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 precl

scientific article published on August 2007

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 precl is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1158/1535-7163.MCT-07-0231
P698PubMed publication ID17699718
P5875ResearchGate publication ID6139447

P2093author name stringPaul Martin
Paul D Smith
Barry R Davies
Mark Cockerill
Armelle Logie
Jennifer S McKay
Richard Jenkins
Samantha Steele
Sue Cartlidge
P2860cites workMutations of the BRAF gene in human cancerQ27860760
P433issue8
P921main subjectpharmacokineticsQ323936
pharmacodynamicsQ725307
P304page(s)2209-2219
P577publication date2007-08-01
P1433published inMolecular Cancer TherapeuticsQ2363144
P1476titleAZD6244 (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 precl
P478volume6

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cites work (P2860)
Q4049203617-allylamino-17-demethoxygeldanamycin and MEK1/2 inhibitors kill GI tumor cells via Ca2+-dependent suppression of GRP78/BiP and induction of ceramide and reactive oxygen species
Q92761643A DSTYK mutation activates ERK1/2 signaling to promote intraspinal dissemination in a case of solitary fibrous tumor/hemangiopericytoma
Q27316326A MAPK-Driven Feedback Loop Suppresses Rac Activity to Promote RhoA-Driven Cancer Cell Invasion
Q33426534A Phase II Trial of AZD6244 (Selumetinib, ARRY-142886), an Oral MEK1/2 Inhibitor, in Relapsed/Refractory Multiple Myeloma
Q42673662A 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
Q82758717A 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
Q28475822A kernelisation approach for multiple d-Hitting Set and its application in optimal multi-drug therapeutic combinations
Q24651455A new fork for clinical application: targeting forkhead transcription factors in cancer
Q42363767A phase I dose-escalation study of Selumetinib in combination with Erlotinib or Temsirolimus in patients with advanced solid tumors
Q33439877A phase I dose-escalation study of selumetinib in combination with docetaxel or dacarbazine in patients with advanced solid tumors
Q36677966A phase I study of selumetinib (AZD6244/ARRY-142866), a MEK1/2 inhibitor, in combination with cetuximab in refractory solid tumors and KRAS mutant colorectal cancer
Q35563528A 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
Q48220009Activating KRAS mutations are characteristic of oncocytic sinonasal papilloma and associated sinonasal squamous cell carcinoma.
Q33956177Activation of FOXO3a is sufficient to reverse mitogen-activated protein/extracellular signal-regulated kinase kinase inhibitor chemoresistance in human cancer
Q39352296Activity of the MEK inhibitor selumetinib (AZD6244; ARRY-142886) in nasopharyngeal cancer cell lines.
Q37182194Acute tumour response to the MEK1/2 inhibitor selumetinib (AZD6244, ARRY-142886) evaluated by non-invasive diffusion-weighted MRI.
Q38091649Advances in personalized targeted treatment of metastatic melanoma and non-invasive tumor monitoring
Q53264472Advances in the preclinical testing of cancer therapeutic hypotheses
Q38148583Advances towards the design and development of personalized non-small-cell lung cancer drug therapy.
Q38817910Allosteric modulators of MEK1: drug design and discovery
Q36544152Antitumor activity of a potent MEK inhibitor, TAK-733, against colorectal cancer cell lines and patient derived xenografts.
Q42437883Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells
Q33820374Antitumor activity of selective MEK1/2 inhibitor AZD6244 in combination with PI3K/mTOR inhibitor BEZ235 in gefitinib-resistant NSCLC xenograft models
Q37345775Apigenin potentiates TRAIL therapy of non-small cell lung cancer via upregulating DR4/DR5 expression in a p53-dependent manner
Q37410515Apigenin sensitizes colon cancer cells to antitumor activity of ABT-263.
