Id: acc0923
Group: 2sens
Protein: MET
Gene Symbol: MET
Protein Id: P08581
Protein Name: MET_HUMAN
PTM: phosphorylation
Site: Tyr1234
Site Sequence: LARDMYDKEYYSVHNKTGAKL
Disease Category: Cancer
Disease: Lung Cancer
Disease Subtype: SCC
Disease Cellline: HCC366
Disease Info:
Drug: dasatinib
Drug Info: "Dasatinib is a tyrosine kinase inhibitor that targets BCR-ABL and SRC family kinases, used in the treatment of chronic myeloid leukemia (CML) and Philadelphia chromosome-positive acute lymphoblastic leukemia (Ph+ ALL), particularly in patients resistant or intolerant to prior therapy including imatinib."
Effect: inhibit
Effect Info: EGFR and MET phosphorylation render human lung SCC tissues intrinsically resistant to dasatinib.
Note:
Score: 5.0
Pubmed(PMID): 25348954
Sentence Index:
Sentence:

Sequence & Structure:

MKAPAVLAPGILVLLFTLVQRSNGECKEALAKSEMNVNMKYQLPNFTAETPIQNVILHEHHIFLGATNYIYVLNEEDLQKVAEYKTGPVLEHPDCFPCQDCSSKANLSGGVWKDNINMALVVDTYYDDQLISCGSVNRGTCQRHVFPHNHTADIQSEVHCIFSPQIEEPSQCPDCVVSALGAKVLSSVKDRFINFFVGNTINSSYFPDHPLHSISVRRLKETKDGFMFLTDQSYIDVLPEFRDSYPIKYVHAFESNNFIYFLTVQRETLDAQTFHTRIIRFCSINSGLHSYMEMPLECILTEKRKKRSTKKEVFNILQAAYVSKPGAQLARQIGASLNDDILFGVFAQSKPDSAEPMDRSAMCAFPIKYVNDFFNKIVNKNNVRCLQHFYGPNHEHCFNRTLLRNSSGCEARRDEYRTEFTTALQRVDLFMGQFSEVLLTSISTFIKGDLTIANLGTSEGRFMQVVVSRSGPSTPHVNFLLDSHPVSPEVIVEHTLNQNGYTLVITGKKITKIPLNGLGCRHFQSCSQCLSAPPFVQCGWCHDKCVRSEECLSGTWTQQICLPAIYKVFPNSAPLEGGTRLTICGWDFGFRRNNKFDLKKTRVLLGNESCTLTLSESTMNTLKCTVGPAMNKHFNMSIIISNGHGTTQYSTFSYVDPVITSISPKYGPMAGGTLLTLTGNYLNSGNSRHISIGGKTCTLKSVSNSILECYTPAQTISTEFAVKLKIDLANRETSIFSYREDPIVYEIHPTKSFISGGSTITGVGKNLNSVSVPRMVINVHEAGRNFTVACQHRSNSEIICCTTPSLQQLNLQLPLKTKAFFMLDGILSKYFDLIYVHNPVFKPFEKPVMISMGNENVLEIKGNDIDPEAVKGEVLKVGNKSCENIHLHSEAVLCTVPNDLLKLNSELNIEWKQAISSTVLGKVIVQPDQNFTGLIAGVVSISTALLLLLGFFLWLKKRKQIKDLGSELVRYDARVHTPHLDRLVSARSVSPTTEMVSNESVDYRATFPEDQFPNSSQNGSCRQVQYPLTDMSPILTSGDSDISSPLLQNTVHIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLDNDGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDLAARNCMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESLQTQKFTTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATYVNVKCVAPYPSLLSSEDNADDEVDTRPASFWETS

Select PDB:

Known Drugs:

source: Multi-Sources

(see table)

