2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide
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Pyrethroid Insecticide Cypermethrin Modulates Gonadotropin Synthesis via Calcium Homeostasis and ERK1/2 Signaling in LβT2 Mouse Pituitary Cells. | Toxicological sciences : an official journal of the Society of Toxicology 20180301 |
Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells. | Toxicology 20171201 |
Anti-androgen 2-hydroxyflutamide modulates cadherin, catenin and androgen receptor phosphorylation in androgen-sensitive LNCaP and androgen-independent PC3 prostate cancer cell lines acting via PI3K/Akt and MAPK/ERK1/2 pathways. | Toxicology in vitro : an international journal published in association with BIBRA 20170401 |
Endoplasmic Reticulum Stress Induction and ERK1/2 Activation Contribute to Nefazodone-Induced Toxicity in Hepatic Cells. | Toxicological sciences : an official journal of the Society of Toxicology 20161201 |
Hydroxyflutamide affects connexin 43 via the activation of PI3K/Akt-dependent pathway but has no effect on the crosstalk between PI3K/Akt and ERK1/2 pathways at the Raf-1 kinase level in primary rat Sertoli cells. | Toxicology in vitro : an international journal published in association with BIBRA 20160301 |
U0126, a mitogen-activated protein kinase kinase 1 and 2 (MEK1 and 2) inhibitor, selectively up-regulates main isoforms of CYP3A subfamily via a pregnane X receptor (PXR) in HepG2 cells. | Archives of toxicology 20141201 |
Endocrine disrupting effects of dichlorodiphenyltrichloroethane analogues on gonadotropin hormones in pituitary gonadotrope cells. | Environmental toxicology and pharmacology 20140501 |
Pau d'arco activates Nrf2-dependent gene expression via the MEK/ERK-pathway. | The Journal of toxicological sciences 20140401 |
Sertraline, an antidepressant, induces apoptosis in hepatic cells through the mitogen-activated protein kinase pathway. | Toxicological sciences : an official journal of the Society of Toxicology 20140201 |
Cadmium induces N-cadherin cleavage via ERK-mediated γ-secretase activation in C6 astroglia cells. | Toxicology letters 20131024 |
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 |
Inhibition of MEK pathway in vestibular schwannoma cell culture. | The Laryngoscope 20121001 |
Impact of oncogenic driver mutations on feedback between the PI3K and MEK pathways in cancer cells. | Bioscience reports 20120801 |
Morphine activates the E twenty six-like transcription factor-1/serum response factor pathway via extracellular signal-regulated kinases 1/2 in F11 cells derived from dorsal root ganglia neurons. | The Journal of pharmacology and experimental therapeutics 20120701 |
Phosphorylation of serine 21 modulates the proliferation inhibitory more than the differentiation inducing effects of C/EBPα in K562 cells. | Journal of cellular biochemistry 20120501 |
MEK/Erk-based negative feedback mechanism involved in control of Steel Factor-triggered production of Krüppel-like factor 2 in mast cells. | Cellular signalling 20120401 |
3,5-Disubstituted-thiazolidine-2,4-dione analogs as anticancer agents: design, synthesis and biological characterization. | European journal of medicinal chemistry 20120101 |
Nilotinib and MEK inhibitors induce synthetic lethality through paradoxical activation of RAF in drug-resistant chronic myeloid leukemia. | Cancer cell 20111213 |
Comprehensive analysis of kinase inhibitor selectivity. | Nature biotechnology 20111030 |
ERK1/2 and ERK5 have distinct roles in the regulation of brain-derived neurotrophic factor expression. | Journal of neuroscience research 20111001 |
Cigarette smoke components induce matrix metalloproteinase-1 in aortic endothelial cells through inhibition of mTOR signaling. | Toxicological sciences : an official journal of the Society of Toxicology 20111001 |