Q28749134Apoptosis Induction by MEK Inhibition in Human Lung Cancer Cells Is Mediated by Bim
Q37605160Apoptosis and autophagy: BIM as a mediator of tumour cell death in response to oncogene-targeted therapeutics
Q26750639Apoptosis as anticancer mechanism: function and dysfunction of its modulators and targeted therapeutic strategies
Q37268123BCL-2 family inhibitors enhance histone deacetylase inhibitor and sorafenib lethality via autophagy and overcome blockade of the extrinsic pathway to facilitate killing
Q37772444BRAF, a target in melanoma: implications for solid tumor drug development
Q38945477BYL719, a selective inhibitor of phosphoinositide 3-Kinase α, enhances the effect of selumetinib (AZD6244, ARRY-142886) in KRAS-mutant non-small cell lung cancer
Q42478581Basal and treatment-induced activation of AKT mediates resistance to cell death by AZD6244 (ARRY-142886) in Braf-mutant human cutaneous melanoma cells
Q37154615Bevacizumab-based treatment in colorectal cancer with a NRAS Q61K mutation
Q35939402Binimetinib inhibits MEK and is effective against neuroblastoma tumor cells with low NF1 expression
Q41503593Biomarker-driven phase 2 study of MK-2206 and selumetinib (AZD6244, ARRY-142886) in patients with colorectal cancer
Q33732534Blockade of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase and murine double minute synergistically induces Apoptosis in acute myeloid leukemia via BH3-only proteins Puma and Bim.
Q36813976CInQ-03, a novel allosteric MEK inhibitor, suppresses cancer growth in vitro and in vivo
Q57468729Canadian Cancer Trials Group (CCTG) IND215: A phase Ib study of Selumetinib in patients with untreated advanced or metastatic NSCLC who are receiving standard chemotherapy regimens
Q35501246Chemotherapy and target therapy for hepatocellular carcinoma: New advances and challenges
Q51437778Clarifying binding difference of ATP and ADP to extracellular signal-regulated kinase 2 by using molecular dynamics simulations
Q44004637Clinical responses to selumetinib (AZD6244; ARRY-142886)-based combination therapy stratified by gene mutations in patients with metastatic melanoma
Q36698868Collections of simultaneously altered genes as biomarkers of cancer cell drug response
Q41836780Colorectal cancer cells with the BRAF(V600E) mutation are addicted to the ERK1/2 pathway for growth factor-independent survival and repression of BIM.
Q54314770Combine MEK inhibition with PI3K/mTOR inhibition exert inhibitory tumor growth effect on KRAS and PIK3CA mutation CRC xenografts due to reduced expression of VEGF and matrix metallopeptidase-9.
Q33685977Combined MEK and JAK inhibition abrogates murine myeloproliferative neoplasm
Q35836350Combined MEK and VEGFR inhibition in orthotopic human lung cancer models results in enhanced inhibition of tumor angiogenesis, growth, and metastasis
Q47123785Combined targeting of Raf and Mek synergistically inhibits tumorigenesis in triple negative breast cancer model systems
Q39142678Comparative analysis of MAPK and PI3K/AKT pathway activation and inhibition in human and canine melanoma.
Q28542683Comprehensive suppression of all apoptosis-induced proliferation pathways as a proposed approach to colorectal cancer prevention and therapy
Q39916105Converting cell lines representing hematological malignancies from glucocorticoid-resistant to glucocorticoid-sensitive: signaling pathway interactions
Q47145152Correlation between MEK signature and Ras gene alteration in advanced gastric cancer
Q41654291Cox-2-derived PGE2 induces Id1-dependent radiation resistance and self-renewal in experimental glioblastoma.
Q27022355Current and future trials of targeted therapies in cutaneous melanoma
Q42202805DNA vaccine elicits an efficient antitumor response by targeting the mutant Kras in a transgenic mouse lung cancer model.
Q28542760Data-derived modeling characterizes plasticity of MAPK signaling in melanoma
Q37803366Dermatologic side effects associated with the MEK 1/2 inhibitor selumetinib (AZD6244, ARRY-142886).
Q27644273Design and Optimization of Potent and Orally Bioavailable Tetrahydronaphthalene Raf Inhibitors
Q64263114Design, synthesis, and anticancer evaluation of novel quinoline derivatives of ursolic acid with hydrazide, oxadiazole, and thiadiazole moieties as potent MEK inhibitors
Q51572072Determination of selumetinib, N-desmethyl selumetinib and selumetinib amide in human biological samples by LC-MS/MS.
