ArticleOncogene2002
K252a inhibits the oncogenic properties of Met, the HGF receptor.
Article in Oncogene, 2002. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 45 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
45 citing papers in PubMed, 142 citations in OpenAlex.
- Article
- A novel c-Met/TRK inhibitor 1D228 efficiently inhibits tumor growth by targeting angiogenesis and tumor cell proliferation.Cell death & disease · 2023Article
- A selective c-Met and Trks inhibitor Indo5 suppresses hepatocellular carcinoma growth.Journal of experimental & clinical cancer research : CR · 2019Article
- Aging Increases Hippocampal DUSP2 by a Membrane Cholesterol Loss-Mediated RTK/p38MAPK Activation Mechanism.Frontiers in neurology · 2019Article
- Clinical significance of MET in gastric cancer.World journal of gastrointestinal oncology · 2015Review
- Knockdown of c-MET induced apoptosis in ABCB1-overexpressed multidrug-resistance cancer cell lines.Cancer gene therapy · 2015Article
- Met degradation by SAIT301, a Met monoclonal antibody, reduces the invasion and migration of nasopharyngeal cancer cells via inhibition of EGR-1 expression.Cell death & disease · 2014Article
- Article
- Targeting the epithelial to mesenchymal transition in glioblastoma: the emerging role of MET signaling.OncoTargets and therapy · 2014Review
- MET as a possible target for non-small-cell lung cancer.Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2013Review
- MET inhibitors in combination with other therapies in non-small cell lung cancer.Translational lung cancer research · 2012Review
- Murine double minute 2 regulates Hu antigen R stability in human liver and colon cancer through NEDDylation.Hepatology (Baltimore, Md.) · 2012Article
- K252a induces anoikis-sensitization with suppression of cellular migration in Epstein-Barr virus (EBV)--associated nasopharyngeal carcinoma cells.Investigational new drugs · 2012Article
- Graded activation of the MEK1/MT1-MMP axis determines renal epithelial cell tumor phenotype.Carcinogenesis · 2011Article
- Amelioration of central cardiovascular regulatory dysfunction by tropomyocin receptor kinase B in a mevinphos intoxication model of brain stem death.British journal of pharmacology · 2011Article
- More expressions of BDNF and TrkB in multiple hepatocellular carcinoma and anti-BDNF or K252a induced apoptosis, supressed invasion of HepG2 and HCCLM3 cells.Journal of experimental & clinical cancer research : CR · 2011Article
- AAK1 identified as an inhibitor of neuregulin-1/ErbB4-dependent neurotrophic factor signaling using integrative chemical genomics and proteomics.Chemistry & biology · 2011Article
- DNA triplex-mediated inhibition of MET leads to cell death and tumor regression in hepatoma.Cancer gene therapy · 2011Article
- Structural basis for selective small molecule kinase inhibition of activated c-Met.The Journal of biological chemistry · 2011Article
- Cell delivery of Met docking site peptides inhibit angiogenesis and vascular tumor growth.Oncogene · 2010Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The ATP analog K252a is a potent inhibitor for receptor tyrosine kinases of the Trk family. Here we show that nanomolar concentrations of K252a prevent HGF-mediated scattering in MLP-29 cells (30 nM), reduce Met-driven proliferation in GTL-16 gastric carcinoma cells (100 nM), and cause reversion in NIH3T3 fibroblasts transformed by the oncogenic form of the receptor, Tpr-Met (75 nM). K252a inhibits Met autophosphorylation in cultured cells and in immunoprecipitates and prevents activation of its downstream effectors MAPKinase and Akt. Interestingly, K252a seems to be more effective at inhibiting the mutated form of Met (M1268T) found in papillary carcinoma of the kidney than the wild type receptor. Pretreatment of both Tpr-Met-transformed NIH3T3 fibroblasts and of GTL-16 gastric carcinoma cells with K252a results in loss of their ability to form lung metastases in nude mice upon injection into the caudal vein. These observations suggest that K252a derivatives, which are active in vivo as anti-cancer drugs in models of Trk-driven malignancies, should also be effective for treatment of Met-mediated tumors.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.