Selumetinib
| Title | Journal |
|---|---|
| Paradoxical activation of MEK/ERK signaling induced by B-Raf inhibition enhances DR5 expression and DR5 activation-induced apoptosis in Ras-mutant cancer cells. | Scientific reports 20160101 |
| Harmine Induces Adipocyte Thermogenesis through RAC1-MEK-ERK-CHD4 Axis. | Scientific reports 20160101 |
| Targeting TBK1 inhibits migration and resistance to MEK inhibitors in mutant NRAS melanoma. | Molecular cancer research : MCR 20141001 |
| Synergistic induction of human cathelicidin antimicrobial peptide gene expression by vitamin D and stilbenoids. | Molecular nutrition & food research 20140301 |
| Flavanoids induce expression of the suppressor of cytokine signalling 3 (SOCS3) gene and suppress IL-6-activated signal transducer and activator of transcription 3 (STAT3) activation in vascular endothelial cells. | The Biochemical journal 20130901 |
| Identification of potent Yes1 kinase inhibitors using a library screening approach. | Bioorganic & medicinal chemistry letters 20130801 |
| Optimization of allosteric MEK inhibitors. Part 1: Venturing into underexplored SAR territories. | Bioorganic & medicinal chemistry letters 20130415 |
| MEK and the inhibitors: from bench to bedside. | Journal of hematology & oncology 20130101 |
| Combined PI3K/mTOR and MEK inhibition provides broad antitumor activity in faithful murine cancer models. | Clinical cancer research : an official journal of the American Association for Cancer Research 20121001 |
| Combination of the ERK inhibitor AZD6244 and low-dose sorafenib in a xenograft model of human renal cell carcinoma. | International journal of oncology 20120801 |
| Antitumor action of the MET tyrosine kinase inhibitor crizotinib (PF-02341066) in gastric cancer positive for MET amplification. | Molecular cancer therapeutics 20120701 |
| A phase II open-label randomized study to assess the efficacy and safety of selumetinib (AZD6244 [ARRY-142886]) versus capecitabine in patients with advanced or metastatic pancreatic cancer who have failed first-line gemcitabine therapy. | Investigational new drugs 20120601 |
| Intrinsic resistance to selumetinib, a selective inhibitor of MEK1/2, by cAMP-dependent protein kinase A activation in human lung and colorectal cancer cells. | British journal of cancer 20120508 |
| Dynamic reprogramming of the kinome in response to targeted MEK inhibition in triple-negative breast cancer. | Cell 20120413 |
| The synergistic interaction of MEK and PI3K inhibitors is modulated by mTOR inhibition. | British journal of cancer 20120410 |
| Enhanced apoptosis and tumor growth suppression elicited by combination of MEK (selumetinib) and mTOR kinase inhibitors (AZD8055). | Cancer research 20120401 |
| Cancer: Clinical trials unite mice and humans. | Nature 20120328 |
| A murine lung cancer co-clinical trial identifies genetic modifiers of therapeutic response. | Nature 20120318 |
| Combined MEK and VEGFR inhibition in orthotopic human lung cancer models results in enhanced inhibition of tumor angiogenesis, growth, and metastasis. | Clinical cancer research : an official journal of the American Association for Cancer Research 20120315 |
| The MEK1/2 inhibitor, selumetinib (AZD6244; ARRY-142886), enhances anti-tumour efficacy when combined with conventional chemotherapeutic agents in human tumour xenograft models. | British journal of cancer 20120227 |
| Preclinical activity of the rational combination of selumetinib (AZD6244) in combination with vorinostat in KRAS-mutant colorectal cancer models. | Clinical cancer research : an official journal of the American Association for Cancer Research 20120215 |
| The Akt inhibitor MK2206 synergizes, but perifosine antagonizes, the BRAF(V600E) inhibitor PLX4032 and the MEK1/2 inhibitor AZD6244 in the inhibition of thyroid cancer cells. | The Journal of clinical endocrinology and metabolism 20120201 |
| Sorafenib and Mek inhibition is synergistic in medullary thyroid carcinoma in vitro. | Endocrine-related cancer 20120201 |
| MEK1/2 inhibitor selumetinib (AZD6244) inhibits growth of ovarian clear cell carcinoma in a PEA-15-dependent manner in a mouse xenograft model. | Molecular cancer therapeutics 20120201 |
| Phase II, open-label, randomized trial of the MEK1/2 inhibitor selumetinib as monotherapy versus temozolomide in patients with advanced melanoma. | Clinical cancer research : an official journal of the American Association for Cancer Research 20120115 |
