MAPK‐Targeted Drug Delivered by a pH‐Sensitive MSNP Nanocarrier Synergizes with PD‐1 Blockade in Melanoma without T‐Cell Suppression
Sign Up to like & getrecommendations! Published in 2019 at "Advanced Functional Materials"
DOI: 10.1002/adfm.201806916
Abstract: The combination of BRAF/MEK‐targeted therapy with immune checkpoint blockade is regarded as a promising regimen for patients with metastatic melanoma due to their complementary advantages. However, MEK‐inhibitor‐induced T‐cell toxicity impedes effective cooperation. In this experiment,… read more here.
Keywords: mapk targeted; mek inhibitor; suppression; inhibitor ... See more keywords
An injectable microparticle formulation for the sustained release of the specific MEK inhibitor PD98059: in vitro evaluation and pharmacokinetics
Sign Up to like & getrecommendations! Published in 2020 at "Drug Delivery and Translational Research"
DOI: 10.1007/s13346-020-00758-9
Abstract: PD98059 is a reversible MEK inhibitor that we are investigating as a potential treatment for neurochemical changes in the brain that drive neurohumoral excitation in heart failure. In a rat model that closely resembles human… read more here.
Keywords: pd98059; mek inhibitor; heart failure; release ... See more keywords
Clinical implications of ALDH1A1 and ALDH1A3 mRNA expression in melanoma subtypes.
Sign Up to like & getrecommendations! Published in 2019 at "Chemico-biological interactions"
DOI: 10.1016/j.cbi.2019.108822
Abstract: Aldehyde dehydrogenase (ALDH) activity is not only a valuable marker for cancer cells with stem-like features, but also plays a vital role in drug resistance and disease progression in many tumors including melanoma. However, the… read more here.
Keywords: melanoma; braf mek; mek inhibitor; expression ... See more keywords
Analysis of NRAS gain in 657 patients with melanoma and evaluation of its sensitivity to a MEK inhibitor.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of cancer"
DOI: 10.1016/j.ejca.2017.11.011
Abstract: BACKGROUND Neuroblastoma rat-sarcoma (NRAS) mutations have been described in Chinese patients with melanoma. However, the status and the clinical significance of NRAS gain have not been investigated on a large scale. METHODS A total of… read more here.
Keywords: patients melanoma; nras gain; mek inhibitor;
Genome-wide CRISPR-cas9 knockout screening identifies GRB7 as a driver for MEK inhibitor resistance in KRAS mutant colon cancer
Sign Up to like & getrecommendations! Published in 2021 at "Oncogene"
DOI: 10.1038/s41388-021-02077-w
Abstract: Targeting the KRAS pathway is a promising but challenging approach for colorectal cancer therapy. Despite showing potent efficacy in BRAF-mutated melanoma, MEK inhibitors appeared to be tolerated by colorectal cancer cells due to their intrinsic… read more here.
Keywords: genome wide; plk1; mek inhibitor; mek inhibitors ... See more keywords
Triple blockade of EGFR, MEK and PD-L1 as effective antitumor treatment in PD-L1 overexpressing, MEK inhibitor resistant colon cancer cells
Sign Up to like & getrecommendations! Published in 2019 at "Annals of Oncology"
DOI: 10.1093/annonc/mdz238.010
Abstract: Abstract Background Molecular mechanisms driving acquired resistance to anti-EGFR therapies in metastatic Colorectal Cancer (mCRC) are complex but generally involve the activation of the downstream RAS-RAF-MEK-MAPK pathway. Methods In order to understand the mechanism underlying… read more here.
Keywords: meki; egfr; mek inhibitor; treatment ... See more keywords
A novel preclinical model of RAF-independent MEK1 mutant tumors and its treatment with novel ATP competitive MEK inhibitor
Sign Up to like & getrecommendations! Published in 2019 at "Annals of Oncology"
DOI: 10.1093/annonc/mdz268.085
Abstract: Abstract Background A subgroup of MEK1 mutations in human tumors were recently described as RAF- and phosphorylation independent and as insensitive to currently clinically used allosteric MEK inhibitors. We established a novel cell line that… read more here.
Keywords: inhibitor; mek inhibitor; atp competitive; mek ... See more keywords
A phase I trial of the MEK inhibitor selumetinib (AZD6244) in pediatric patients with recurrent or refractory low-grade glioma: a Pediatric Brain Tumor Consortium (PBTC) study
Sign Up to like & getrecommendations! Published in 2017 at "Neuro-Oncology"
DOI: 10.1093/neuonc/now282
Abstract: Background Activation of the mitogen-activated protein kinase pathway is important for growth of pediatric low-grade gliomas (LGGs). The aim of this study was to determine the recommended phase II dose (RP2D) and the dose-limiting toxicities… read more here.
Keywords: selumetinib; mek inhibitor; grade; study ... See more keywords
Heterogeneous alteration of the ERBB3–MYC axis associated with MEK inhibitor resistance in a KRAS-mutated low-grade serous ovarian cancer patient
Sign Up to like & getrecommendations! Published in 2019 at "Cold Spring Harbor Molecular Case Studies"
DOI: 10.1101/mcs.a004341
Abstract: Low-grade serous ovarian cancer (LGSOC) is relatively chemoresistant, and no precision therapy is approved for this indication. Despite promising results in phase II trials, MEK inhibitors have failed to show improved progression-free survival in a… read more here.
Keywords: kras mutated; inhibitor; mek inhibitor; inhibitor resistance ... See more keywords
HDAC Inhibition Enhances the In Vivo Efficacy of MEK Inhibitor Therapy in Uveal Melanoma
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DOI: 10.1158/1078-0432.ccr-18-3382
Abstract: Purpose: The clinical use of MEK inhibitors in uveal melanoma is limited by the rapid acquisition of resistance. This study has used multiomics approaches and drug screens to identify the pan-HDAC inhibitor panobinostat as an… read more here.
Keywords: uveal melanoma; mek; hdac; mek inhibitor ... See more keywords
Discovery of a novel ATP-competitive MEK inhibitor DS03090629 that overcomes resistance conferred by BRAF overexpression in BRAF-mutated melanoma.
Sign Up to like & getrecommendations! Published in 2023 at "Molecular cancer therapeutics"
DOI: 10.1158/1535-7163.mct-22-0306
Abstract: Melanoma patients with activating BRAF mutations (BRAF V600E/K) initially respond to combination therapy of BRAF and MEK inhibitors. However, their clinical efficacy is limited by acquired resistance, in some cases driven by amplification of the… read more here.
Keywords: braf; mek; resistance; mek inhibitor ... See more keywords