Q35677936Diffusion-weighted MRI for imaging cell death after cytotoxic or apoptosis-inducing therapy.
Q39134511Downregulation of Stat3 in melanoma: reprogramming the immune microenvironment as an anticancer therapeutic strategy
Q26781362Dual Inhibition of MEK and PI3K Pathway in KRAS and BRAF Mutated Colorectal Cancers
Q39140529Dual Inhibition of PI3K-AKT-mTOR- and RAF-MEK-ERK-signaling is synergistic in cholangiocarcinoma and reverses acquired resistance to MEK-inhibitors
Q50981985Dual blockade of PI3K/AKT/mTOR (NVP-BEZ235) and Ras/Raf/MEK (AZD6244) pathways synergistically inhibit growth of primary endometrioid endometrial carcinoma cultures, whereas NVP-BEZ235 reduces tumor growth in the corresponding xenograft models
Q34644692Dual inhibition of phosphatidylinositol 3-kinase/mammalian target of rapamycin and mitogen activated protein kinase pathways in non-Hodgkin lymphoma
Q37038401Dysfunctional oxidative phosphorylation makes malignant melanoma cells addicted to glycolysis driven by the (V600E)BRAF oncogene.
Q40457293ERK Signaling Is Essential for Macrophage Development.
Q41882870ERK1/2 signalling protects against apoptosis following endoplasmic reticulum stress but cannot provide long-term protection against BAX/BAK-independent cell death.
Q36507554Effect of SMURF2 targeting on susceptibility to MEK inhibitors in melanoma
Q39178760Effect of selumetinib on the growth of anastrozole-resistant tumors
Q35213763Effects of ulinastatin and docetaxel on breast cancer invasion and expression of uPA, uPAR and ERK
Q64075146Elucidating the transcriptional program of feline injection-site sarcoma using a cross-species mRNA-sequencing approach
Q37691441Emerging MEK inhibitors.
Q38172608Emerging protein kinase inhibitors for non-small cell lung cancer
Q37421296Enhanced anti-tumour activity of the combination of the novel MEK inhibitor WX-554 and the novel PI3K inhibitor WX-037.
Q38973740Enhanced dependency of KRAS-mutant colorectal cancer cells on RAD51-dependent homologous recombination repair identified from genetic interactions in Saccharomyces cerevisiae.
Q35146186Enhancement of 5-Fluorouracil-induced In Vitro and In Vivo Radiosensitization with MEK Inhibition
Q35675442Evaluation of efficacy of a new MEK inhibitor, RO4987655, in human tumor xenografts by [(18)F] FDG-PET imaging combined with proteomic approaches.
Q41697013Ex vivo treatment of patient biopsies as a novel method to assess colorectal tumour response to the MEK1/2 inhibitor, Selumetinib
Q39623358Exploiting the origins of Ras mediated squamous cell carcinoma to develop novel therapeutic interventions
Q33767083FOXD3 is a mutant B-RAF-regulated inhibitor of G(1)-S progression in melanoma cells
Q33698374From basic research to clinical development of MEK1/2 inhibitors for cancer therapy
Q37999967From genes to drugs: targeted strategies for melanoma
Q47356048Generation of stable PDX derived cell lines using conditional reprogramming
Q36563659Genetics of melanoma
Q43189894Genome-wide identification of chemosensitive single nucleotide polymorphism markers in colorectal cancers
Q36628641Glucocorticoid-induced apoptosis of healthy and malignant lymphocytes
Q36618983Grifolin directly targets ERK1/2 to epigenetically suppress cancer cell metastasis
Q37632192HER2, MET and FGFR2 oncogenic driver alterations define distinct molecular segments for targeted therapies in gastric carcinoma
Q92084382Helping the Released Guardian: Drug Combinations for Supporting the Anticancer Activity of HDM2 (MDM2) Antagonists
Q33717222High level of AKT activity is associated with resistance to MEK inhibitor AZD6244 (ARRY-142886)
Q37635287High-throughput mutation profiling of CTCL samples reveals KRAS and NRAS mutations sensitizing tumors toward inhibition of the RAS/RAF/MEK signaling cascade.
