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Article
Open AccessPD 0332991, a selective cyclin D kinase 4/6 inhibitor, preferentially inhibits proliferation of luminal estrogen receptor-positive human breast cancer cell lines in vitro
Alterations in cell cycle regulators have been implicated in human malignancies including breast cancer. PD 0332991 is an orally active, highly selective inhibitor of the cyclin D kinases (CDK)4 and CDK6 with ...
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Article
RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)
Although clinical trials have shown that RAF inhibitors prolong the survival of patients with BRAF-mutant melanoma, resistance inevitably develops; resistance is shown here to be frequently mediated by the exp...
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Article
Open AccessAntitumor effects of the investigational selective MEK inhibitor TAK733 against cutaneous and uveal melanoma cell lines
TAK733 is a novel allosteric, non-ATP-binding, inhibitor of the BRAF substrates MEK-1/2.
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Article
Open AccessPET imaging to non-invasively study immune activation leading to antitumor responses with a 4-1BB agonistic antibody
Molecular imaging with positron emission tomography (PET) may allow the non-invasive study of the pharmacodynamic effects of agonistic monoclonal antibodies (mAb) to 4-1BB (CD137). 4-1BB is a member of the tum...
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Article
Open AccessEffects of AKT inhibitor therapy in response and resistance to BRAF inhibition in melanoma
The clinical use of BRAF inhibitors for treatment of metastatic melanoma is limited by the development of drug resistance. In this study we investigated whether co-targeting the MAPK and the PI3K-AKT pathway c...
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Article
Open AccessCombination of pan-RAF and MEK inhibitors in NRAS mutant melanoma
Approximately 20% of melanomas contain a mutation in NRAS. However no direct inhibitor of NRAS is available. One of the main signaling pathways downstream of NRAS is the MAPK pathway. In this study we investig...
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Article
Open AccessCRAF R391W is a melanoma driver oncogene
Approximately 75% of melanomas have known driver oncogenic mutations in BRAF, NRAS, GNA11 or GNAQ, while the mutations providing constitutive oncogenic signaling in the remaining melanomas are not known. We es...
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Article
Open AccessCutaneous wound healing through paradoxical MAPK activation by BRAF inhibitors
BRAF inhibitors are highly effective therapies for the treatment of BRAFV600-mutated melanoma, with the main toxicity being a variety of hyperproliferative skin conditions due to paradoxical activation of the mit...
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Article
Open AccessJUN dependency in distinct early and late BRAF inhibition adaptation states of melanoma
A prominent mechanism of acquired resistance to BRAF inhibitors in BRAFV600-mutant melanoma is associated with the upregulation of receptor tyrosine kinases. Evidences suggested that this resistance mechanism is ...
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Article
A highly sensitive electrochemical biosensor for dopamine and uric acid in the presence of a high concentration of ascorbic acid
Applying zein nanoparticles in addition to MWCNTs, a bio-nanocomposite has been produced to modify glass carbon electrodes. The modified electrode has been used as an economically affordable electrochemical bi...