| Impact of combined mTOR and MEK inhibition in uveal melanoma is driven by tumor genotype. | PloS one 20120101 |
| A phase I, open-label, randomized crossover study to assess the effect of dosing of the MEK 1/2 inhibitor Selumetinib (AZD6244; ARRY-142866) in the presence and absence of food in patients with advanced solid tumors. | Cancer chemotherapy and pharmacology 20111201 |
| Small molecule inhibition of the steroid receptor coactivators, SRC-3 and SRC-1. | Molecular endocrinology (Baltimore, Md.) 20111201 |
| Cytokinetically quiescent (G0/G1) human multiple myeloma cells are susceptible to simultaneous inhibition of Chk1 and MEK1/2. | Blood 20111110 |
| Comprehensive analysis of kinase inhibitor selectivity. | Nature biotechnology 20111030 |
| A Phase II, open-label, randomised study to assess the efficacy and safety of the MEK1/2 inhibitor AZD6244 (ARRY-142886) versus capecitabine monotherapy in patients with colorectal cancer who have failed one or two prior chemotherapeutic regimens. | Investigational new drugs 20111001 |
| Exon capture analysis of G protein-coupled receptors identifies activating mutations in GRM3 in melanoma. | Nature genetics 20110925 |
| Simultaneous exposure of transformed cells to SRC family inhibitors and CHK1 inhibitors causes cell death. | Cancer biology & therapy 20110801 |
| Enhancement of 5-fluorouracil-induced in vitro and in vivo radiosensitization with MEK inhibition. | Clinical cancer research : an official journal of the American Association for Cancer Research 20110801 |
| Nilotinib alone or in combination with selumetinib is a drug candidate for neurofibromatosis type 2. | Neuro-oncology 20110701 |
| Phase II study of the mitogen-activated protein kinase 1/2 inhibitor selumetinib in patients with advanced hepatocellular carcinoma. | Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20110610 |
| NSCLC drug targets acquire new visibility. | Journal of the National Cancer Institute 20110302 |
| Regulation of mesenchymal stem cell activity by endothelial cells. | Stem cells and development 20110301 |
| Pharmacokinetics and pharmacodynamics of AZD6244 (ARRY-142886) in tumor-bearing nude mice. | Cancer chemotherapy and pharmacology 20110201 |
| Could HBx protein expression affect signal pathway inhibition by gefitinib or selumetinib, a MEK inhibitor, in hepatocellular carcinoma cell lines? | Journal of Korean medical science 20110201 |
| EZH2 promotes expansion of breast tumor initiating cells through activation of RAF1-β-catenin signaling. | Cancer cell 20110118 |
| MEK1/2 inhibitors AS703026 and AZD6244 may be potential therapies for KRAS mutated colorectal cancer that is resistant to EGFR monoclonal antibody therapy. | Cancer research 20110115 |
| Reversing melanoma cross-resistance to BRAF and MEK inhibitors by co-targeting the AKT/mTOR pathway. | PloS one 20110101 |
| Vertical targeting of the phosphatidylinositol-3 kinase pathway as a strategy for treating melanoma. | Clinical cancer research : an official journal of the American Association for Cancer Research 20101215 |
| Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. | Chemistry & biology 20101124 |
| A phase II, open-label, randomized study to assess the efficacy and safety of AZD6244 (ARRY-142886) versus pemetrexed in patients with non-small cell lung cancer who have failed one or two prior chemotherapeutic regimens. | Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20101001 |
| Inhibition of MEK/ERK signaling induces apoptosis of acute myelogenous leukemia cells via inhibition of eukaryotic initiation factor 4E-binding protein 1 and down-regulation of Mcl-1. | Apoptosis : an international journal on programmed cell death 20100701 |
| AZD6244 (ARRY-142886) enhances the antitumor activity of rapamycin in mouse models of human hepatocellular carcinoma. | Cancer 20100301 |
| The first-in-human study of the hydrogen sulfate (Hyd-sulfate) capsule of the MEK1/2 inhibitor AZD6244 (ARRY-142886): a phase I open-label multicenter trial in patients with advanced cancer. | Clinical cancer research : an official journal of the American Association for Cancer Research 20100301 |
| Mitogen-activated protein/extracellular signal-regulated kinase kinase inhibition results in biphasic alteration of epidermal homeostasis with keratinocytic apoptosis and pigmentation disorders. | Clinical cancer research : an official journal of the American Association for Cancer Research 20100201 |