Q55079595Homoharringtonine induced immune alteration for an Efficient Anti-tumor Response in Mouse Models of Non-small Cell Lung Adenocarcinoma Expressing Kras Mutation.
Q64921561Hyaluronic Acid Layered Chimeric Nanoparticles: Targeting MAPK-PI3K Signaling Hub in Colon Cancer Cells.
Q41782221Identification of DYRK1B as a substrate of ERK1/2 and characterisation of the kinase activity of DYRK1B mutants from cancer and metabolic syndrome.
Q34129528Identification of common predictive markers of in vitro response to the Mek inhibitor selumetinib (AZD6244; ARRY-142886) in human breast cancer and non-small cell lung cancer cell lines
Q37596249Identification of predictive markers of response to the MEK1/2 inhibitor selumetinib (AZD6244) in K-ras-mutated colorectal cancer.
Q49787333Implications of KRAS mutations in acquired resistance to treatment in NSCLC.
Q33557673In vitro and in vivo radiosensitization with AZD6244 (ARRY-142886), an inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase 1/2 kinase
Q38402255Induction of immunoglobulin transcription factor 2 and resistance to MEK inhibitor in melanoma cells
Q35944601Inhibition of Ras for Cancer Treatment: The Search Continues
Q39396267Inhibition of metadherin sensitizes breast cancer cells to AZD6244
Q41345175Inhibition of the PI3K/AKT/mTOR pathway activates autophagy and compensatory Ras/Raf/MEK/ERK signalling in prostate cancer
Q34415484Initial testing (stage 1) of AZD6244 (ARRY-142886) by the Pediatric Preclinical Testing Program.
Q34273541Intrinsic resistance to selumetinib, a selective inhibitor of MEK1/2, by cAMP-dependent protein kinase A activation in human lung and colorectal cancer cells
Q34544971KRAS driven expression signature has prognostic power superior to mutation status in non-small cell lung cancer
Q38390027KRAS mutant NSCLC, a new opportunity for the synthetic lethality therapeutic approach
Q42062700KRAS mutational subtype and copy number predict in vitro response of human pancreatic cancer cell lines to MEK inhibition
Q49887897KRAS oncogene in non-small cell lung cancer: clinical perspectives on the treatment of an old target
Q38669282KRAS-Mutant Lung Cancers in the Era of Targeted Therapy
Q39860040KRAS/BRAF mutation status and ERK1/2 activation as biomarkers for MEK1/2 inhibitor therapy in colorectal cancer
Q38254501MEK inhibition in non-small cell lung cancer
Q92531455MEK inhibition remodels the active chromatin landscape and induces SOX10 genomic recruitment in BRAF(V600E) mutant melanoma cells
Q38092584MEK inhibitors as a chemotherapeutic intervention in multiple myeloma
Q56889985MEK inhibitors for the treatment of NRAS mutant melanoma
Q47318847MEK inhibitors under development for treatment of non-small-cell lung cancer
Q27777362MEK1 mutations confer resistance to MEK and B-RAF inhibition
Q36328021MEK1/2 Inhibitors: Molecular Activity and Resistance Mechanisms
Q36976683MEK1/2 inhibition enhances the radiosensitivity of cancer cells by downregulating survival and growth signals mediated by EGFR ligands
Q37179748MEK1/2 inhibition suppresses tamoxifen toxicity on CNS glial progenitor cells.
Q35872321MEK1/2 inhibitor selumetinib (AZD6244) inhibits growth of ovarian clear cell carcinoma in a PEA-15-dependent manner in a mouse xenograft model
Q38179145MEK1/2 inhibitors in the treatment of gynecologic malignancies.
