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MET proto-oncogene, receptor tyrosine kinase

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Immunopharmacology Ligand  Target has curated data in GtoImmuPdb

Target id: 1815

Nomenclature: MET proto-oncogene, receptor tyrosine kinase

Abbreviated Name: MET

Family: Type X RTKs: HGF (hepatocyte growth factor) receptor family

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 1 1390 7q31 MET MET proto-oncogene, receptor tyrosine kinase
Mouse 1 1379 6 7.83 cM Met met proto-oncogene
Rat 1 1382 4q21 Met MET proto-oncogene, receptor tyrosine kinase
Previous and Unofficial Names Click here for help
RCCP2 | c-Met | HGF receptor | HGF/SF receptor | scatter factor receptor | Par4 | hepatocyte growth factor receptor | mesenchymal-epithelial transition factor (c-Met) receptor | MET proto-oncogene
Database Links Click here for help
Alphafold
BRENDA
CATH/Gene3D
ChEMBL Target
DrugBank Target
Ensembl Gene
Entrez Gene
Human Protein Atlas
KEGG Enzyme
KEGG Gene
OMIM
Orphanet
Pharos
RefSeq Nucleotide
RefSeq Protein
SynPHARM
UniProtKB
Wikipedia
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  x-ray structure of c-Met with inhibitor.
PDB Id:  2RFN
Ligand:  AM7
Resolution:  2.5Å
Species:  Human
References:  3
Image of receptor 3D structure from RCSB PDB
Description:  CRYSTAL STRUCTURE OF THE TYROSINE KINASE DOMAIN OF THE HEPATOCYTE GROWTH FACTOR RECEPTOR C-MET
PDB Id:  1R1W
Resolution:  1.8Å
Species:  Human
References:  39
Image of receptor 3D structure from RCSB PDB
Description:  Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors.
PDB Id:  4R1V
Ligand:  tepotinib
Resolution:  1.2Å
Species:  Human
References:  16
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of c-Met in complex with triazolopyridazine inhibitor 2.
PDB Id:  4DEG
Ligand:  AMG-337
Resolution:  2.0Å
Species:  Human
References:  6
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of c-Met in complex with LY2801653 (merestinib).
PDB Id:  4EEV
Ligand:  merestinib
Resolution:  1.8Å
Species:  Human
References:  49
Enzyme Reaction Click here for help
EC Number: 2.7.10.1
Natural/Endogenous Ligands Click here for help
hepatocyte growth factor {Sp: Human}

