mertk inhibitor

| n = 3–4 independent experiments, *, P < 0.05; **, P < 0.01; ***, P < 0.001, one-way ANOVA. Minson KA, et al. IL-12 produced by dendritic cells augments CD8, Henry CJ, et al.

Inhibition of MERTK Promotes Suppression of Tumor Growth in BRAF Mutant and BRAF Wild-Type Melanoma, A landscape of driver mutations in melanoma, Improved survival with vemurafenib in melanoma with BRAF V600E mutation, Improved survival with ipilimumab in patients with metastatic melanoma, Frequencies of BRAF and NRAS mutations are different in histological types and sites of origin of cutaneous melanoma: a meta-analysis, BRAF inhibitors induce metastasis in RAS mutant or inhibitor-resistant melanoma cells by reactivating MEK and ERK signaling, Reversing melanoma cross-resistance to BRAF and MEK inhibitors by co-targeting the AKT/mTOR pathway, Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation, RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E), Binimetinib versus dacarbazine in patients with advanced NRAS-mutant melanoma (NEMO): a multicentre, open-label, randomised, phase 3 trial, Recovery of phospho-ERK activity allows melanoma cells to escape from BRAF inhibitor therapy, Dabrafenib and trametinib versus dabrafenib and placebo for Val600 BRAF-mutant melanoma: a multicentre, double-blind, phase 3 randomised controlled trial, Current status and perspectives in immunotherapy for metastatic melanoma, TAM receptor tyrosine kinases: biologic functions, signaling, and potential therapeutic targeting in human cancer, Small molecule inhibition of MERTK is efficacious in non-small cell lung cancer models independent of driver oncogene status, Inhibition of Mer and Axl receptor tyrosine kinases in astrocytoma cells leads to increased apoptosis and improved chemosensitivity, Ectopic expression of the proto-oncogene Mer in pediatric T-cell acute lymphoblastic leukemia, Mer or Axl receptor tyrosine kinase inhibition promotes apoptosis, blocks growth and enhances chemosensitivity of human non-small cell lung cancer, Signal pathways in up-regulation of chemokines by tyrosine kinase MER/NYK in prostate cancer cells, MerTK inhibition in tumor leukocytes decreases tumor growth and metastasis, Mer receptor tyrosine kinase inhibition impedes glioblastoma multiforme migration and alters cellular morphology, Phosphoproteomic screen identifies potential therapeutic targets in melanoma, Human cutaneous melanomas lacking MITF and melanocyte differentiation antigens express a functional Axl receptor kinase, MERTK receptor tyrosine kinase is a therapeutic target in melanoma, A genomic screen identifies TYRO3 as a MITF regulator in melanoma, Evaluation of Tyro3 expression, Gas6-mediated Akt phosphorylation, and the impact of anti-Tyro3 antibodies in melanoma cell lines, MERTK controls melanoma cell migration and survival and differentially regulates cell behavior relative to AXL, Targeting the cancer kinome through polypharmacology, Receptor tyrosine kinase coactivation networks in cancer, mTORC1/autophagy-regulated MerTK in mutant BRAFV600 melanoma with acquired resistance to BRAF inhibition, UNC2025, a potent and orally bioavailable MER/FLT3 dual inhibitor, UNC2025, a MerTK small molecule inhibitor, is therapeutically effective alone and in combination with methotrexate in leukemia models, COSMIC: somatic cancer genetics at high-resolution, COSMIC, Catalogue of Somatic Mutations in Cancer 13-Feb-18 [cited 2018 Apr 24], ALK inhibitor response in melanomas expressing EML4-ALK fusions and alternate ALK isoforms, Patient-derived tumour xenografts as models for oncology drug development, Development and maintenance of a preclinical patient derived tumor xenograft model for the investigation of novel anti-cancer therapies, The TAM family: phosphatidylserine sensing receptor tyrosine kinases gone awry in cancer, The RAS/RAF/MEK/ERK and PI3K/AKT signaling pathways present molecular targets for the effective treatment of advanced melanoma, Validating survivin as a cancer therapeutic target, Role of the apoptotic and mitotic regulator survivin in melanoma, Survivin expression by metastatic melanoma predicts poor disease outcome in patients receiving adjuvant polyvalent vaccine, Survivin, bcl-2, bax, and bcl-X gene expression in sentinel lymph nodes from melanoma patients, MERTK inhibition induces polyploidy and promotes cell death and cellular senescence in glioblastoma multiforme, Overexpression of MERTK receptor tyrosine kinase in epithelial cancer cells drives efferocytosis in a gain-of-function capacity, Pembrolizumab versus investigator-choice chemotherapy for ipilimumab-refractory melanoma (KEYNOTE-002): a randomised, controlled, phase 2 trial, Expression and function of Flt3/flk2 in human tumor cell lines, Expression of activated TrkA protein in melanocytic tumors: relationship to cell proliferation and clinical outcome, TrkA is amplified in malignant melanoma patients and induces an anti-proliferative response in cell lines, Osimertinib in NSCLC Patients with Uncommon EGFR Mutations, CB-03–10 AR/GR Antagonist for AR-resistant Solid Tumors, Cancer Epidemiology, Biomarkers & Prevention, Disclosure of Potential Conflicts of Interest. |, Find articles by (B) Phosphorylated and total MERTK were quantified by densitometry. Camenisch TD, Koller BH, Earp HS, Matsushima GK. Uptake of dyes was assessed by flow cytometry using a CyAn or Cytoflex analyzer (Beckman Coulter) and FlowJo software (FlowJo, LLC). Mutated NRAS is the second most common oncogenic driver in melanoma and the MEK inhibitor binimetinib has had clinical efficacy in this setting, but improvements in progression-free survival over standard chemotherapy have been limited to only 1 to 2 months (10). Merestinib (LY2801653) also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively.