Q89303329Management of KRAS-Mutant Non-Small Cell Lung Cancer in the Era of Precision Medicine
Q38007869Mechanisms of acquired resistance to ERK1/2 pathway inhibitors
Q91891857Mechanisms of suppression of cell growth by dual inhibition of ALK and MEK in ALK-positive non-small cell lung cancer
Q26738377Metastatic disease from uveal melanoma: treatment options and future prospects
Q28468669Microvesicle removal of anticancer drugs contributes to drug resistance in human pancreatic cancer cells
Q36979035Mitogen-activated protein kinase kinase 1/2 inhibitors and 17-allylamino-17-demethoxygeldanamycin synergize to kill human gastrointestinal tumor cells in vitro via suppression of c-FLIP-s levels and activation of CD95.
Q30433431Molecular genesis of non-muscle-invasive urothelial carcinoma (NMIUC)
Q34052520Molecular pathways: targeting NRAS in melanoma and acute myelogenous leukemia
Q42330675NRF2 Promotes Tumor Maintenance by Modulating mRNA Translation in Pancreatic Cancer
Q37888981New Strategies in Metastatic Melanoma: Oncogene-Defined Taxonomy Leads to Therapeutic Advances
Q37345841New treatment options for advanced pancreatic cancer
Q34671658Novel Approaches to Treatment of Advanced Melanoma: A Review on Targeted Therapy and Immunotherapy
Q38799963Novel investigational therapies for treating biliary tract carcinoma
Q37828536Novel mitogen-activated protein kinase kinase inhibitors
Q34774990Oncogenic Kras Promotes Chemotherapy-Induced Growth Factor Shedding via ADAM17
Q50061136Oncogenic RAC1 and NRAS drive resistance to endoplasmic reticulum stress through MEK/ERK signalling.
Q35896845Optimized sgRNA design to maximize activity and minimize off-target effects of CRISPR-Cas9.
Q44502910Overcoming resistance to single-agent therapy for oncogenic BRAF gene fusions via combinatorial targeting of MAPK and PI3K/mTOR signaling pathways.
Q51650705Overproduction of IGF-2 drives a subset of colorectal cancer cells, which specifically respond to an anti-IGF therapeutic antibody and combination therapies
Q100490609Overview of current targeted therapy in gallbladder cancer
Q35096292Pharmacokinetics and pharmacodynamics of AZD6244 (ARRY-142886) in tumor-bearing nude mice
Q54982668Pharmacology of Pimasertib, A Selective MEK1/2 Inhibitor.
Q27851426Phase I pharmacokinetic and pharmacodynamic study of the oral, small-molecule mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancers
Q35023451Phase II Study of the Mitogen-Activated Protein Kinase 1/2 Inhibitor Selumetinib in Patients With Advanced Hepatocellular Carcinoma
Q37505185Phase II efficacy and pharmacogenomic study of Selumetinib (AZD6244; ARRY-142886) in iodine-131 refractory papillary thyroid carcinoma with or without follicular elements
Q27853084Phase II study of selumetinib (AZD6244, ARRY-142886) plus irinotecan as second-line therapy in patients with K-RAS mutated colorectal cancer.
Q27852623Phase II study of the oral MEK inhibitor selumetinib in advanced acute myelogenous leukemia: a University of Chicago phase II consortium trial.
Q34633455Phase II, open-label, randomized trial of the MEK1/2 inhibitor selumetinib as monotherapy versus temozolomide in patients with advanced melanoma
Q38757884Phosphoproteomics Reveals MAPK Inhibitors Enhance MET- and EGFR-Driven AKT Signaling in KRAS-Mutant Lung Cancer.
Q33729778Population Pharmacokinetics of Selumetinib and Its Metabolite N-desmethyl-selumetinib in Adult Patients With Advanced Solid Tumors and Children With Low-Grade Gliomas
Q37421431Preclinical activity of the rational combination of selumetinib (AZD6244) in combination with vorinostat in KRAS-mutant colorectal cancer models.
Q38256348Profile of selumetinib and its potential in the treatment of melanoma
Q34749852Prognostic and Predictive Value of KRAS Mutations in Advanced Non-Small Cell Lung Cancer
Q50938980Protein Tyrosine Signaling and its Potential Therapeutic Implications in Carcinogenesis.