Target Drug name MOA Phase Status Disease Source
MET CABOZANTINIB S-MALATE Hepatocyte growth factor receptor inhibitor 4 - hepatocellular carcinoma EMA
MET CRIZOTINIB Hepatocyte growth factor receptor inhibitor 4 - diffuse large B-cell lymphoma DailyMed
MET CABOZANTINIB Hepatocyte growth factor receptor inhibitor 4 - neoplasm ATC
MET AMIVANTAMAB Hepatocyte growth factor receptor inhibitor 4 - neoplasm ATC
MET CAPMATINIB Hepatocyte growth factor receptor inhibitor 4 - neoplasm ATC
MET TEPOTINIB Hepatocyte growth factor receptor inhibitor 4 - neoplasm ATC
MET CRIZOTINIB Hepatocyte growth factor receptor inhibitor 4 - neoplasm ATC
MET CABOZANTINIB S-MALATE Hepatocyte growth factor receptor inhibitor 4 - renal cell carcinoma EMA
DailyMed
MET CABOZANTINIB S-MALATE Hepatocyte growth factor receptor inhibitor 4 - thyroid carcinoma DailyMed
MET CAPMATINIB HYDROCHLORIDE Hepatocyte growth factor receptor inhibitor 4 - non-small cell lung carcinoma EMA
FDA
DailyMed
MET CRIZOTINIB Hepatocyte growth factor receptor inhibitor 4 - non-small cell lung carcinoma EMA
DailyMed
MET CRIZOTINIB Hepatocyte growth factor receptor inhibitor 4 Terminated non-small cell lung carcinoma ClinicalTrials
MET CRIZOTINIB Hepatocyte growth factor receptor inhibitor 4 Active, not recruiting non-small cell lung carcinoma ClinicalTrials
MET AMIVANTAMAB Hepatocyte growth factor receptor inhibitor 4 - non-small cell lung carcinoma EMA
FDA
MET TEPOTINIB HYDROCHLORIDE Hepatocyte growth factor receptor inhibitor 4 - non-small cell lung carcinoma EMA
FDA
DailyMed
MET TIVANTINIB Hepatocyte growth factor receptor inhibitor 3 Completed hepatocellular carcinoma ClinicalTrials
MET CABOZANTINIB Hepatocyte growth factor receptor inhibitor 3 Active, not recruiting hepatocellular carcinoma ClinicalTrials
MET CABOZANTINIB Hepatocyte growth factor receptor inhibitor 3 Completed hepatocellular carcinoma ClinicalTrials
MET CRIZOTINIB Hepatocyte growth factor receptor inhibitor 3 Completed carcinoma ClinicalTrials
MET CRIZOTINIB Hepatocyte growth factor receptor inhibitor 3 Recruiting lung adenocarcinoma ClinicalTrials
MET CRIZOTINIB Hepatocyte growth factor receptor inhibitor 3 Recruiting neoplasm ClinicalTrials
MET ONARTUZUMAB Hepatocyte growth factor receptor antagonist 3 Completed neoplasm ClinicalTrials
MET CABOZANTINIB Hepatocyte growth factor receptor inhibitor 3 Active, not recruiting renal cell carcinoma ClinicalTrials
ClinicalTrials
ClinicalTrials
ClinicalTrials
MET CABOZANTINIB Hepatocyte growth factor receptor inhibitor 3 Terminated renal cell carcinoma ClinicalTrials
MET SAVOLITINIB Hepatocyte growth factor receptor inhibitor 3 Active, not recruiting renal cell carcinoma ClinicalTrials

Note: Only show clinically investigational or approved drugs with protein targets.

Protein Tractability:

source: Open Targets
Small molecule
Antibody
PROTAC
Other modalities
Approved Drug
Advanced Clinical
Phase 1 Clinical
Structure with Ligand
High-Quality Ligand
High-Quality Pocket
Med-Quality Pocket
Druggable Family
Approved Drug
Advanced Clinical
Phase 1 Clinical
UniProt loc high conf
GO CC high conf
UniProt loc med conf
UniProt SigP or TMHMM
GO CC med conf
Human Protein Atlas loc
Approved Drug
Advanced Clinical
Phase 1 Clinical
Literature
UniProt Ubiquitination
Database Ubiquitination
Half-life Data
Small Molecule Binder
Approved Drug
Advanced Clinical
Phase 1 Clinical

PTM Intensity:

source: CPTAC
MET-Tyr1234
Cancer Intensity
BRCA
COAD
HGSC
ccRCC
GBM
HNSC
LUAD
LUSC
non_ccRCC
PDAC
UCEC

PTM-Disease Association:

source: PTMD
Residue Position State Disease Class PMID
Y 1234 P Lung cancer/carcinoma Phosphorylation 23973484
Y 1234 U Prostate cancer Phosphorylation 33705609
Y 1234 U Bladder cancer Phosphorylation 17062641
Y 1234 U Hepatocellular carcinoma/hepatocarcinoma/hepatoma Phosphorylation 21455220

State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.

PTM-Drug Perturbation Response:

source: DecryptM

No data.

Function score:

source: funscoR

No data.

Cross Links: