Target Information
Target General Information | Top | |||||
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Target ID |
T40474
(Former ID: TTDC00110)
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Target Name |
Proto-oncogene c-Met (MET)
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Synonyms |
Tyrosine-protein kinase Met; Scatter factor receptor; SF receptor; Met proto-oncogene tyrosine kinase; Hepatocyte growth factor receptor; HGF/SF receptor; HGF-SF receptor; HGF receptor; C-met; C-Met receptor tyrosine kinase
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Gene Name |
MET
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Target Type |
Successful target
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[1] | ||||
Disease | [+] 3 Target-related Diseases | + | ||||
1 | Lung cancer [ICD-11: 2C25] | |||||
2 | Non-small cell lung cancer [ICD-11: 2C25] | |||||
3 | Thyroid cancer [ICD-11: 2D10] | |||||
Function |
Regulates many physiological processes including proliferation, scattering, morphogenesis and survival. Ligand binding at the cell surface induces autophosphorylation of MET on its intracellular domain that provides docking sites for downstream signaling molecules. Following activation by ligand, interacts with the PI3-kinase subunit PIK3R1, PLCG1, SRC, GRB2, STAT3 or the adapter GAB1. Recruitment of these downstream effectors by MET leads to the activation of several signaling cascades including the RAS-ERK, PI3 kinase-AKT, or PLCgamma-PKC. The RAS-ERK activation is associated with the morphogenetic effects while PI3K/AKT coordinates prosurvival effects. During embryonic development, MET signaling plays a role in gastrulation, development and migration of muscles and neuronal precursors, angiogenesis and kidney formation. In adults, participates in wound healing as well as organ regeneration and tissue remodeling. Promotes also differentiation and proliferation of hematopoietic cells. May regulate cortical bone osteogenesis. Receptor tyrosine kinase that transduces signals from the extracellular matrix into the cytoplasm by binding to hepatocyte growth factor/HGF ligand.
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BioChemical Class |
Kinase
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UniProt ID | ||||||
EC Number |
EC 2.7.10.1
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Sequence |
MKAPAVLAPGILVLLFTLVQRSNGECKEALAKSEMNVNMKYQLPNFTAETPIQNVILHEH
HIFLGATNYIYVLNEEDLQKVAEYKTGPVLEHPDCFPCQDCSSKANLSGGVWKDNINMAL VVDTYYDDQLISCGSVNRGTCQRHVFPHNHTADIQSEVHCIFSPQIEEPSQCPDCVVSAL GAKVLSSVKDRFINFFVGNTINSSYFPDHPLHSISVRRLKETKDGFMFLTDQSYIDVLPE FRDSYPIKYVHAFESNNFIYFLTVQRETLDAQTFHTRIIRFCSINSGLHSYMEMPLECIL TEKRKKRSTKKEVFNILQAAYVSKPGAQLARQIGASLNDDILFGVFAQSKPDSAEPMDRS AMCAFPIKYVNDFFNKIVNKNNVRCLQHFYGPNHEHCFNRTLLRNSSGCEARRDEYRTEF TTALQRVDLFMGQFSEVLLTSISTFIKGDLTIANLGTSEGRFMQVVVSRSGPSTPHVNFL LDSHPVSPEVIVEHTLNQNGYTLVITGKKITKIPLNGLGCRHFQSCSQCLSAPPFVQCGW CHDKCVRSEECLSGTWTQQICLPAIYKVFPNSAPLEGGTRLTICGWDFGFRRNNKFDLKK TRVLLGNESCTLTLSESTMNTLKCTVGPAMNKHFNMSIIISNGHGTTQYSTFSYVDPVIT SISPKYGPMAGGTLLTLTGNYLNSGNSRHISIGGKTCTLKSVSNSILECYTPAQTISTEF AVKLKIDLANRETSIFSYREDPIVYEIHPTKSFISGGSTITGVGKNLNSVSVPRMVINVH EAGRNFTVACQHRSNSEIICCTTPSLQQLNLQLPLKTKAFFMLDGILSKYFDLIYVHNPV