ArticleOncotarget2016
PIM kinases as therapeutic targets against advanced melanoma.
Article in Oncotarget, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 21 citations in OpenAlex.
- PIM1 kinase and its diverse substrate in solid tumors.Cell communication and signaling : CCS · 2024Review
- Polyamine and EIF5A hypusination downstream of c-Myc confers targeted therapy resistance in BRAF mutant melanoma.Molecular cancer · 2024Article
- Epithelial-mesenchymal transition interaction with CD8+ T cell, dendritic cell and immune checkpoints in the development of melanoma.Cancer biomarkers : section A of Disease markers · 2022Article
- BRAF inhibition curtails IFN-gamma-inducible PD-L1 expression and upregulates the immunoregulatory protein galectin-1 in melanoma cells.Molecular oncology · 2020Article
- Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials.Science translational medicine · 2019Article
- BRAF Targeting Sensitizes Resistant Melanoma to Cytotoxic T Cells.Clinical cancer research : an official journal of the American Association for Cancer Research · 2019Article
- Human melanoma brain metastases cell line MUG-Mel1, isolated clones and their detailed characterization.Scientific reports · 2019Article
- Acetylsalicylic Acid Governs the Effect of Sorafenib inClinical cancer research : an official journal of the American Association for Cancer Research · 2018Article
- Ginsenoside G-Rh2 synergizes with SMI-4a in anti-melanoma activity through autophagic cell death.Chinese medicine · 2018Article
- Review
- HistoneH3 demethylase JMJD2A promotes growth of liver cancer cells through up-regulating miR372.Oncotarget · 2017Article
- High-content screen using zebrafish (Danio rerio) embryos identifies a novel kinase activator and inhibitor.Bioorganic & medicinal chemistry letters · 2017Article
Corrections and comments
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Authors and funding
21 authors at 5 institutions in 2 countries.
Funding
Abstract
Therapeutic strategies for the treatment of metastatic melanoma show encouraging results in the clinic; however, not all patients respond equally and tumor resistance still poses a challenge. To identify novel therapeutic targets for melanoma, we screened a panel of structurally diverse organometallic inhibitors against human-derived normal and melanoma cells. We observed that a compound that targets PIM kinases (a family of Ser/Thr kinases) preferentially inhibited melanoma cell proliferation, invasion, and viability in adherent and three-dimensional (3D) melanoma models. Assessment of tumor tissue from melanoma patients showed that PIM kinases are expressed in pre- and post-treatment tumors, suggesting PIM kinases as promising targets in the clinic. Using knockdown studies, we showed that PIM1 contributes to melanoma cell proliferation and tumor growth in vivo; however, the presence of PIM2 and PIM3 could also influence the outcome. The inhibition of all PIM isoforms using SGI-1776 (a clinically-available PIM inhibitor) reduced melanoma proliferation and survival in preclinical models of melanoma. This was potentiated in the presence of the BRAF inhibitor PLX4720 and in the presence of PI3K inhibitors. Our findings suggest that PIM inhibitors provide promising additions to the targeted therapies available to melanoma patients.
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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 OpenQuestion graph.