5B). The mean trough plasma concentration in mice treated with UNC2025 using this dosing strategy is of 161 nmol/L (16), which corresponds with the doses that mediate effective antitumor activity in cell culture assays (Fig. Kaplan-Meier survival curves were analyzed using the Mantel-Cox test. MERTK inhibition increases survival in an immunocompetent MERTK-negative B-ALL model. In this model, MRX-2843 mediated a dose-dependent reduction in tumor burden indicated by decreased bioluminescence compared with vehicle treatment (Figure 1, B and C). Find NCBI SARS-CoV-2 literature, sequence, and clinical content: https://www.ncbi.nlm.nih.gov/sars-cov-2/. To determine whether UNC2025 has therapeutic activity against melanoma, PDX models were generated by transplanting biologically stable tumor samples into immune-compromised athymic nude mice (37) and the impact of treatment with UNC2025 on tumor growth was monitored. Polyploidy was detected by propidium iodide staining and metaphase spread. C, The indicated cell lines were treated with UNC2025 for 72 hours. A, Serum starved BRAFmt G361 cell cultures were treated with 300 nmol/L UNC2025 and/or 675 nmol/L vemurafenib or DMSO vehicle for 90 minutes and then stimulated with 200 nmol/L GAS6 ligand or an equivalent volume of vehicle for an additional 10 minutes. Increased infiltration of M2-macrophages, T-cells and PD-L1 expression in high grade leiomyosarcomas supports immunotherapeutic strategies. Tumor volumes were measures at intervals. Cummings CT, Zhang W, Davies KD, Kirkpatrick GD, Zhang D, DeRyckere D, Wang X, Frye SV, Earp HS, Graham DK. The J774 cell line was obtained from the ATCC. Combined treatment with BRAF and MEK inhibitors, such as vemurafenib and cobimetinib, delayed onset of resistance compared with BRAF inhibition alone (11), leading to improved clinical responses and prolonged survival (12). eCollection 2020. Mice with established tumors were randomized to groups and treated with UNC2025 twice daily, vemurafenib once daily, UNC2025 and vemurafinib combined, or 10 mL/kg vehicle.

(C) Analysis of interactions between UNC2025 and CCNU. Additionally, PD-L1 and PD-L2 are both independent prognostic markers in several tumor types (34, 35), and PD-L1/PD-L2 coexpression has been associated with significantly shorter overall survival in patients with esophageal cancer compared with patients whose tumors did not express PD-1 ligands (21). PubMed

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