FKPFEKPVMISMGNENVLEIKGNDIDPEAVKGEVLKVGNKSCENIHLHSEAVLCTVPNDL LKLNSELNIEWKQAISSTVLGKVIVQPDQNFTGLIAGVVSISTALLLLLGFFLWLKKRKQ IKDLGSELVRYDARVHTPHLDRLVSARSVSPTTEMVSNESVDYRATFPEDQFPNSSQNGS CRQVQYPLTDMSPILTSGDSDISSPLLQNTVHIDLSALNPELVQAVQHVVIGPSSLIVHF NEVIGRGHFGCVYHGTLLDNDGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVL SLLGICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKF VHRDLAARNCMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESLQTQKF TTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVMLKCW HPKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATYVNVKCVAPYPSLLSSEDNADDEVD TRPASFWETS Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | AlphaFold | ||||
HIT2.0 ID | T92AMR |
Drugs and Modes of Action | Top | |||||
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Approved Drug(s) | [+] 4 Approved Drugs | + | ||||
1 | Cabozantinib | Drug Info | Approved | Thyroid cancer | [2], [3] | |
2 | Capmatinib | Drug Info | Approved | Non-small-cell lung cancer | [4] | |
3 | Crizotinib | Drug Info | Approved | Non-small-cell lung cancer | [5], [6] | |
4 | Tepotinib | Drug Info | Approved | Non-small cell lung cancer | [7] | |
Clinical Trial Drug(s) | [+] 41 Clinical Trial Drugs | + | ||||
1 | Amivantamab | Drug Info | Phase 3 | Non-small-cell lung cancer | [8] | |
2 | Beperminogene perplasmid | Drug Info | Phase 3 | Heart disease | [9] | |
3 | RG3638 | Drug Info | Phase 3 | Non-small-cell lung cancer | [10] | |
4 | Savolitinib | Drug Info | Phase 3 | Renal cell carcinoma | [11] | |
5 | Tivantinib | Drug Info | Phase 3 | Solid tumour/cancer | [12], [13] | |
6 | MGCD516 | Drug Info | Phase 2/3 | Solid tumour/cancer | [14] | |
7 | AMG 208 | Drug Info | Phase 2 | Solid tumour/cancer | [15] | |
8 | AMG 337 | Drug Info | Phase 2 | Solid tumour/cancer | [16] | |
9 | APL-101 | Drug Info | Phase 2 | Non-small cell lung cancer | [17] | |
10 | CMX-2043 | Drug Info | Phase 2 | Myocardial reperfusion injury | [18] | |
11 | Emibetuzumab | Drug Info | Phase 2 | Solid tumour/cancer | [19] | |
12 | HM-5016504 | Drug Info | Phase 2 | Solid tumour/cancer | [20] | |
13 | LY-2875358 | Drug Info | Phase 2 | Solid tumour/cancer | [21] | |
14 | LY2801653 | Drug Info | Phase 2 | Solid tumour/cancer | [22] | |
15 | SAR-125844 | Drug Info | Phase 2 | Solid tumour/cancer | [23] | |
16 | Telisotuzumab vedotin | Drug Info | Phase 2 | Non-small-cell lung cancer | [24] | |
17 | XL880 | Drug Info | Phase 2 | Squamous head and neck cell carcinom | [25], [26] | |
18 | Anti-C-met CAR-T cells | Drug Info | Phase 1/2 | Colorectal cancer | [27] | |
19 | ChronSeal | Drug Info | Phase 1/2 | Fibrosis | [28] | |
20 | MK-2461 | Drug Info | Phase 1/2 | Alzheimer disease | [29] | |
21 | Sym015 | Drug Info | Phase 1/2 | Solid tumour/cancer | [11], [19] | |
22 | ABBV-399 | Drug Info | Phase 1 | Solid tumour/cancer | [30] | |
23 | ABT-700 | Drug Info | Phase 1 | Advanced solid tumour | [31] | |
24 | Altiratinib | Drug Info | Phase 1 | Solid tumour/cancer | [32] | |
25 | Autologous T Cells Expressing MET scFv CAR | Drug Info | Phase 1 | Melanoma | [33] | |
26 | BPI-9016 M | Drug Info | Phase 1 | Solid tumour/cancer | [34] | |