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Inhibitors
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
SGX-523 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 9.7 pKd 15
pKd 9.7 (Kd 1.9x10-10 M) [15]
PHA-665752 Small molecule or natural product Primary target of this compound Hs Inhibition 9.6 pKd 15
pKd 9.6 (Kd 2.7x10-10 M) [15]
foretinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.9 pKd 15
pKd 8.9 (Kd 1.4x10-9 M) [15]
crizotinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.7 pKi 13
pKi 8.7 (Ki 2x10-9 M) [13]
merestinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.7 pKi 49
pKi 8.7 (Ki 2x10-9 M) [49]
PHA-665752 Small molecule or natural product Primary target of this compound Hs Inhibition 8.4 pKi 11
pKi 8.4 (Ki 4x10-9 M) [11]
pamufetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.4 pKi 18
pKi 7.4 (Ki 3.9x10-8 M) [18]
tivantinib Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 6.4 pKi 32
pKi 6.4 (Ki 3.55x10-7 M) [32]
tanespimycin Small molecule or natural product Immunopharmacology Ligand Hs Inhibition 18.0 pIC50 42
pIC50 18.0 [42]
Description: Measuring downstream uPA-plasmin inhibition.
capmatinib Small molecule or natural product Approved drug Primary target of this compound Hs Inhibition 9.9 pIC50 28
pIC50 9.9 (IC50 1.3x10-10 M) [28]
glumetinib Small molecule or natural product Hs Inhibition 9.4 pIC50 1
pIC50 9.4 (IC50 4.2x10-10 M) [1]
Description: Inhibition of the kinase activity of purified c-Met using ELISA kinase assay.
foretinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.3 – 9.4 pIC50 27,33
pIC50 9.3 – 9.4 (IC50 5x10-10 – 4x10-10 M) [27,33]
ensartinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 9.1 pIC50 29
pIC50 9.1 (IC50 7.4x10-10 M) [29]
Description: Result from DiscoveRx KINOMEscan® selectivity screen.
crizotinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 9.1 pIC50 43
pIC50 9.1 (IC50 7.8x10-10 M) [43]
cabozantinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.9 pIC50 48
pIC50 8.9 (IC50 1.3x10-9 M) [48]
MK-2461 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.6 pIC50 35
pIC50 8.6 (IC50 2.5x10-9 M) [35]
altiratinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.6 pIC50 17
pIC50 8.6 (IC50 2.7x10-9 M) [17]
tepotinib Small molecule or natural product Approved drug Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.5 pIC50 5
pIC50 8.5 (IC50 3x10-9 M) [5]
Description: Measured in a flash-plate assay using recombinant human c-Met kinase domain and a biotinylated peptide substrate.
OMO-1 Small molecule or natural product Hs Inhibition 7.9 – 9.0 pIC50 30
pIC50 9.0 (IC50 1x10-9 M) [30]
Description: Inhibition of c-Met autophosphorylation measured in a time resolved fluorescence assay (DELFIA).
pIC50 7.9 (IC50 1.2x10-8 M) [30]
Description: Inhibition of HGF stimulated c-Met phosphorylation in a cell-based assay.
BMS-777607 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.4 pIC50 41
pIC50 8.4 (IC50 3.9x10-9 M) [41]
SGX-523 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.4 pIC50 8
pIC50 8.4 (IC50 4x10-9 M) [8]
merestinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.3 pIC50 49
pIC50 8.3 (IC50 4.7x10-9 M) [49]
Description: Inhibition of in vitro biochemical activity by EMD Millipore assay.
AMG-337 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.3 pIC50 7
pIC50 8.3 (IC50 5x10-9 M) [7]
Description: Biochemically assessed value.
savolitinib Small molecule or natural product Ligand has a PDB structure Hs Inhibition 8.3 pIC50 24
pIC50 8.3 (IC50 5x10-9 M) [24]
compound 1o [PMID: 24210504] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.1 pIC50 10
pIC50 8.1 (IC50 8x10-9 M) [10]
SU11274 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 8.0 pIC50 44
pIC50 8.0 (IC50 1x10-8 M) [44]
Description: Assay used a GST fusion with the cytoplasmic domain of human Met.
compound 27 [PMID: 21123062] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 8.0 pIC50 45
pIC50 8.0 (IC50 1x10-8 M) [45]
golvatinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 34
pIC50 7.8 (IC50 1.4x10-8 M) [34]
Description: Measured as inhibition of c-MET phosphorylation in MKN45 cells
compound 19a [PMID: 30503936] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 38
pIC50 7.8 (IC50 1.5x10-8 M) [38]
AM7 Small molecule or natural product Ligand has a PDB structure Hs Inhibition 7.8 pIC50 3
pIC50 7.8 (IC50 1.7x10-8 M) [3]
ningetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pIC50 47
pIC50 7.7 (IC50 1.9x10-8 M) [47]
sitravatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.7 pIC50 36
pIC50 7.7 (IC50 2x10-8 M) [36]
Description: In a biochemical enzyme activity assay.
compound R-16 [PMID: 21967808] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.6 pIC50 31
pIC50 7.6 (IC50 2.4x10-8 M) [31]
glesatinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.5 pIC50 12
pIC50 7.5 (IC50 2.9x10-8 M) [12]
compound 16 [PMID: 18945615] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.1 pIC50 40
pIC50 7.1 (IC50 8.5x10-8 M) [40]
compound 8i [PMID: 22765894] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 6.3 pIC50 50
pIC50 6.3 (IC50 4.63x10-7 M) [50]
RIPK3 inhibitor 18 Small molecule or natural product Click here for species-specific activity table Immunopharmacology Ligand Hs Inhibition 6.0 pIC50 20
pIC50 6.0 (IC50 1.1x10-6 M) [20]
alectinib Small molecule or natural product Approved drug Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition <5.3 pIC50 25
pIC50 <5.3 (IC50 >5x10-6 M) [25]
vebreltinib Small molecule or natural product Hs Inhibition - - 21
[21]
Description: PLB-1001 inhibited MET activity by 95% in a LANCE enzyme assay
Inhibitor Comments
Tepotinib was shown to have an IC50 of <1nM in an in vitro study with recombinant human MET [16]. Tanespimycin is reported as a femtomolar inhibitor of MET-induced urokinase plasminogen activation (uPA) pathway [42].
Antibodies
Key to terms and symbols Click column headers to sort
Antibody Sp. Action Value Parameter Reference
amivantamab Peptide Approved drug Primary target of this compound Click here for species-specific activity table Hs Binding 10.4 pKd 23
pKd 10.4 (Kd 4x10-11 M) [23]
Description: Binding affinity determined by surface plasmon resonance.
emibetuzumab Peptide Primary target of this compound Hs Binding >10.0 pKd 14
pKd >10.0 (Kd <1x10-10 M) [14]
Description: binding constant for hMET extracellular domain measured using proprietary BIACore® technology
onartuzumab Peptide Primary target of this compound Hs Binding 8.4 pIC50 22,26
pIC50 8.4 (IC50 4.3x10-9 M) [22,26]
Other Binding Ligands
Key to terms and symbols Click column headers to sort
Ligand Sp. Action Value Parameter Reference
GE-137 Peptide Primary target of this compound Ligand is labelled Hs Binding 8.5 pKd 9
pKd 8.5 (Kd 3x10-9 M) [9]
Description: In vitro fluorescence polarization assay.
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: 15,46