Epidermal growth factor induces matrix metalloproteinase-1 (MMP-1) expression and invasion in glioma cell lines via the MAPK pathway. | Journal of neuro-oncology 20110901 |
Constitutive ERK activity induces downregulation of tristetraprolin, a major protein controlling interleukin8/CXCL8 mRNA stability in melanoma cells. | American journal of physiology. Cell physiology 20110901 |
BCR-ABL- and Ras-independent activation of Raf as a novel mechanism of Imatinib resistance in CML. | International journal of oncology 20110901 |
Compartmentalization of the MAPK scaffold protein KSR1 modulates synaptic plasticity in hippocampal neurons. | FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20110701 |
The MEK inhibitor PD184352 enhances BMS-214662-induced apoptosis in CD34+ CML stem/progenitor cells. | Leukemia 20110701 |
Mitogen-activated protein kinase kinase 1 (MEK1) stabilizes MyoD through direct phosphorylation at tyrosine 156 during myogenic differentiation. | The Journal of biological chemistry 20110527 |
Coordinated waves of gene expression during neuronal differentiation of embryonic stem cells as basis for novel approaches to developmental neurotoxicity testing. | Cell death and differentiation 20110301 |
ERK5 signalling in prostate cancer promotes an invasive phenotype. | British journal of cancer 20110215 |
Synergy between inhibitors of androgen receptor and MEK has therapeutic implications in estrogen receptor-negative breast cancer. | Breast cancer research : BCR 20110101 |
Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. | Chemistry & biology 20101124 |
MEK inhibitors suppress beta-amyloid production by altering the level of a beta-C-terminal fragment of amyloid precursor protein in neuronal cells. | FEBS letters 20100804 |
Discovery of 3-(2-aminoethyl)-5-(3-phenyl-propylidene)-thiazolidine-2,4-dione as a dual inhibitor of the Raf/MEK/ERK and the PI3K/Akt signaling pathways. | Bioorganic & medicinal chemistry letters 20100801 |
Regulation of the miR-212/132 locus by MSK1 and CREB in response to neurotrophins. | The Biochemical journal 20100513 |
Three inhibitors of FGF receptor, ERK, and GSK3 establishes germline-competent embryonic stem cells of C57BL/6N mouse strain with high efficiency and stability. | Genesis (New York, N.Y. : 2000) 20100501 |
Hepatitis C virus RNA replication is regulated by Ras-Erk signalling. | The Journal of general virology 20100301 |
Three-dimensional overlay culture models of human breast cancer reveal a critical sensitivity to mitogen-activated protein kinase kinase inhibitors. | The Journal of pharmacology and experimental therapeutics 20100301 |
Inhibition of MEK/ERK1/2 sensitizes lymphoma cells to sorafenib-induced apoptosis. | Leukemia research 20100301 |
Blockade of the extracellular signal-regulated kinase pathway enhances the therapeutic efficacy of microtubule-destabilizing agents in human tumor xenograft models. | Clinical cancer research : an official journal of the American Association for Cancer Research 20100215 |
Growth of hormone-dependent MCF-7 breast cancer cells is promoted by constitutive caveolin-1 whose expression is lost in an EGF-R-mediated manner during development of tamoxifen resistance. | Breast cancer research and treatment 20100201 |
Blockade of the ERK or PI3K-Akt signaling pathway enhances the cytotoxicity of histone deacetylase inhibitors in tumor cells resistant to gefitinib or imatinib. | Biochemical and biophysical research communications 20100122 |
Simvastatin inhibits angiotensin II-induced abdominal aortic aneurysm formation in apolipoprotein E-knockout mice: possible role of ERK. | Arteriosclerosis, thrombosis, and vascular biology 20091101 |
MEK inhibitors potentiate dexamethasone lethality in acute lymphoblastic leukemia cells through the pro-apoptotic molecule BIM. | Leukemia 20091001 |
Suppression of Erk signalling promotes ground state pluripotency in the mouse embryo. | Development (Cambridge, England) 20091001 |
