanib Small molecule or natural product Hs Inhibitor Inhibition 8.1 pKd
vatalanib Small molecule or natural product Hs Inhibitor Inhibition 8.0 pKd
brivanib Small molecule or natural product Hs Inhibitor Inhibition 8.0 pKd
motesanib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 7.8 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: 2,10
Key to terms and symbols Click column headers to sort
Target used in screen: Flt1/FLT1(VEGFR1)
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
PDK1/Akt/Flt dual pathway inhibitor Small molecule or natural product Hs Inhibitor Inhibition 3.1 115.0 89.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 0.0 -0.5
TWS119 Small molecule or natural product Hs Inhibitor Inhibition 8.6 0.0 0.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 11.4 0.0 -1.0
SB 218078 Small molecule or natural product Hs Inhibitor Inhibition 13.3 7.0 4.0
Gö 6983 Small molecule or natural product Hs Inhibitor Inhibition 22.0 2.0 0.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 23.2 0.0 0.0
VEGF receptor tyrosine kinase inhibitor II Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 24.8 0.0 2.0
dovitinib Small molecule or natural product Hs Inhibitor Inhibition 26.2
pazopanib Small molecule or natural product Approved drug Hs Inhibitor Inhibition 27.2
Displaying the top 10 most potent ligands  View all ligands in screen »
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Chemotaxis & migration
Immuno Process:  Immune regulation
Immuno Process:  Cytokine production & signalling
Immuno Process:  Immune system development

References

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1. Albert DH, Tapang P, Magoc TJ, Pease LJ, Reuter DR, Wei RQ, Li J, Guo J, Bousquet PF, Ghoreishi-Haack NS et al.. (2006) Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol Cancer Ther, 5 (4): 995-1006. [PMID:16648571]

2. Anastassiadis T, Deacon SW, Devarajan K, Ma H, Peterson JR. (2011) Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1039-45. [PMID:22037377]

3. Antczak C, Mahida JP, Bhinder B, Calder PA, Djaballah H. (2012) A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery. J Biomol Screen, 17 (7): 885-99. [PMID:22573732]

4. Bachegowda L, Morrone K, Winski SL, Mantzaris I, Bartenstein M, Ramachandra N, Giricz O, Sukrithan V, Nwankwo G, Shahnaz S et al.. (2016) Pexmetinib: A Novel Dual Inhibitor of Tie2 and p38 MAPK with Efficacy in Preclinical Models of Myelodysplastic Syndromes and Acute Myeloid Leukemia. Cancer Res, 76 (16): 4841-4849. [PMID:27287719]

5. Bhide RS, Cai ZW, Zhang YZ, Qian L, Wei D, Barbosa S, Lombardo LJ, Borzilleri RM, Zheng X, Wu LI et al.. (2006) Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor. J Med Chem, 49 (7): 2143-6. [PMID:16570908]

6. Bold G, Altmann KH, Frei J, Lang M, Manley PW, Traxler P, Wietfeld B, Brüggen J, Buchdunger E, Cozens R et al.. (2000) New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. J Med Chem, 43 (12): 2310-23. [PMID:10882357]

7. Chen GP. (2008) Spiro substituted compounds as angiogenesis inhibitors. Patent number: WO2008112407 A1. Assignee: Advenchen Laboratories, Llc. Priority date: 14/03/2007. Publication date: 18/09/2008.

8. Davis MI, Hunt JP, Herrgard S, Ciceri P, Wodicka LM, Pallares G, Hocker M, Treiber DK, Zarrinkar PP. (2011) Comprehensive analysis of kinase inhibitor selectivity. Nat Biotechnol, 29 (11): 1046-51. [PMID:22037378]

9. Fedorov O, Marsden B, Pogacic V, Rellos P, Müller S, Bullock AN, Schwaller J, Sundström M, Knapp S. (2007) A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. Proc Natl Acad Sci USA, 104 (51): 20523-8. [PMID:18077363]