27 | C-Met/PD-L1 CAR-T Cell | Drug Info | Phase 1 | Hepatocellular carcinoma | [35] | |
28 | CBT-101 | Drug Info | Phase 1 | Solid tumour/cancer | [11] | |
29 | E-7050 | Drug Info | Phase 1 | Head and neck cancer | [36], [37] | |
30 | EMD-1204831 | Drug Info | Phase 1 | Solid tumour/cancer | [38] | |
31 | Hepapoietin | Drug Info | Phase 1 | Liver disease | [39] | |
32 | JNJ-38877605 | Drug Info | Phase 1 | Solid tumour/cancer | [40] | |
33 | LY3164530 | Drug Info | Phase 1 | Advanced cancer | [41] | |
34 | MK-8033 | Drug Info | Phase 1 | Solid tumour/cancer | [42] | |
35 | PF-4217903 | Drug Info | Phase 1 | Solid tumour/cancer | [43] | |
36 | REGN5093 | Drug Info | Phase 1 | Non-small-cell lung cancer | [44] | |
37 | RXDX-106 | Drug Info | Phase 1 | Solid tumour/cancer | [45] | |
38 | SGX523 | Drug Info | Phase 1 | Solid tumour/cancer | [46], [47] | |
39 | TPX-0022 | Drug Info | Phase 1 | Solid tumour/cancer | [48] | |
40 | TR1801-ADC | Drug Info | Phase 1 | Solid tumour/cancer | [49] | |
41 | XL092 | Drug Info | Phase 1 | Solid tumour/cancer | [50] | |
Preclinical Drug(s) | [+] 2 Preclinical Drugs | + | ||||
1 | Mteron-F1 | Drug Info | Preclinical | Mucositis | [51] | |
2 | NPS-1034 | Drug Info | Preclinical | Solid tumour/cancer | [52] | |
Mode of Action | [+] 5 Modes of Action | + | ||||
Inhibitor | [+] 49 Inhibitor drugs | + | ||||
1 | Cabozantinib | Drug Info | [3], [53] | |||
2 | Amivantamab | Drug Info | [54] | |||
3 | Savolitinib | Drug Info | [11] | |||
4 | Tivantinib | Drug Info | [12] | |||
5 | MGCD516 | Drug Info | [56] | |||
6 | MGCD516 | Drug Info | [57] | |||
7 | APL-101 | Drug Info | [60] | |||
8 | Emibetuzumab | Drug Info | [19] | |||
9 | HM-5016504 | Drug Info | [56] | |||
10 | SAR-125844 | Drug Info | [66] | |||
11 | BMS-777607 | Drug Info | [69] | |||
12 | ChronSeal | Drug Info | [70] | |||
13 | MK-2461 | Drug Info | [29] | |||
14 | Sym015 | Drug Info | [11] | |||
15 | ABBV-399 | Drug Info | [19] | |||
16 | Altiratinib | Drug Info | [53], [72] | |||
17 | BPI-9016 M | Drug Info | [73] | |||
18 | CBT-101 | Drug Info | [11] | |||
19 | EMD-1204831 | Drug Info | [75] | |||
20 | Hepapoietin | Drug Info | [76] | |||
21 | JNJ-38877605 | Drug Info | [77] | |||
22 | MK-8033 | Drug Info | [79] | |||
23 | PF-4217903 | Drug Info | [80] | |||
24 | REGN5093 | Drug Info | [81] | |||
25 | RXDX-106 | Drug Info | [82] | |||
26 | SGX523 | Drug Info | [83] | |||
27 | TPX-0022 | Drug Info | [84] | |||
28 | XL092 | Drug Info | [86] | |||
29 | NPS-1034 | Drug Info | [87] | |||
30 | 1-(2-nitrophenethyl)-1H-pyrrolo[3,2-b]pyridine | Drug Info | [88] | |||
31 | 1-(phenylsulfonyl)-1H-pyrrolo[3,2-b]pyridine | Drug Info | [88] | |||
32 | 1-benzyl-1H-pyrrolo[3,2-b]pyridine | Drug Info | [88] | |||
33 | 3-(phenylsulfonyl)-1H-pyrrolo[2,3-b]pyridine | Drug Info | [88] | |||
34 | AM7 | Drug Info | [89] | |||
35 | Anti-cMET mab | Drug Info | [56] | |||
36 | APS-3010 | Drug Info | [56] | |||
37 | BAY-85-3474 | Drug Info | [56] | |||
38 | BMS-536924 | Drug Info | [90] | |||
39 | CMET Avimer polypeptides | Drug Info | [56] | |||
40 | DP-3590 | Drug Info | [56] | |||
41 | PF-00614435 | Drug Info | [56] | |||
42 | PHA-665752 | Drug Info | [56] | |||
43 | PMID21123062C27 | Drug Info | [92] | |||