Response and resistance to MEK inhibition in leukaemias initiated by hyperactive Ras. | Nature 20090917 |
Induction of Bim expression contributes to the antitumor synergy between sorafenib and mitogen-activated protein kinase/extracellular signal-regulated kinase kinase inhibitor CI-1040 in hepatocellular carcinoma. | Clinical cancer research : an official journal of the American Association for Cancer Research 20090915 |
Distinct genetic alterations in the mitogen-activated protein kinase pathway dictate sensitivity of thyroid cancer cells to mitogen-activated protein kinase kinase 1/2 inhibition. | Thyroid : official journal of the American Thyroid Association 20090801 |
Combined inhibition of MEK and mammalian target of rapamycin abolishes phosphorylation of cyclin-dependent kinase 4 in glioblastoma cell lines and prevents their proliferation. | Cancer research 20090601 |
Inhibition of the growth of papillary thyroid carcinoma cells by CI-1040. | Archives of otolaryngology--head & neck surgery 20090401 |
Mitogen-activated protein kinase inhibition induces translocation of Bmf to promote apoptosis in melanoma. | Cancer research 20090301 |
LKB1/KRAS mutant lung cancers constitute a genetic subset of NSCLC with increased sensitivity to MAPK and mTOR signalling inhibition. | British journal of cancer 20090127 |
The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. | Bioorganic & medicinal chemistry letters 20081215 |
2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase). | Bioorganic & medicinal chemistry letters 20081201 |
Targeting MEK/MAPK signal transduction module potentiates ATO-induced apoptosis in multiple myeloma cells through multiple signaling pathways. | Blood 20080915 |
Reduction of chronic allograft nephropathy by inhibition of extracellular signal-regulated kinase 1 and 2 signaling. | American journal of physiology. Renal physiology 20080901 |
Cellular energetic status supervises the synthesis of bis-diphosphoinositol tetrakisphosphate independently of AMP-activated protein kinase. | Molecular pharmacology 20080801 |
Restoration of PTEN expression alters the sensitivity of prostate cancer cells to EGFR inhibitors. | The Prostate 20080615 |
Increase of MCP-1 (CCL2) in myelin mutant Schwann cells is mediated by MEK-ERK signaling pathway. | Glia 20080601 |
K-ras as a target for lung cancer therapy. | Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20080601 |
The ground state of embryonic stem cell self-renewal. | Nature 20080522 |
Enzyme kinetics and binding studies on inhibitors of MEK protein kinase. | Biochemistry 20080429 |
Pharmacophore identification of Raf-1 kinase inhibitors. | Bioorganic & medicinal chemistry letters 20080401 |
The selectivity of protein kinase inhibitors: a further update. | The Biochemical journal 20071215 |
Inhibitory effects of the mitogen-activated protein kinase kinase inhibitor CI-1040 on the proliferation and tumor growth of thyroid cancer cells with BRAF or RAS mutations. | The Journal of clinical endocrinology and metabolism 20071201 |
PD184352 releases the regular hypoxic reversible DNA replication arrest in T24 cells. | Journal of biochemistry and molecular biology 20071130 |
4-anilino-5-carboxamido-2-pyridone derivatives as noncompetitive inhibitors of mitogen-activated protein kinase kinase. | Journal of medicinal chemistry 20071018 |
Central role of the MEK/ERK MAP kinase pathway in a mouse model of rheumatoid arthritis: potential proinflammatory mechanisms. | Arthritis and rheumatism 20071001 |
MEK1/2 inhibitors potentiate UCN-01 lethality in human multiple myeloma cells through a Bim-dependent mechanism. | Blood 20070915 |
Requirement for ERK MAP kinase in mouse preimplantation development. | Development (Cambridge, England) 20070801 |
Selective inhibition of MEK1/2 reveals a differential requirement for ERK1/2 signalling in the regulation of HIF-1 in response to hypoxia and IGF-1. | Oncogene 20070607 |