Key to terms and symbols Click column headers to sort
Target used in screen: MET
Ligand Sp. Type Action Value Parameter
SGX-523 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.7 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 9.6 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.7 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 6.5 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 6.4 pKd
Target used in screen: MET(M1250T)
Ligand Sp. Type Action Value Parameter
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 9.3 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 9.2 pKd
SGX-523 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.1 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.2 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.0 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 6.7 pKd
tamatinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.6 pKd
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 6.3 pKd
Target used in screen: MET(Y1235D)
Ligand Sp. Type Action Value Parameter
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.1 pKd
PHA-665752 Small molecule or natural product Hs Inhibitor Inhibition 9.1 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.8 pKd
SGX-523 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
lestaurtinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.4 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.7 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.4 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 6.3 pKd
midostaurin Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 6.3 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: 2,19

Key to terms and symbols Click column headers to sort
Target used in screen: Met/c-MET
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
SU11274 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 1.2 2.0 0.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 32.7 4.0 1.0
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 40.4 3.0 0.0
K-252a Small molecule or natural product Hs Inhibitor Inhibition 53.2 6.0 13.0
PDGF RTK inhibitor Small molecule or natural product Hs Inhibitor Inhibition 60.4 28.0 4.0
GSK-3beta inhibitor I Small molecule or natural product Hs Inhibitor Inhibition 64.2 141.0 95.0
GSK-3 inhibitor IX Small molecule or natural product Hs Inhibitor Inhibition 70.0 118.0 97.0
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 70.9
erlotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 71.4
Cdk2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 73.2 122.0 85.0
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
The leucine-rich repeat (LRR)-containing protein InlB of Listeria monocytogenes is reported to mediate bacterial entry in to non-phagocytic host cells by binding to the MET proto-oncogene, receptor tyrosine kinase (MET, or hepatocyte growth factor receptor, HGFR) [4]. Tanespimycin (a potent inhibitor of MET [42], in addition to Hsp90) has reported efficacy against intracellular infection of non-phagocytic cells by L. monocytogenes [37].
Immuno Process Associations
Immuno Process:  Barrier integrity
GO Annotations:  Associated to 1 GO processes
GO:0035635 entry of bacterium into host cell TAS
Immuno Process:  Cytokine production & signalling
GO Annotations:  Associated to 3 GO processes
GO:0032675 regulation of interleukin-6 production IMP
GO:0071354 cellular response to interleukin-6 IEP
GO:0071635 negative regulation of transforming growth factor beta production IMP
Immuno Process:  Inflammation
GO Annotations:  Associated to 1 GO processes
GO:0006909 phagocytosis IBA
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Pediatric hepatocellular carcinoma
Disease Ontology: DOID:684
OMIM: 114550
Orphanet: ORPHA33402
Disease:  Renal cell carcinoma, papillary, 1; RCCP1
Synonyms: Hereditary papillary renal cell carcinoma [Orphanet: ORPHA47044]
Papillary renal cell carcinoma [Disease Ontology: DOID:4465]
Disease Ontology: DOID:4465
OMIM: 605074
Orphanet: ORPHA47044