44 | PMID21967808CR-16 | Drug Info | [93] | |||
45 | PMID24210504C1o | Drug Info | [94] | |||
46 | PRS-110 | Drug Info | [56] | |||
47 | RP-1040 | Drug Info | [56] | |||
48 | SU11274 | Drug Info | [95] | |||
49 | TP-801 | Drug Info | [56] | |||
Modulator | [+] 14 Modulator drugs | + | ||||
1 | Capmatinib | Drug Info | [4] | |||
2 | Crizotinib | Drug Info | [1] | |||
3 | Tepotinib | Drug Info | [7] | |||
4 | Beperminogene perplasmid | Drug Info | [55] | |||
5 | RG3638 | Drug Info | [56] | |||
6 | AMG 208 | Drug Info | [58] | |||
7 | AMG 337 | Drug Info | [59] | |||
8 | CMX-2043 | Drug Info | [61] | |||
9 | LY2801653 | Drug Info | [64], [65] | |||
10 | XL880 | Drug Info | [68] | |||
11 | ABT-700 | Drug Info | [71] | |||
12 | E-7050 | Drug Info | [74] | |||
13 | LY3164530 | Drug Info | [78] | |||
14 | GE-137 | Drug Info | [91] | |||
CAR-T-Cell-Therapy | [+] 2 CAR-T-Cell-Therapy drugs | + | ||||
1 | Anti-C-met CAR-T cells | Drug Info | [27] | |||
2 | Autologous T Cells Expressing MET scFv CAR | Drug Info | [33] | |||
CAR-T-Cell-Therapy(Dual specific) | [+] 1 CAR-T-Cell-Therapy(Dual specific) drugs | + | ||||
1 | C-Met/PD-L1 CAR-T Cell | Drug Info | [35] | |||
Stimulator | [+] 1 Stimulator drugs | + | ||||
1 | Mteron-F1 | Drug Info | [51] |
Chemical Structure based Activity Landscape of Target | Top |
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Drug Property Profile of Target | Top | |
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(1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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(5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five |
Co-Targets | Top | |||||
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Co-Targets |
Target Poor or Non Binders | Top | |||||
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Target Poor or Non Binders |
Target Regulators | Top | |||||
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Target-regulating microRNAs | ||||||
Target-interacting Proteins |
Target Profiles in Patients | Top | |||||
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Target Expression Profile (TEP) |
Target-Related Models and Studies | Top | |||||
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Target Validation |
References | Top | |||||
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REF 1 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | |||||
REF 2 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5887). | |||||
REF 3 | Clinical pipeline report, company report or official report of Exelixis (2011). | |||||
REF 4 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020 | |||||
REF 5 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4903). | |||||
REF 6 | 2011 FDA drug approvals. Nat Rev Drug Discov. 2012 Feb 1;11(2):91-4. | |||||
REF 7 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2021 | |||||
REF 8 | ClinicalTrials.gov (NCT04538664) A Study of Combination Amivantamab and Carboplatin-Pemetrexed Therapy, Compared With Carboplatin-Pemetrexed, in Participants With Advanced or Metastatic Non-Small Cell Lung Cancer Characterized by Epidermal Growth Factor Receptor (EGFR) Exon 20 Insertions (PAPILLON). U.S. National Institutes of Health. | |||||
REF 9 | ClinicalTrials.gov (NCT02144610) Safety and Efficacy of Subjects With Critical Limb Ischemia. U.S. National Institutes of Health. | |||||
REF 10 | ClinicalTrials.gov (NCT02488330) An Extension Study of Onartuzumab in Patients With Solid Tumors on Study Treatment Previously Enrolled in a Company Sponsored Study. | |||||
REF 11 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 12 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7948). | |||||
REF 13 | A phase II trial of a selective c-Met inhibitor tivantinib (ARQ 197) monotherapy as a second- or third-line therapy in the patients with metastatic gastric cancer. Invest New Drugs. 2014 Apr;32(2):355-61. | |||||
REF 14 | ClinicalTrials.gov (NCT04887870) Study of Sitravatinib With or Without Other Anticancer Therapies Receiving Clinical Benefit From Parent Study. U.S. National Institutes of Health. | |||||
REF 15 | ClinicalTrials.gov (NCT02420587) AMG 208 Tumor Microenvironment in Metastatic Castration Resistant Prostate Cancer (mCRPC). U.S. National Institutes of Health. | |||||
REF 16 | ClinicalTrials.gov (NCT02016534) Phase 2 Study of AMG 337 in MET Amplified Gastric/Esophageal Adenocarcinoma or Other Solid Tumors. U.S. National Institutes of Health. | |||||
REF 17 | ClinicalTrials.gov (NCT04258033) A Study of PLB1001 in Non-small Cell Lung Cancer With c-Met Dysregulation. U.S. National Institutes of Health. | |||||
REF 18 | ClinicalTrials.gov (NCT02103959) Safety and Efficacy of CMX-2043 for Protection of the Heart and Kidneys in Subjects Undergoing Coronary Angiography. U.S. National Institutes of Health. | |||||
REF 19 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 20 | ClinicalTrials.gov (NCT02127710) A Phase II Trial to Evaluate the Efficacy of AZD6094 (HMPL-504) in Patients With Papillary Renal Cell Carcinoma (PRCC). U.S. National Institutes of Health. | |||||
REF 21 | ClinicalTrials.gov (NCT01900652) A Study of LY2875358 in Non Small Cell Lung Cancer (NSCLC) Participants. U.S. National Institutes of Health. | |||||
REF 22 | ClinicalTrials.gov (NCT01285037) A Study of LY2801653 in Advanced Cancer. U.S. National Institutes of Health. | |||||
REF 23 | ClinicalTrials.gov (NCT02435121) A Study Assessing Efficacy and Safety of SAR125844 in NSCLC Patients With MET Amplification. U.S. National Institutes of Health. | |||||
REF 24 | ClinicalTrials.gov (NCT03539536) Study of Telisotuzumab Vedotin (ABBV-399) in Participants With Previously Treated c-Met+ Non-Small Cell Lung Cancer. U.S. National Institutes of Health. | |||||
REF 25 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5679). | |||||
REF 26 | Clinical pipeline report, company report or official report of Exelixis (2011). | |||||
REF 27 | ClinicalTrials.gov (NCT03638206) Autologous CAR-T/TCR-T Cell Immunotherapy for Malignancies | |||||
REF 28 | ClinicalTrials.gov (NCT00797706) Phase I/II Dose Ranging CHRONSEAL Study in Venous Leg Ulcers. U.S. National Institutes of Health. | |||||
REF 29 | MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor. Cancer Res. 2010 Feb 15;70(4):1524-33. | |||||
REF 30 | ClinicalTrials.gov (NCT02099058) A Phase 1/1b Study With ABBV-399, an Antibody Drug Conjugate, in Subjects With Advanced Solid Cancer Tumors. U.S. National Institutes of Health. | |||||