Mutations in BRAF and KRAS converge on activation of the mitogen-activated protein kinase pathway in lung cancer mouse models. | Cancer research 20070515 |
MEK1/2 inhibitors sensitize Bcr/Abl+ human leukemia cells to the dual Abl/Src inhibitor BMS-354/825. | Blood 20070501 |
ERK1/2-driven and MKP-mediated inhibition of EGF-induced ERK5 signaling in human proximal tubular cells. | Journal of cellular physiology 20070401 |
Inhibition of the MAP kinase activity suppresses estrogen-induced breast tumor growth both in vitro and in vivo. | International journal of oncology 20070401 |
MEK blockade converts AML differentiating response to retinoids into extensive apoptosis. | Blood 20070301 |
Dual mitogen-activated protein kinase and epidermal growth factor receptor inhibition in biliary and pancreatic cancer. | Molecular cancer therapeutics 20070301 |
Upstream signaling inhibition enhances rapamycin effect on growth of kidney cancer cells. | Urology 20070301 |
Lovastatin inhibits the extracellular-signal-regulated kinase pathway in immortalized rat brain neuroblasts. | The Biochemical journal 20070101 |
The INT6 cancer gene and MEK signaling pathways converge during zebrafish development. | PloS one 20070101 |
Dissecting the roles of checkpoint kinase 1/CDC2 and mitogen-activated protein kinase kinase 1/2/extracellular signal-regulated kinase 1/2 in relation to 7-hydroxystaurosporine-induced apoptosis in human multiple myeloma cells. | Molecular pharmacology 20061201 |
A novel BH3 mimetic reveals a mitogen-activated protein kinase-dependent mechanism of melanoma cell death controlled by p53 and reactive oxygen species. | Cancer research 20061201 |
Protein kinases as drug targets in cancer. | Current cancer drug targets 20061101 |
MEK1/2 inhibition promotes Taxotere lethality in mammary tumors in vivo. | Cancer biology & therapy 20061001 |
New molecular targeted therapies in thyroid cancer. | Anti-cancer drugs 20060901 |
An in vivo platform for translational drug development in pancreatic cancer. | Clinical cancer research : an official journal of the American Association for Cancer Research 20060801 |
Assessment of gefitinib- and CI-1040-mediated changes in epidermal growth factor receptor signaling in HuCCT-1 human cholangiocarcinoma by serial fine needle aspiration. | Molecular cancer therapeutics 20060701 |
MEK1 inhibition sensitizes primary acute myelogenous leukemia to arsenic trioxide-induced apoptosis. | Blood 20060601 |
Extracellular signal-regulated kinase inhibition slows disease progression in mice with polycystic kidney disease. | Journal of the American Society of Nephrology : JASN 20060601 |
Synergistic interactions between DMAG and mitogen-activated protein kinase kinase 1/2 inhibitors in Bcr/abl+ leukemia cells sensitive and resistant to imatinib mesylate. | Clinical cancer research : an official journal of the American Association for Cancer Research 20060401 |
Bidirectional cross talk between ERalpha and EGFR signalling pathways regulates tamoxifen-resistant growth. | Breast cancer research and treatment 20060301 |
Blockade of the ERK pathway markedly sensitizes tumor cells to HDAC inhibitor-induced cell death. | Biochemical and biophysical research communications 20060127 |
BRAF mutation predicts sensitivity to MEK inhibition. | Nature 20060119 |
The mitogen-activated protein kinase/extracellular signal-regulated kinase kinase inhibitor PD184352 (CI-1040) selectively induces apoptosis in malignant schwannoma cell lines. | The Journal of pharmacology and experimental therapeutics 20060101 |
Development of a conditional in vivo model to evaluate the efficacy of small molecule inhibitors for the treatment of Raf-transformed hematopoietic cells. | Cancer research 20051101 |
Transient exposure of mammary tumors to PD184352 and UCN-01 causes tumor cell death in vivo and prolonged suppression of tumor regrowth. | Cancer biology & therapy 20051101 |
