Id: | acc3332 |
Group: | 2sens |
Protein: | c-Met |
Gene Symbol: | MET |
Protein Id: | P08581 |
Protein Name: | MET_HUMAN |
PTM: | phosphorylation |
Site: | Tyr1234 |
Site Sequence: | LARDMYDKEYYSVHNKTGAKL |
Disease Category: | Cancer |
Disease: | Prostate Cancer |
Disease Subtype: | |
Disease Cellline: | DU145 |
Disease Info: | |
Drug: | Isothiocyanatostilbenes |
Drug Info: | Isothiocyanatostilbenes are a class of chemical compounds that may have potential pharmacological activities. |
Effect: | modulate |
Effect Info: | "DIDS can inhibit and reverse c-Met phosphorylation, thereby suppressing cancer." |
Note: | |
Score: | 4.0 |
Pubmed(PMID): | 26543230 |
Sentence Index: | 26543230_3-4 |
Sentence: | "The research presented here demonstrates a particular class of compounds known as isothiocyanatostilbenes can act as c-Met inhibitors in multiple cancer cell lines. Specifically, we found that 4,4'-Diisothiocyanatostilbene-2,2'-disulfonic acid (DIDS) and 4,4'-Diisothiocyanatodihydrostilbene-2,2'-disulfonic acid (H2DIDS) had c-Met inhibitory effective doses in the low micromolar range while 4-acetamido-4'-isothiocyanatostilbene-2,2'-disulfonic acid (SITS) and 4,4'-dinitrostilbene-2, 2'-disulfonic acid (DNDS) exhibited IC50s 100 to 1000 fold higher." |
Sequence & Structure:
MKAPAVLAPGILVLLFTLVQRSNGECKEALAKSEMNVNMKYQLPNFTAETPIQNVILHEHHIFLGATNYIYVLNEEDLQKVAEYKTGPVLEHPDCFPCQDCSSKANLSGGVWKDNINMALVVDTYYDDQLISCGSVNRGTCQRHVFPHNHTADIQSEVHCIFSPQIEEPSQCPDCVVSALGAKVLSSVKDRFINFFVGNTINSSYFPDHPLHSISVRRLKETKDGFMFLTDQSYIDVLPEFRDSYPIKYVHAFESNNFIYFLTVQRETLDAQTFHTRIIRFCSINSGLHSYMEMPLECILTEKRKKRSTKKEVFNILQAAYVSKPGAQLARQIGASLNDDILFGVFAQSKPDSAEPMDRSAMCAFPIKYVNDFFNKIVNKNNVRCLQHFYGPNHEHCFNRTLLRNSSGCEARRDEYRTEFTTALQRVDLFMGQFSEVLLTSISTFIKGDLTIANLGTSEGRFMQVVVSRSGPSTPHVNFLLDSHPVSPEVIVEHTLNQNGYTLVITGKKITKIPLNGLGCRHFQSCSQCLSAPPFVQCGWCHDKCVRSEECLSGTWTQQICLPAIYKVFPNSAPLEGGTRLTICGWDFGFRRNNKFDLKKTRVLLGNESCTLTLSESTMNTLKCTVGPAMNKHFNMSIIISNGHGTTQYSTFSYVDPVITSISPKYGPMAGGTLLTLTGNYLNSGNSRHISIGGKTCTLKSVSNSILECYTPAQTISTEFAVKLKIDLANRETSIFSYREDPIVYEIHPTKSFISGGSTITGVGKNLNSVSVPRMVINVHEAGRNFTVACQHRSNSEIICCTTPSLQQLNLQLPLKTKAFFMLDGILSKYFDLIYVHNPVFKPFEKPVMISMGNENVLEIKGNDIDPEAVKGEVLKVGNKSCENIHLHSEAVLCTVPNDLLKLNSELNIEWKQAISSTVLGKVIVQPDQNFTGLIAGVVSISTALLLLLGFFLWLKKRKQIKDLGSELVRYDARVHTPHLDRLVSARSVSPTTEMVSNESVDYRATFPEDQFPNSSQNGSCRQVQYPLTDMSPILTSGDSDISSPLLQNTVHIDLSALNPELVQAVQHVVIGPSSLIVHFNEVIGRGHFGCVYHGTLLDNDGKKIHCAVKSLNRITDIGEVSQFLTEGIIMKDFSHPNVLSLLGICLRSEGSPLVVLPYMKHGDLRNFIRNETHNPTVKDLIGFGLQVAKGMKYLASKKFVHRDLAARNCMLDEKFTVKVADFGLARDMYDKEYYSVHNKTGAKLPVKWMALESLQTQKFTTKSDVWSFGVLLWELMTRGAPPYPDVNTFDITVYLLQGRRLLQPEYCPDPLYEVMLKCWHPKAEMRPSFSELVSRISAIFSTFIGEHYVHVNATYVNVKCVAPYPSLLSSEDNADDEVDTRPASFWETS
Select PDB:
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 TargetsPTM Intensity:
source: CPTACMET-Tyr1234 | |
---|---|
Cancer | Intensity |
BRCA | |
COAD | |
HGSC | |
ccRCC | |
GBM | |
HNSC | |
LUAD | |
LUSC | |
non_ccRCC | |
PDAC | |
UCEC |
PTM-Disease Association:
source: PTMDResidue | 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: DecryptMNo data.
Function score:
source: funscoRNo data.