| Targeting ERK1/2 activation and proliferation in human primary schwannoma cells with MEK1/2 inhibitor AZD6244. | Neurobiology of disease 20100101 |
| AZD6244 enhances the anti-tumor activity of sorafenib in ectopic and orthotopic models of human hepatocellular carcinoma (HCC). | Journal of hepatology 20100101 |
| Apoptosis induction by MEK inhibition in human lung cancer cells is mediated by Bim. | PloS one 20100101 |
| Combination treatment with MEK and AKT inhibitors is more effective than each drug alone in human non-small cell lung cancer in vitro and in vivo. | PloS one 20100101 |
| Detection of BRAF mutations in the tumour and serum of patients enrolled in the AZD6244 (ARRY-142886) advanced melanoma phase II study. | British journal of cancer 20091117 |
| Dual inhibition of mitogen-activated protein kinase kinase and mammalian target of rapamycin in differentiated and anaplastic thyroid cancer. | The Journal of clinical endocrinology and metabolism 20091001 |
| A combined, rational approach towards inhibition of the MEK-ERK and mTOR pathways in pancreatic ductal adenocarcinoma: promise or deja vu? | Cancer biology & therapy 20091001 |
| Effects of combined inhibition of MEK and mTOR on downstream signaling and tumor growth in pancreatic cancer xenograft models. | Cancer biology & therapy 20091001 |
| Blockade of MEK signaling potentiates 5-Aza-2'-deoxycytidine-induced apoptosis and upregulation of p21(waf1) in acute myelogenous leukemia cells. | International journal of cancer 20090901 |
| Inhibition of MEK signaling enhances the ability of cytarabine to induce growth arrest and apoptosis of acute myelogenous leukemia cells. | Apoptosis : an international journal on programmed cell death 20090901 |
| AZD6244 (ARRY-142886) enhances the therapeutic efficacy of sorafenib in mouse models of gastric cancer. | Molecular cancer therapeutics 20090901 |
| Combination of EGFR and MEK1/2 inhibitor shows synergistic effects by suppressing EGFR/HER3-dependent AKT activation in human gastric cancer cells. | Molecular cancer therapeutics 20090901 |
| Trial offers early test case for personalized medicine. | Journal of the National Cancer Institute 20090204 |
| Inhibition of MEK/ERK signaling synergistically potentiates histone deacetylase inhibitor-induced growth arrest, apoptosis and acetylation of histone H3 on p21waf1 promoter in acute myelogenous leukemia cell. | Leukemia 20080701 |
| Advances in the development of cancer therapeutics directed against the RAS-mitogen-activated protein kinase pathway. | Clinical cancer research : an official journal of the American Association for Cancer Research 20080615 |
| Blockade of MEK/ERK signaling enhances sunitinib-induced growth inhibition and apoptosis of leukemia cells possessing activating mutations of the FLT3 gene. | Leukemia research 20080601 |
| BRAFV600E mutation is associated with preferential sensitivity to mitogen-activated protein kinase kinase inhibition in thyroid cancer cell lines. | The Journal of clinical endocrinology and metabolism 20080601 |
| The mitogen-activated protein/extracellular signal-regulated kinase kinase inhibitor AZD6244 (ARRY-142886) induces growth arrest in melanoma cells and tumor regression when combined with docetaxel. | Clinical cancer research : an official journal of the American Association for Cancer Research 20080101 |
| Targeting MEK induces myeloma-cell cytotoxicity and inhibits osteoclastogenesis. | Blood 20070901 |
| AZD6244 and doxorubicin induce growth suppression and apoptosis in mouse models of hepatocellular carcinoma. | Molecular cancer therapeutics 20070901 |
| AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical models. | Molecular cancer therapeutics 20070801 |
| ZD6474 induces growth arrest and apoptosis of human leukemia cells, which is enhanced by concomitant use of a novel MEK inhibitor, AZD6244. | Leukemia 20070601 |
| Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. | Clinical cancer research : an official journal of the American Association for Cancer Research 20070301 |
| Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma. | Molecular cancer therapeutics 20070101 |
| Targeted agents for the treatment of advanced renal cell carcinoma. | Current drug targets 20051101 |
| Mutations of the BRAF gene in human cancer. | Nature 20020627 |