Two targets are better than one. Promising combination therapy to treat breast cancer. | Cancer biology & therapy 20051101 |
ERK1/2 inhibition increases antiestrogen treatment efficacy by interfering with hypoxia-induced downregulation of ERalpha: a combination therapy potentially targeting hypoxic and dormant tumor cells. | Oncogene 20051013 |
Anticancer Drug Discovery and Development - SRI's Seventh Annual Summit. | IDrugs : the investigational drugs journal 20051001 |
Quantitative single cell determination of ERK phosphorylation and regulation in relapsed and refractory primary acute myeloid leukemia. | Leukemia 20050901 |
Synergistic interactions between MEK1/2 and histone deacetylase inhibitors in BCR/ABL+ human leukemia cells. | Leukemia 20050901 |
Activation of mitogen-activated protein kinase is required for migration and invasion of placental site trophoblastic tumor. | The American journal of pathology 20050901 |
Phase I and pharmacodynamic study of the oral MEK inhibitor CI-1040 in patients with advanced malignancies. | Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20050810 |
Treating cancer by blocking cell signals. | Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20050810 |
Enhancement of the therapeutic efficacy of taxol by the mitogen-activated protein kinase kinase inhibitor CI-1040 in nude mice bearing human heterotransplants. | Cancer research 20050401 |
A role for K-ras in conferring resistance to the MEK inhibitor, CI-1040. | Neoplasia (New York, N.Y.) 20050401 |
Inactivation of the mitogen-activated protein kinase pathway as a potential target-based therapy in ovarian serous tumors with KRAS or BRAF mutations. | Cancer research 20050301 |
ERK kinase inhibition stabilizes the aryl hydrocarbon receptor: implications for transcriptional activation and protein degradation. | The Journal of biological chemistry 20050211 |
Increased dissolution rate and bioavailability through comicronization with microcrystalline cellulose. | Pharmaceutical development and technology 20050101 |
Identification of filamin C as a new physiological substrate of PKBalpha using KESTREL. | The Biochemical journal 20041215 |
Multicenter phase II study of the oral MEK inhibitor, CI-1040, in patients with advanced non-small-cell lung, breast, colon, and pancreatic cancer. | Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20041115 |
Molecular cross-talk between MEK1/2 and mTOR signaling during recovery of 293 cells from hypertonic stress. | The Journal of biological chemistry 20041029 |
In vitro and in vivo metabolism of the anti-cancer agent CI-1040, a MEK inhibitor, in rat, monkey, and human. | Pharmaceutical research 20040901 |
Inhibition of constitutively activated nuclear factor-kappaB radiosensitizes human melanoma cells. | Molecular cancer therapeutics 20040801 |
Treatment with arsenic trioxide (ATO) and MEK1 inhibitor activates the p73-p53AIP1 apoptotic pathway in leukemia cells. | Blood 20040715 |
Stress- and mitogen-induced phosphorylation of the synapse-associated protein SAP90/PSD-95 by activation of SAPK3/p38gamma and ERK1/ERK2. | The Biochemical journal 20040515 |
Use of mitogenic cascade blockers for treatment of C-Raf induced lung adenoma in vivo: CI-1040 strongly reduces growth and improves lung structure. | BMC cancer 20040101 |
Central role of Fas-associated death domain protein in apoptosis induction by the mitogen-activated protein kinase kinase inhibitor CI-1040 (PD184352) in acute lymphocytic leukemia cells in vitro. | The Journal of biological chemistry 20031121 |
Feedback control of the protein kinase TAK1 by SAPK2a/p38alpha. | The EMBO journal 20031103 |
CI-1040 (PD184352), a targeted signal transduction inhibitor of MEK (MAPKK). | Seminars in oncology 20031001 |
Synthesis and evaluation of 4-anilino-6,7-dialkoxy-3-quinolinecarbonitriles as inhibitors of kinases of the Ras-MAPK signaling cascade. | Bioorganic & medicinal chemistry letters 20030915 |