REF 31 | ClinicalTrials.gov (NCT01472016) Study of ABT-700 in Subjects With Advanced Solid Tumors. U.S. National Institutes of Health. | |||||
REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800040094) | |||||
REF 33 | ClinicalTrials.gov (NCT03060356) Autologous T Cells Expressing MET scFv CAR (RNA CART-cMET) | |||||
REF 34 | ClinicalTrials.gov (NCT02478866) Safety and Pharmacokinetics of BPI-9016M in Patients With Advanced Solid Tumors. U.S. National Institutes of Health. | |||||
REF 35 | ClinicalTrials.gov (NCT03672305) Clinical Study on the Efficacy and Safety of c-Met/PD-L1 CAR-T Cell Injection in the Treatment of HCC | |||||
REF 36 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7956). | |||||
REF 37 | ClinicalTrials.gov (NCT02533102) Pharmacokinetics and Food Effect of Single Oral Dose of E7050 in Healthy Volunteers. | |||||
REF 38 | ClinicalTrials.gov (NCT01110083) First-in-Man, Dose-escalation Trial of c-Met Kinase Inhibitor EMD 1204831 in Subjects With Advanced Solid Tumors. U.S. National Institutes of Health. | |||||
REF 39 | Pharmacokinetics and biochemical effects of hepapoietin in patients with chronic liver disease. Aliment Pharmacol Ther. 2002 Feb;16(2):235-42. | |||||
REF 40 | ClinicalTrials.gov (NCT00651365) A Safety and Dose-finding Study of JNJ-38877605 in Patients With Advanced or Refractory Solid Tumors.. U.S. National Institutes of Health. | |||||
REF 41 | ClinicalTrials.gov (NCT02221882) A Study of LY3164530 in Participants With Cancer | |||||
REF 42 | ClinicalTrials.gov (NCT00559182) A Study of MK-8033 in Patients With Advanced Solid Tumors (MK-8033-001). U.S. National Institutes of Health. | |||||
REF 43 | ClinicalTrials.gov (NCT00706355) A Study of PF-04217903 in Patients With Advanced Cancer. U.S. National Institutes of Health. | |||||
REF 44 | ClinicalTrials.gov (NCT04077099) REGN5093 in Patients With MET-Altered Advanced Non-Small Cell Lung Cancer. U.S. National Institutes of Health. | |||||
REF 45 | ClinicalTrials.gov (NCT03454243) Oral Immunomodulatory Tyrosine Kinase Inhibitor in Patients With Locally Advanced or Metastatic Solid Tumors (TITAN). U.S. National Institutes of Health. | |||||
REF 46 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5709). | |||||
REF 47 | ClinicalTrials.gov (NCT00607399) Safety Study of SGX523, a Small Molecule Met Inhibitor, to Treat Solid Tumors. U.S. National Institutes of Health. | |||||
REF 48 | ClinicalTrials.gov (NCT03993873) Phase 1 Study of TPX-0022, a MET/CSF1R/SRC Inhibitor, in Patients With Advanced Solid Tumors Harboring Genetic Alterations in MET. U.S. National Institutes of Health. | |||||
REF 49 | ClinicalTrials.gov (NCT03859752) TR1801-ADC in Patients With Tumors That Express c-Met. U.S. National Institutes of Health. | |||||
REF 50 | ClinicalTrials.gov (NCT03845166) A Study of XL092 as Single-Agent and Combination Therapy in Subjects With Solid Tumors. U.S. National Institutes of Health. | |||||
REF 51 | Emerging drugs for chemotherapy-induced mucositis. Expert Opin Emerg Drugs. 2008 Sep;13(3):511-22. | |||||
REF 52 | AXL receptor tyrosine kinase as a promising anti-cancer approach: functions, molecular mechanisms and clinical applications. Mol Cancer. 2019 Nov 4;18(1):153. | |||||
