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Cellular and Molecular Life Sciences, ISSN 1420-682X, 3/2016, Volume 73, Issue 5, pp. 985 - 1001
Journal Article
Journal Article
International Journal of Cancer, ISSN 0020-7136, 11/2013, Volume 133, Issue 9, pp. 2089 - 2101
The RAS/RAF/MEK/MAPK and the PTEN/PI3K/AKT/mTOR pathways are key regulators of proliferation and survival in human cancer cells. Selective inhibitors of... 
lung cancer | colorectal cancer | combination of molecular targeted therapies | MEK inhibitors | SIGNALING PATHWAYS | ACTIVATION | RAS | AZD6244 | ARRY-142886 | IDENTIFICATION | PI3K | ONCOLOGY | SELUMETINIB | KRAS | TUMOR-GROWTH | Lung Neoplasms - drug therapy | Oligonucleotide Array Sequence Analysis | TOR Serine-Threonine Kinases - metabolism | Apoptosis - drug effects | Phosphatidylinositol 3-Kinase - antagonists & inhibitors | Humans | Lung Neoplasms - metabolism | Lung Neoplasms - pathology | Gene Expression Profiling | TOR Serine-Threonine Kinases - antagonists & inhibitors | Colorectal Neoplasms - drug therapy | Biomarkers, Tumor - metabolism | Female | Tumor Cells, Cultured | Proto-Oncogene Proteins c-akt - metabolism | Phosphatidylinositol 3-Kinase - metabolism | Colorectal Neoplasms - metabolism | MAP Kinase Kinase 1 - antagonists & inhibitors | PTEN Phosphohydrolase - metabolism | MAP Kinase Kinase 1 - metabolism | MAP Kinase Kinase 2 - metabolism | Blotting, Western | Xenograft Model Antitumor Assays | Animals | Signal Transduction - drug effects | MAP Kinase Kinase 2 - antagonists & inhibitors | Biomarkers, Tumor - genetics | Cell Proliferation - drug effects | Mice | Mice, Inbred BALB C | Phenylurea Compounds - pharmacology | Protein Kinase Inhibitors - pharmacology | Pyridines - pharmacology | Cell Cycle - drug effects | Colorectal Neoplasms - pathology | Proto-Oncogene Proteins c-akt - antagonists & inhibitors | Drug Resistance, Neoplasm - drug effects | Colorectal cancer | Tumors | Chemotherapy | Pharmacology | Kinases | Lung cancer
Journal Article
Clinical Cancer Research, ISSN 1078-0432, 01/2013, Volume 19, Issue 1, pp. 279 - 290
Journal Article
Cancer, ISSN 0008-543X, 06/2017, Volume 123, Issue S11, pp. 2118 - 2129
The identification of driver mutations in melanoma has changed the field of cancer treatment. BRAF and NRAS mutations are predominant in melanoma and lead to... 
targeted therapy | phosphatidylinositol 3‐kinase (PI3K)/protein kinase B (AKT) pathway | BRAF inhibitors | mitogen‐activated protein kinase kinase (MEK) inhibitors | immunotherapy | melanoma | mitogen‐activated protein kinase (MAPK) pathway | phosphatidylinositol 3-kinase (PI3K)/protein kinase B (AKT) pathway | mitogen-activated protein kinase kinase (MEK) inhibitors | mitogen-activated protein kinase (MAPK) pathway | MUTANT MELANOMA | PD-L1 EXPRESSION | ACQUIRED-RESISTANCE | OPEN-LABEL | MEK INHIBITORS | METASTATIC MELANOMA | PHASE-II TRIAL | ONCOLOGY | CUTANEOUS MELANOMA | BRAF INHIBITOR RESISTANCE | RAF INHIBITORS | Niacinamide - analogs & derivatives | Immunotherapy - methods | Skin Neoplasms - drug therapy | Humans | Ipilimumab | Antibodies, Monoclonal - therapeutic use | Drug Resistance, Neoplasm | Programmed Cell Death 1 Receptor - antagonists & inhibitors | Antineoplastic Agents - therapeutic use | Molecular Targeted Therapy | Phosphatidylinositol 3-Kinases - antagonists & inhibitors | Proto-Oncogene Proteins c-akt - genetics | MAP Kinase Kinase 1 - genetics | Melanoma - genetics | Benzimidazoles - therapeutic use | MAP Kinase Kinase 1 - antagonists & inhibitors | Antibodies, Monoclonal, Humanized - therapeutic use | Drug Administration Schedule | Signal Transduction | Niacinamide - therapeutic use | Phenylurea Compounds - therapeutic use | Phosphatidylinositol 3-Kinases - genetics | Proto-Oncogene Proteins B-raf - antagonists & inhibitors | Sulfonamides - therapeutic use | Antineoplastic Combined Chemotherapy Protocols - therapeutic use | Protein Kinase Inhibitors - therapeutic use | Proto-Oncogene Proteins B-raf - genetics | Pyrimidines - therapeutic use | Quinazolines - therapeutic use | Melanoma - drug therapy | Skin Neoplasms - genetics | Indoles - therapeutic use | CTLA-4 Antigen - antagonists & inhibitors | Proto-Oncogene Proteins c-akt - antagonists & inhibitors | Therapy | Melanoma | MAP kinase | AKT protein | Drug resistance | Kinases | Cancer therapies | Patients | 1-Phosphatidylinositol 3-kinase | Metastases | Signal transduction | Inhibitors | Pathways | New combinations | Effectors | Mutation | Cancer
Journal Article
Biochemical Pharmacology, ISSN 0006-2952, 08/2014, Volume 90, Issue 3, pp. 197 - 207
While PI3K/AKT/mTOR pathway is altered in a variety of cancers including non small cell lung cancer, abnormalities in this pathway are more common in squamous... 