Treatment of metastatic melanoma with an orally available inhibitor of the Ras-Raf-MAPK cascade. | Cancer research 20030915 |
Effects of the MEK inhibitor CI-1040 (PD 184352) on progenitor growth from normal and myelodysplastic marrow. | Haematologica 20030901 |
Specific blockade of the ERK pathway inhibits the invasiveness of tumor cells: down-regulation of matrix metalloproteinase-3/-9/-14 and CD44. | Biochemical and biophysical research communications 20030516 |
Chronic activation of extracellular-signal-regulated protein kinases by phenylephrine is required to elicit a hypertrophic response in cardiac myocytes. | The Biochemical journal 20030401 |
Proliferation of cancer cells despite CDK2 inhibition. | Cancer cell 20030301 |
A conserved role for the MEK signalling pathway in neural tissue specification and posteriorisation in the invertebrate chordate, the ascidian Ciona intestinalis. | Development (Cambridge, England) 20030101 |
Combined treatment with the checkpoint abrogator UCN-01 and MEK1/2 inhibitors potently induces apoptosis in drug-sensitive and -resistant myeloma cells through an IL-6-independent mechanism. | Blood 20021101 |
Ras/Erk signaling is essential for activation of protein synthesis by Gq protein-coupled receptor agonists in adult cardiomyocytes. | Circulation research 20021101 |
Targeting intracellular signal transduction. A new paradigm for a brave new world of molecularly targeted therapeutics. | Hematology/oncology clinics of North America 20021001 |
Cell-cycle arrest by PD184352 requires inhibition of extracellular signal-regulated kinases (ERK) 1/2 but not ERK5/BMK1. | The Biochemical journal 20020901 |
Synergistic induction of apoptosis by simultaneous disruption of the Bcl-2 and MEK/MAPK pathways in acute myelogenous leukemia. | Blood 20020501 |
Pharmacologic mitogen-activated protein/extracellular signal-regulated kinase kinase/mitogen-activated protein kinase inhibitors interact synergistically with STI571 to induce apoptosis in Bcr/Abl-expressing human leukemia cells. | Cancer research 20020101 |
Agents targeting ras signaling pathway. | Current pharmaceutical design 20020101 |
Coadministration of UCN-01 with MEK1/2 inhibitors potently induces apoptosis in BCR/ABL+ leukemia cells sensitive and resistant to ST1571. | Cancer biology & therapy 20020101 |
Beyond directed therapeutics--are two drugs always better than one? | Cancer biology & therapy 20020101 |
Suppression of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD)-mediated CYP1A1 and CYP1B1 induction by 12-O-tetradecanoylphorbol-13-acetate: role of transforming growth factor beta and mitogen-activated protein kinases. | Biochemical pharmacology 20011201 |
Antagonistic effects of phorbol esters on insulin regulation of insulin-like growth factor-binding protein-1 (IGFBP-1) but not glucose-6-phosphatase gene expression. | The Biochemical journal 20011101 |
Therapeutic targeting of the MEK/MAPK signal transduction module in acute myeloid leukemia. | The Journal of clinical investigation 20010915 |
MEK1/2 inhibitors promote Ara-C-induced apoptosis but not loss of Deltapsi(m) in HL-60 cells. | Biochemical and biophysical research communications 20010907 |
Effects of MAP kinase cascade inhibitors on the MKK5/ERK5 pathway. | FEBS letters 20010727 |
Pharmacological inhibitors of the mitogen-activated protein kinase (MAPK) kinase/MAPK cascade interact synergistically with UCN-01 to induce mitochondrial dysfunction and apoptosis in human leukemia cells. | Cancer research 20010701 |
Role of the ERK pathway in the activation of store-mediated calcium entry in human platelets. | The Journal of biological chemistry 20010511 |
Specificity and mechanism of action of some commonly used protein kinase inhibitors. | The Biochemical journal 20001001 |
Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo. | Nature medicine 19990701 |