Q38132900Protein kinase inhibitors in melanoma
Q34580110Ras pathway mutations are prevalent in relapsed childhood acute lymphoblastic leukemia and confer sensitivity to MEK inhibition
Q38227885Ras/Raf/MEK/ERK Pathway Activation in Childhood Acute Lymphoblastic Leukemia and Its Therapeutic Targeting
Q34307356Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR cascade inhibitors: how mutations can result in therapy resistance and how to overcome resistance
Q35679353Ras/Raf/MEK/ERK and PI3K/PTEN/Akt/mTOR inhibitors: rationale and importance to inhibiting these pathways in human health
Q39140763Rational Combination of a MEK Inhibitor, Selumetinib, and the Wnt/Calcium Pathway Modulator, Cyclosporin A, in Preclinical Models of Colorectal Cancer
Q42613657Regulation of autophagy by ceramide-CD95-PERK signaling
Q35971560Regulation of ubiquitination-mediated protein degradation by survival kinases in cancer
Q54109659Research Progress of KRAS Mutation in Non-small Cell Lung Cancer
Q34417585Resistance to Selumetinib (AZD6244) in colorectal cancer cell lines is mediated by p70S6K and RPS6 activation.
Q38723005Role of key genetic mutations on increasing migration of brain cancer cells through confinement.
Q47432675SELECT-2: a phase II, double-blind, randomized, placebo-controlled study to assess the efficacy of selumetinib plus docetaxel as a second-line treatment of patients with advanced or metastatic non-small-cell lung cancer
Q35035656SMK-17, a MEK1/2-specific inhibitor, selectively induces apoptosis in β-catenin-mutated tumors
Q54310457Selumetinib for the treatment of cancer
Q38798084Selumetinib for the treatment of metastatic uveal melanoma: past and future perspectives
Q38663069Selumetinib for the treatment of non-small cell lung cancer
Q38836927Selumetinib in the treatment of non-small-cell lung cancer
Q34652628Selumetinib plus dacarbazine versus placebo plus dacarbazine as first-line treatment for BRAF-mutant metastatic melanoma: a phase 2 double-blind randomised study
Q27851971Selumetinib plus docetaxel for KRAS-mutant advanced non-small-cell lung cancer: a randomised, multicentre, placebo-controlled, phase 2 study
Q39466460Selumetinib: A Promising Pharmacologic Approach for KRAS -Mutant Advanced Non-Small-Cell Lung Cancer
Q36560775Sensitivity to the MEK inhibitor E6201 in melanoma cells is associated with mutant BRAF and wildtype PTEN status
Q38747573Signaling pathways as therapeutic targets in biliary tract cancer.
Q38090664Small-molecule inhibitors binding to protein kinase. Part II: the novel pharmacophore approach of type II and type III inhibition
Q34104350Sorafenib Activates CD95 and Promotes Autophagy and Cell Death via Src Family Kinases in Gastrointestinal Tumor Cells
Q37268127Sorafenib and vorinostat kill colon cancer cells by CD95-dependent and -independent mechanisms
Q39725762Sorafenib combined vitamin K induces apoptosis in human pancreatic cancer cell lines through RAF/MEK/ERK and c-Jun NH2-terminal kinase pathways.
Q38585847Stamping out RAF and MEK1/2 to inhibit the ERK1/2 pathway: an emerging threat to anticancer therapy.
Q30384829Study design and rationale for a randomised, placebo-controlled, double-blind study to assess the efficacy of selumetinib (AZD6244; ARRY-142886) in combination with dacarbazine in patients with metastatic uveal melanoma (SUMIT).
Q35691935Synergistic Effect between Erlotinib and MEK Inhibitors in KRAS Wild-Type Human Pancreatic Cancer Cells
Q39206681Synergistic anticancer activity of HS-173, a novel PI3K inhibitor in combination with Sorafenib against pancreatic cancer cells
Q38702245Synergistic effect of MEK inhibitor and metformin combination in low grade serous ovarian cancer.
Q35018805Synergistic effects of concurrent blockade of PI3K and MEK pathways in pancreatic cancer preclinical models
Q92862513Synthesis and biological evaluation of novel N-(piperazin-1-yl)alkyl-1H-dibenzo[a,c]carbazole derivatives of dehydroabietic acid as potential MEK inhibitors
Q35584299Systematic review of medical treatment in melanoma: current status and future prospects.