10. Gao Y, Davies SP, Augustin M, Woodward A, Patel UA, Kovelman R, Harvey KJ. (2013) A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. Biochem J, 451 (2): 313-28. [PMID:23398362]

11. Garton AJ, Crew AP, Franklin M, Cooke AR, Wynne GM, Castaldo L, Kahler J, Winski SL, Franks A, Brown EN et al.. (2006) OSI-930: a novel selective inhibitor of Kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models. Cancer Res, 66 (2): 1015-24. [PMID:16424037]

12. Glaser KB, Li J, Marcotte PA, Magoc TJ, Guo J, Reuter DR, Tapang P, Wei RQ, Pease LJ, Bui MH et al.. (2012) Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J Pharmacol Exp Ther, 343 (3): 617-27. [PMID:22935731]

13. Harris PA, Boloor A, Cheung M, Kumar R, Crosby RM, Davis-Ward RG, Epperly AH, Hinkle KW, Hunter 3rd RN, Johnson JH et al.. (2008) Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor. J Med Chem, 51 (15): 4632-40. [PMID:18620382]

14. Hennequin LF, Thomas AP, Johnstone C, Stokes ES, Plé PA, Lohmann JJ, Ogilvie DJ, Dukes M, Wedge SR, Curwen JO et al.. (1999) Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors. J Med Chem, 42 (26): 5369-89. [PMID:10639280]

15. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J et al.. (2008) BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res, 68 (12): 4774-82. [PMID:18559524]

16. Hudkins RL, Becknell NC, Zulli AL, Underiner TL, Angeles TS, Aimone LD, Albom MS, Chang H, Miknyoczki SJ, Hunter K et al.. (2012) Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent. J Med Chem, 55 (2): 903-13. [PMID:22148921]

17. Kim MH, Tsuhako AL, Co EW, Aftab DT, Bentzien F, Chen J, Cheng W, Engst S, Goon L, Klein RR et al.. (2012) The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors. Bioorg Med Chem Lett, 22 (15): 4979-85. [PMID:22765894]

18. Kiselyov AS, Semenova M, Semenov VV, Piatnitski E, Ouyang S. (2006) Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II. Bioorg Med Chem Lett, 16 (5): 1440-4. [PMID:16321531]

19. Lin R, Connolly PJ, Huang S, Wetter SK, Lu Y, Murray WV, Emanuel SL, Gruninger RH, Fuentes-Pesquera AR, Rugg CA et al.. (2005) 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities. J Med Chem, 48 (13): 4208-11. [PMID:15974571]

20. Machrouhi F, Ouhamou N, Laderoute K, Calaoagan J, Bukhtiyarova M, Ehrlich PJ, Klon AE. (2010) The rational design of a novel potent analogue of the 5'-AMP-activated protein kinase inhibitor compound C with improved selectivity and cellular activity. Bioorg Med Chem Lett, 20 (22): 6394-9. [PMID:20932747]

21. Musumeci F, Radi M, Brullo C, Schenone S. (2012) Vascular endothelial growth factor (VEGF) receptors: drugs and new inhibitors. J Med Chem, 55 (24): 10797-822. [PMID:23098265]

22. Pan BS, Chan GK, Chenard M, Chi A, Davis LJ, Deshmukh SV, Gibbs JB, Gil S, Hang G, Hatch H et al.. (2010) MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res, 70 (4): 1524-33. [PMID:20145145]

23. Patwardhan PP, Ivy KS, Musi E, de Stanchina E, Schwartz GK. (2016) Significant blockade of multiple receptor tyrosine kinases by MGCD516 (Sitravatinib), a novel small molecule inhibitor, shows potent anti-tumor activity in preclinical models of sarcoma. Oncotarget, 7 (4): 4093-109. [PMID:26675259]

24. Patyna S, Laird AD, Mendel DB, O'farrell AM, Liang C, Guan H, Vojkovsky T, Vasile S, Wang X, Chen J et al.. (2006) SU14813: a novel multiple receptor tyrosine kinase inhibitor with potent antiangiogenic and antitumor activity. Mol Cancer Ther, 5 (7): 1774-82. [PMID:16891463]