mTOR | AKT | SQCLC | PI3K | NSCLC | MAMMALIAN TARGET | I PI3K INHIBITOR | ONCOGENE MUTATIONS | AKT INHIBITOR | ANTITUMOR-ACTIVITY | DOSE-ESCALATION | TYROSINE KINASE INHIBITOR | PHARMACOLOGY & PHARMACY | ADVANCED NSCLC | PHASE-I | MTOR INHIBITOR | Lung Neoplasms - drug therapy | TOR Serine-Threonine Kinases - metabolism | Phosphatidylinositol 3-Kinase - antagonists & inhibitors | Humans | Lung Neoplasms - metabolism | Antineoplastic Combined Chemotherapy Protocols - adverse effects | Drug Resistance, Neoplasm | Neoplasm Proteins - antagonists & inhibitors | Antineoplastic Agents - therapeutic use | Antineoplastic Agents - administration & dosage | Neoplasm Proteins - metabolism | Enzyme Inhibitors - administration & dosage | TOR Serine-Threonine Kinases - antagonists & inhibitors | Antineoplastic Agents - adverse effects | Proto-Oncogene Proteins c-akt - metabolism | Phosphatidylinositol 3-Kinase - metabolism | Enzyme Inhibitors - adverse effects | Molecular Targeted Therapy - adverse effects | Lung Neoplasms - enzymology | Carcinoma, Non-Small-Cell Lung - metabolism | Enzyme Inhibitors - therapeutic use | Animals | Signal Transduction - drug effects | Antineoplastic Combined Chemotherapy Protocols - therapeutic use | Carcinoma, Non-Small-Cell Lung - drug therapy | Carcinoma, Non-Small-Cell Lung - enzymology | Proto-Oncogene Proteins c-akt - antagonists & inhibitors
Journal Article
CLINICAL CANCER RESEARCH, ISSN 1078-0432, 01/2017, Volume 23, Issue 1, pp. 26 - 34
Purpose: Alpelisib, a selective oral inhibitor of the class I PI3K catalytic subunit p110 alpha, has shown synergistic antitumor activity with endocrine... 
ACTIVATION | NVP-BYL719 | PIK3CA MUTATIONS | PI3K | ONCOLOGY | PHOSPHATIDYLINOSITOL 3-KINASE | GROWTH | ESTROGEN DEPRIVATION | RESISTANCE | ALPHA | TUMORS | Triazoles - administration & dosage | Receptors, Estrogen - metabolism | Humans | Middle Aged | Receptor, ErbB-2 - metabolism | Antineoplastic Combined Chemotherapy Protocols - adverse effects | Thiazoles - administration & dosage | Phosphatidylinositol 3-Kinases - antagonists & inhibitors | Receptor, Fibroblast Growth Factor, Type 1 - genetics | Biomarkers, Tumor | Breast Neoplasms - metabolism | Nitriles - administration & dosage | Neoplasm Metastasis | DNA Mutational Analysis | Adult | Female | Aromatase Inhibitors - administration & dosage | Receptors, Estrogen - genetics | In Situ Hybridization, Fluorescence | Treatment Outcome | Breast Neoplasms - drug therapy | Phosphatidylinositol 3-Kinases - genetics | Maximum Tolerated Dose | Breast Neoplasms - genetics | Antineoplastic Combined Chemotherapy Protocols - therapeutic use | Breast Neoplasms - pathology | Cell Line, Tumor | Aged | Mutation | Neoplasm Staging | Letrozole | Therapy | Toxicity | p53 Protein | Exanthema | Clinical trials | Metastasis | K-Ras protein | Metastases | Gene sequencing | Anticancer properties | Hyperglycemia | Safety engineering | Catalysis | Fibroblast growth factor receptor 1 | Deoxyribonucleic acid--DNA | Diarrhea | Endocrine therapy | Fatigue | Nausea | Breast cancer | Patients | ErbB-2 protein | 1-Phosphatidylinositol 3-kinase | Inhibitors | Experimental design | Breast | Antitumor activity | Tumors | DNA sequencing | Cancer
Journal Article
Anti-Cancer Agents in Medicinal Chemistry, ISSN 1871-5206, 2010, Volume 10, Issue 7, pp. 571 - 581
Journal Article
Biochemical Journal, ISSN 0264-6021, 12/2007, Volume 408, Issue 3, pp. 297 - 315
The specificities of 65 compounds reported to be relatively specific inhibitors of protein kinases have been profiled against a panel of 70-80 protein kinases.... 