REF 53 | Tropomyosin receptor kinase inhibitors: an updated patent review for 2010-2016 - Part I.Expert Opin Ther Pat. 2017 Jun;27(6):733-751. | |||||
REF 54 | Antitumor Activity of Amivantamab (JNJ-61186372), an EGFR-MET Bispecific Antibody, in Diverse Models of EGFR Exon 20 Insertion-Driven NSCLC. Cancer Discov. 2020 Aug;10(8):1194-1209. | |||||
REF 55 | Beperminogene perplasmid for the treatment of critical limb ischemia. Expert Rev Cardiovasc Ther. 2014 Oct;12(10):1145-56. | |||||
REF 56 | URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1815). | |||||
REF 57 | Role and relevance of TrkB mutations and expression in non-small cell lung cancer. Clin Cancer Res. 2011 May 1;17(9):2638-45. | |||||
REF 58 | A first-in-human study of AMG 208, an oral MET inhibitor, in adult patients with advanced solid tumors. Oncotarget. 2015 Jul 30;6(21):18693-706. | |||||
REF 59 | J Clin Oncol 32:5s, 2014 (suppl; abstr 2508). | |||||
REF 60 | Clinical pipeline report, company report or official report of Apollomics. | |||||
REF 61 | Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA) | |||||
REF 62 | Clinical pipeline report, company report or official report of Eli Lilly. | |||||
REF 63 | LY2875358, a neutralizing and internalizing anti-MET bivalent antibody, inhibits HGF-dependent and HGF-independent MET activation and tumor growth. Clin Cancer Res. 2014 Dec 1;20(23):6059-70. | |||||
REF 64 | Clinical pipeline report, company report or official report of Eli Lilly. | |||||
REF 65 | LY2801653 is an orally bioavailable multi-kinase inhibitor with potent activity against MET, MST1R, and other oncoproteins, and displays anti-tumor activities in mouse xenograft models. Invest New Drugs. 2013 Aug;31(4):833-44. | |||||
REF 66 | The selective intravenous inhibitor of the MET tyrosine kinase SAR125844 inhibits tumor growth in MET-amplified cancer. Mol Cancer Ther. 2015 Feb;14(2):384-94. | |||||
REF 67 | Clinical pipeline report, company report or official report of AbbVie. | |||||
REF 68 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | |||||
REF 69 | Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607... J Med Chem. 2009 Mar 12;52(5):1251-4. | |||||
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REF 75 | 2012 ASCO Annual Meeting. | |||||
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REF 82 | National Cancer Institute Drug Dictionary (drug name RXDX106). | |||||
REF 83 | CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. | |||||
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REF 89 | c-Met inhibitors with novel binding mode show activity against several hereditary papillary renal cell carcinoma-related mutations. J Biol Chem. 2008 Feb 1;283(5):2675-83. | |||||
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REF 93 | Improvement in oral bioavailability of 2,4-diaminopyrimidine c-Met inhibitors by incorporation of a 3-amidobenzazepin-2-one group. Bioorg Med Chem. 2011 Nov 1;19(21):6274-84. | |||||
REF 94 | 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. 2013 Dec 15;23(24):6711-6. | |||||
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