References

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1. Ai J, Chen Y, Peng X, Ji Y, Xi Y, Shen Y, Yang X, Su Y, Sun Y, Gao Y et al.. (2018) Preclinical Evaluation of SCC244 (Glumetinib), a Novel, Potent, and Highly Selective Inhibitor of c-Met in MET-dependent Cancer Models. Mol Cancer Ther, 17 (4): 751-762. [PMID:29237805]

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. Bellon SF, Kaplan-Lefko P, Yang Y, Zhang Y, Moriguchi J, Rex K, Johnson CW, Rose PE, Long AM, O'Connor AB et al.. (2008) c-Met inhibitors with novel binding mode show activity against several hereditary papillary renal cell carcinoma-related mutations. J Biol Chem, 283 (5): 2675-83. [PMID:18055465]

4. Bierne H, Cossart P. (2002) InlB, a surface protein of Listeria monocytogenes that behaves as an invasin and a growth factor. J Cell Sci, 115 (Pt 17): 3357-67. [PMID:12154067]

5. Bladt F, Faden B, Friese-Hamim M, Knuehl C, Wilm C, Fittschen C, Grädler U, Meyring M, Dorsch D, Jaehrling F et al.. (2013) EMD 1214063 and EMD 1204831 constitute a new class of potent and highly selective c-Met inhibitors. Clin Cancer Res, 19 (11): 2941-51. [PMID:23553846]

6. Bode CM, Boezio AA, Albrecht BK, Bellon SF, Berry L, Broome MA, Choquette D, Dussault I, Lewis RT, Lin MH et al.. (2012) Discovery and optimization of a potent and selective triazolopyridinone series of c-Met inhibitors. Bioorg Med Chem Lett, 22 (12): 4089-93. [PMID:22595176]

7. Boezio AA, Berry L, Albrecht BK, Bauer D, Bellon SF, Bode C, Chen A, Choquette D, Dussault I, Fang M et al.. (2009) Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors. Bioorg Med Chem Lett, 19 (22): 6307-12. [PMID:19819693]

8. Buchanan SG, Hendle J, Lee PS, Smith CR, Bounaud PY, Jessen KA, Tang CM, Huser NH, Felce JD, Froning KJ et al.. (2009) SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol Cancer Ther, 8 (12): 3181-90. [PMID:19934279]

9. Burggraaf J, Kamerling IM, Gordon PB, Schrier L, de Kam ML, Kales AJ, Bendiksen R, Indrevoll B, Bjerke RM, Moestue SA et al.. (2015) Detection of colorectal polyps in humans using an intravenously administered fluorescent peptide targeted against c-Met. Nat Med, 21 (8): 955-61. [PMID:26168295]

10. Cho SY, Lee BH, Jung H, Yun CS, Ha JD, Kim HR, Chae CH, Lee JH, Seo HW, Oh KS. (2013) Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors. Bioorg Med Chem Lett, 23 (24): 6711-6. [PMID:24210504]

11. Christensen JG, Schreck R, Burrows J, Kuruganti P, Chan E, Le P, Chen J, Wang X, Ruslim L, Blake R et al.. (2003) A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo. Cancer Res, 63 (21): 7345-55. [PMID:14612533]

12. Claridge S, Raeppel F, Granger MC, Bernstein N, Saavedra O, Zhan L, Llewellyn D, Wahhab A, Deziel R, Rahil J et al.. (2008) Discovery of a novel and potent series of thieno[3,2-b]pyridine-based inhibitors of c-Met and VEGFR2 tyrosine kinases. Bioorg Med Chem Lett, 18 (9): 2793-8. [PMID:18434145]

