ArticleOncogene2014
A chemical biology approach identifies AMPK as a modulator of melanoma oncogene MITF.
Article in Oncogene, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
What it found
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Who cites it
18 citing papers in PubMed, 30 citations in OpenAlex.
- Multi-omics and tumor immune microenvironment characterization of a prognostic model based on aging-related genes in melanoma.American journal of cancer research · 2024Article
- Istradefylline modulates purinergic enzymes and reduces malignancy-associated factors in B16F10 melanoma cells.Purinergic signalling · 2023Article
- Jeju Magma-Seawater Inhibits α-MSH-Induced Melanogenesis via CaMKKβ-AMPK Signaling Pathways in B16F10 Melanoma Cells.Marine drugs · 2020Article
- AMPK activation induced in pemetrexed-treated cells is associated with development of drug resistance independently of target enzyme expression.Molecular oncology · 2019Article
- Kazinol U inhibits melanogenesis through the inhibition of tyrosinase-related proteins via AMP kinase activation.British journal of pharmacology · 2019Article
- Functional Proteomics and Deep Network Interrogation Reveal a Complex Mechanism of Action of Midostaurin in Lung Cancer Cells.Molecular & cellular proteomics : MCP · 2018Article
- Dissecting the role of AMP-activated protein kinase in human diseases.Acta pharmaceutica Sinica. B · 2017Review
- A spatiotemporal hypothesis for the regulation, role, and targeting of AMPK in prostate cancer.Nature reviews. Urology · 2017Review
- Overcoming MITF-conferred drug resistance through dual AURKA/MAPK targeting in human melanoma cells.Cell death & disease · 2016Article
- Is 5´-AMP-Activated Protein Kinase Both Jekyll and Hyde in Bladder Cancer?International neurourology journal · 2015Review
- Targeting AMPK for cancer prevention and treatment.Oncotarget · 2015Review
- The double-edged sword of AMPK signaling in cancer and its therapeutic implications.Archives of pharmacal research · 2015Review
- Targeting a cell state common to triple-negative breast cancers.Molecular systems biology · 2015Article
- Identification of kinase inhibitor targets in the lung cancer microenvironment by chemical and phosphoproteomics.Molecular cancer therapeutics · 2014Article
- Inhibition of melanogenesis by the antidiabetic metformin.The Journal of investigative dermatology · 2014Article
- Loss of AMPKα1 expression is associated with poor survival in melanoma patients.The Journal of investigative dermatology · 2014Article
- Acid sphingomyelinase determines melanoma progression and metastatic behaviour via the microphtalmia-associated transcription factor signalling pathway.Cell death and differentiation · 2014Article
- 17-β Oestradiol prevents cardiovascular dysfunction in post-menopausal metabolic syndrome by affecting SIRT1/AMPK/H3 acetylation.British journal of pharmacology · 2013Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
11 authors at 3 institutions in 1 country.
Funding
Abstract
The microphthalmia-associated transcription factor (MITF) is indispensable for the viability of melanocytic cells, is an oncogene in melanoma and has a cell type-specific expression pattern. As the modulation of MITF activity by direct chemical targeting remains a challenge, we assessed a panel of drugs for their ability to downregulate MITF expression or activity by targeting its upstream modulators. We found that the multi-kinase inhibitors midostaurin and sunitinib downregulate MITF protein levels. To identify the target molecules shared by both the drugs in melanocytic cells, a chemical proteomic approach was applied and AMP-activated kinase (AMPK) was identified as the relevant target for the observed phenotype. RNA interference and chemical inhibition of AMPK led to a decrease in MITF protein levels. Reduction of MITF protein levels was the result of proteasomal degradation, which was preceded by enhanced phosphorylation of MITF mediated by ERK. As expected, downregulation of MITF protein levels by AMPK inhibition was associated with decreased viability. Together, these results identify AMPK as an important regulator for the maintenance of MITF protein levels in melanocytic cells.
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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 Socratic graph.