Q36233325Targeted Therapy for MAPK Alterations in Pediatric Gliomas
Q38127728Targeted therapy for NSCLC with driver mutations
Q54783170Targeting RAS and PI3K in lung cancer.
Q38272894Targeting RAS-ERK signalling in cancer: promises and challenges
Q38124821Targeting RAS/RAF/MEK/ERK signaling in metastatic melanoma
Q37629722Targeting mitogen-activated protein kinase kinase (MEK) in solid tumors
Q38554422Targeting non-receptor tyrosine kinases using small molecule inhibitors: an overview of recent advances
Q38388217Targeting of MEK in lung cancer therapeutics
Q36068326Targeting the FOXO1/KLF6 axis regulates EGFR signaling and treatment response.
Q38799845Targeting the KRAS Pathway in Non-Small Cell Lung Cancer
Q38682370Targeting the KRAS variant for treatment of non-small cell lung cancer: potential therapeutic applications
Q37745182Targeting the MAPK pathway in melanoma: why some approaches succeed and other fail
Q36278239Targeting the MAPK-RAS-RAF signaling pathway in cancer therapy
Q39270291Targeting the Ras/Raf/MEK/ERK pathway in hepatocellular carcinoma
Q27853330Targeting the mTOR Complex by Everolimus in NRAS Mutant Neuroblastoma
Q38104439That which does not kill me makes me stronger; combining ERK1/2 pathway inhibitors and BH3 mimetics to kill tumour cells and prevent acquired resistance.
Q38621231The MEK inhibitor selumetinib complements CTLA-4 blockade by reprogramming the tumor immune microenvironment
Q35835097The MEK1/2 inhibitor, selumetinib (AZD6244; ARRY-142886), enhances anti-tumour efficacy when combined with conventional chemotherapeutic agents in human tumour xenograft models
Q38397326The RAF-MEK-ERK pathway: targeting ERK to overcome obstacles to effective cancer therapy.
Q38788201The antitumor effect of TIG3 in liver cancer cells is involved in ERK1/2 inhibition.
Q38212717The clinical development of MEK inhibitors
Q35140947The novel anti-MEK small molecule AZD6244 induces BIM-dependent and AKT-independent apoptosis in diffuse large B-cell lymphoma
Q35793641The oncogenic receptor ErbB2 modulates gemcitabine and irinotecan/SN-38 chemoresistance of human pancreatic cancer cells via hCNT1 transporter and multidrug-resistance associated protein MRP-2.
Q39380338The synergistic interaction of MEK and PI3K inhibitors is modulated by mTOR inhibition
Q37951743Towards new therapeutic approaches for malignant melanoma
Q38300326Transcriptional pathway signatures predict MEK addiction and response to selumetinib (AZD6244)
Q38787635Tumor cells with KRAS or BRAF mutations or ERK5/MAPK7 amplification are not addicted to ERK5 activity for cell proliferation.
Q37133208Tumor therapy with a urokinase plasminogen activator-activated anthrax lethal toxin alone and in combination with paclitaxel
Q39301436Tumour cell responses to new fibroblast growth factor receptor tyrosine kinase inhibitors and identification of a gatekeeper mutation in FGFR3 as a mechanism of acquired resistance
Q37290943Tumour cell survival signalling by the ERK1/2 pathway
Q37034487Understanding signaling cascades in melanoma
Q34438500Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R
Q39680200Vorinostat and sorafenib increase CD95 activation in gastrointestinal tumor cells through a Ca(2+)-de novo ceramide-PP2A-reactive oxygen species-dependent signaling pathway
Q37172903Vorinostat and sorafenib increase ER stress, autophagy and apoptosis via ceramide-dependent CD95 and PERK activation
Q36922674Vorinostat and sorafenib synergistically kill tumor cells via FLIP suppression and CD95 activation
Q44561867Whole genome gene copy number profiling of gastric cancer identifies PAK1 and KRAS gene amplification as therapy targets

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