13. Cui JJ, Tran-Dubé M, Shen H, Nambu M, Kung PP, Pairish M, Jia L, Meng J, Funk L, Botrous I et al.. (2011) Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK). J Med Chem, 54 (18): 6342-63. [PMID:21812414]

14. Davies J, Liu L, Lu J, Vaillancourt PE, Wortinger MA, Zeng W. c-Met antibodies. Patent number: US8217148. Assignee: Eli Lilly And Company. Priority date: 21/11/2008. Publication date: 10/07/2012.

15. 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]

16. Dorsch D, Schadt O, Stieber F, Meyring M, Grädler U, Bladt F, Friese-Hamim M, Knühl C, Pehl U, Blaukat A. (2015) Identification and optimization of pyridazinones as potent and selective c-Met kinase inhibitors. Bioorg Med Chem Lett, 25 (7): 1597-602. [PMID:25736998]

17. Flynn DL, Kaufman MD, Smith BD. (2016) Inhibition of tumor cell interactions with the microenvironment resulting in a reduction in tumor growth and disease progression. Patent number: WO2016061231. Assignee: Deciphera Pharmaceuticals, Llc. Priority date: 14/10/2014. Publication date: 21/04/2016.

18. Fujita H, Miyadera K, Kato M, Fujioka Y, Ochiiwa H, Huang J, Ito K, Aoyagi Y, Takenaka T, Suzuki T et al.. (2013) The novel VEGF receptor/MET-targeted kinase inhibitor TAS-115 has marked in vivo antitumor properties and a favorable tolerability profile. Mol Cancer Ther, 12 (12): 2685-96. [PMID:24140932]

19. 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]

20. Hart AC, Abell L, Guo J, Mertzman ME, Padmanabha R, Macor JE, Chaudhry C, Lu H, O'Malley K, Shaw PJ et al.. (2019) Identification of RIPK3 Type II Inhibitors Using High-Throughput Mechanistic Studies in Hit Triage. ACS Med Chem Lett, Article ASAP. DOI: 10.1021/acsmedchemlett.9b00065

21. Hu H, Mu Q, Bao Z, Chen Y, Liu Y, Chen J, Wang K, Wang Z, Nam Y, Jiang B et al.. (2018) Mutational Landscape of Secondary Glioblastoma Guides MET-Targeted Trial in Brain Tumor. Cell, 175 (6): 1665-1678.e18. [PMID:30343896]

22. Huang A, Schwall R, Yansura D. (2005) Monovalent antibody fragments useful as therapeutics. Patent number: US20050227324 A1. Assignee: Genentech, Inc.. Priority date: 19/12/2003. Publication date: 13/10/2005.

23. Jarantow SW, Bushey BS, Pardinas JR, Boakye K, Lacy ER, Sanders R, Sepulveda MA, Moores SL, Chiu ML. (2015) Impact of Cell-surface Antigen Expression on Target Engagement and Function of an Epidermal Growth Factor Receptor × c-MET Bispecific Antibody. J Biol Chem, 290 (41): 24689-704. [PMID:26260789]

24. Jia H, Dai G, Weng J, Zhang Z, Wang Q, Zhou F, Jiao L, Cui Y, Ren Y, Fan S et al.. (2014) Discovery of (S)-1-(1-(Imidazo[1,2-a]pyridin-6-yl)ethyl)-6-(1-methyl-1H-pyrazol-4-yl)-1H-[1,2,3]triazolo[4,5-b]pyrazine (volitinib) as a highly potent and selective mesenchymal-epithelial transition factor (c-Met) inhibitor in clinical development for treatment of cancer. J Med Chem, 57 (18): 7577-89. [PMID:25148209]

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How to cite this page

Type X RTKs: HGF (hepatocyte growth factor) receptor family: MET proto-oncogene, receptor tyrosine kinase. Last modified on 12/08/2021. Accessed on 02/12/2021. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetoimmunopharmacology.org/GRAC/ObjectDisplayForward?objectId=1815.