Drug discovery | Kinase profiling | Protein kinase | Anti-cancer drugs | Inhibitor specificity | RHO-ASSOCIATED KINASE | TUMOR PROGRESSION | FAMILY-MEMBERS | BIOCHEMISTRY & MOLECULAR BIOLOGY | CELL-PROLIFERATION | protein kinase | P38 MAP KINASE | CYCLIN-DEPENDENT KINASES | RECEPTOR TYROSINE KINASES | drug discovery | kinase profiling | SB 203580 | anti-cancer drugs | ISOFORMS IN-VITRO | P90 RSK | inhibitor specificity | Amino Acid Sequence | Cell Line | Phosphorylation | Recombinant Proteins - antagonists & inhibitors | Animals | Mitogen-Activated Protein Kinases - antagonists & inhibitors | Humans | Drug Design | Protein Kinase Inhibitors - pharmacology | Enzyme Activation | Mitogen-Activated Protein Kinases - metabolism | Spodoptera | Yes1, Yamaguchi sarcoma viral oncogene homologue 1 | CSK, C-terminal Src kinase | Lck, lymphocyte cell-specific protein-tyrosine kinase | EGF, epidermal growth factor | FGF-R, fibroblast-growth-factor receptor | PAK, p21-activated protein kinase | PDK, 3-phosphoinositide-dependent protein kinase | PI3K, phosphatidylinositol (phosphoinositide) 3-kinase | NEK, NIMA (never in mitosis in Aspergillus nidulans)-related kinase | RSK, p90 ribosomal S6 kinase | HEK-293 cells, human embryonic kidney-293 cells | VEGF, vascular endothelial growth factor (vasoendothelial growth factor) | EF2K, elongation-factor-2 kinase | CK, casein kinase | PTEN, phosphatase and tensin homologue deleted on chromosome 10 | ERK, extracellular-signal-regulated kinase | ATM, ataxia telangiectasia mutated | SRPK, serine-arginine protein kinase | IL-1, interleukin 1 | MNK, MAPK-integrating protein kinase | ROCK, Rho-dependent protein kinase | CaMKK, CaMK kinase | GST, glutathione transferase | MKK1, MAPK kinase-1 (also called MEK1, MAPK or ERK kinase 1) | GAK, cyclin G-associated kinase | FMK, fluoromethylketone | MST, mammalian homologue Ste20-like kinase | PKA, cAMP-dependent protein kinase | FKBP, FK506-binding protein | PPAR, peroxisome-proliferator-activated receptor | IKK, inhibitory κB kinase | PH, pleckstrin homology | MBP, myelin basic protein | AICAR, aminoimidazole-4-carboxamide-1-β-D-ribofuranoside | MAPKAP-K, MAPK-activated protein kinase | Sf21, Spodoptera frugiperda (fall armyworm) 21 | MARK, microtubule-affinity-regulating kinase | PIM, provirus integration site for Moloney murine leukaemia virus | LPS, lipopolysaccharide | MSK, mitogen- and stress-activated protein kinase | MAPK, mitogen-activated protein kinase | MELK, maternal embryonic leucine-zipper kinase | His6, hexahistidine | CAK, cyclin-dependent kinase-activating kinase | Eph-A2, Ephrin A2 receptor | PLK, polo-like kinase | ATF2, activating transcription factor 2 | PKD, protein kinase D | Src, sarcoma kinase | AMPK, AMP-activated protein kinase | MMS, methyl methanesulfonate | CHK, checkpoint kinase | JNK, c-Jun N-terminal kinase | TORC1, mTOR (mammalian target of rapamycin)–raptor (regulatory associated protein of mTOR) complex | BRSK, brain-specific kinase | RIP2, receptor-interacting protein 2 | IGF-1, insulin-like growth factor-1 | S6K1, S6 kinase 1 | DYRK, dual-specificity tyrosine-phosphorylated and -regulated kinase | HIPK, homeodomain-interacting protein kinase | ZMP, aminoimidazole-4-carboxamide-1-β-D-ribofuranoside monophosphate | PRAK, p38-regulated activated kinase | PKC, protein kinase C | Src-I1, Src inhibitor 1 | TANK, TRAF (tumour-necrosis-factor-receptor-associated factor)-family-member-associated nuclear factor κB activator | NFAT, nuclear factor for activated T-cells | PHK, phosphorylase kinase | GSK3, glycogen synthase kinase 3 | PKB, protein kinase B (also called Akt) | CaMK, calmodulin-dependent kinase | CDK, cyclin-dependent protein kinase | NDRG, N-myc downstream-regulated gene | SmMLCK, smooth-muscle myosin light-chain kinase | TBK1, TANK-binding kinase 1 | PRK, protein kinase C-related kinase | SGK, serum- and glucocorticoid-induced kinase
Journal Article