25. Renhowe PA, Pecchi S, Shafer CM, Machajewski TD, Jazan EM, Taylor C, Antonios-McCrea W, McBride CM, Frazier K, Wiesmann M et al.. (2009) 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. J Med Chem, 52 (2): 278-92. [PMID:19113866]

26. Sun Q, Zhou J, Zhang Z, Guo M, Liang J, Zhou F, Long J, Zhang W, Yin F, Cai H et al.. (2014) Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy. Cancer Biol Ther, 15 (12): 1635-45. [PMID:25482937]

27. Tao ZF, Chen Z, Bui MH, Kovar P, Johnson E, Bouska J, Zhang H, Rosenberg S, Sowin T, Lin NH. (2007) Macrocyclic ureas as potent and selective Chk1 inhibitors: an improved synthesis, kinome profiling, structure-activity relationships, and preliminary pharmacokinetics. Bioorg Med Chem Lett, 17 (23): 6593-601. [PMID:17935989]

28. Tap WD, Wainberg ZA, Anthony SP, Ibrahim PN, Zhang C, Healey JH, Chmielowski B, Staddon AP, Cohn AL, Shapiro GI et al.. (2015) Structure-Guided Blockade of CSF1R Kinase in Tenosynovial Giant-Cell Tumor. N Engl J Med, 373 (5): 428-37. [PMID:26222558]

29. Tovar C, Higgins B, Deo D, Kolinsky K, Liu JJ, Heimbrook DC, Vassilev LT. (2010) Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle, 9 (16): 3364-75. [PMID:20814247]

30. Trudel S, Li ZH, Wei E, Wiesmann M, Chang H, Chen C, Reece D, Heise C, Stewart AK. (2005) CHIR-258, a novel, multitargeted tyrosine kinase inhibitor for the potential treatment of t(4;14) multiple myeloma. Blood, 105 (7): 2941-8. [PMID:15598814]

31. Wedge SR, Kendrew J, Hennequin LF, Valentine PJ, Barry ST, Brave SR, Smith NR, James NH, Dukes M, Curwen JO et al.. (2005) AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer. Cancer Res, 65 (10): 4389-400. [PMID:15899831]

32. Wodicka LM, Ciceri P, Davis MI, Hunt JP, Floyd M, Salerno S, Hua XH, Ford JM, Armstrong RC, Zarrinkar PP et al.. (2010) Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. Chem Biol, 17 (11): 1241-9. [PMID:21095574]

33. Wu F. (2021) Multi-kinase inhibitor compound, and crystal form and use thereof. Patent number: US10889586B2. Assignee: Nanjing Transthera Biosciences Co Ltd. Priority date: 13/12/2016. Publication date: 12/01/2021.

34. You WK, Sennino B, Williamson CW, Falcón B, Hashizume H, Yao LC, Aftab DT, McDonald DM. (2011) VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 71 (14): 4758-68. [PMID:21613405]

35. Zhou Y, Chen Y, Tong L, Xie H, Wen W, Zhang J, Xi Y, Shen Y, Geng M, Wang Y et al.. (2012) AL3810, a multi-tyrosine kinase inhibitor, exhibits potent anti-angiogenic and anti-tumour activity via targeting VEGFR, FGFR and PDGFR. J Cell Mol Med, 16 (10): 2321-30. [PMID:22304225]

36. Zhou Y, Shan S, Li ZB, Xin LJ, Pan DS, Yang QJ, Liu YP, Yue XP, Liu XR, Gao JZ et al.. (2017) CS2164, a novel multi-target inhibitor against tumor angiogenesis, mitosis and chronic inflammation with anti-tumor potency. Cancer Sci, 108 (3): 469-477. [PMID:28004478]

How to cite this page

Type IV RTKs: VEGF (vascular endothelial growth factor) receptor family: fms related receptor tyrosine kinase 1. Last modified on 04/02/2022. Accessed on 19/04/2024. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1812.