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1. Full Text Wnt/β-catenin pathway regulates MGMT gene expression in cancer and inhibition of Wnt signalling prevents chemoresistance
by Wickström, Malin and Dyberg, Cecilia and Milosevic, Jelena and Einvik, Christer and Calero, Raul and Sveinbjörnsson, Baldur and Sandén, Emma and Darabi, Anna and Siesjö, Peter and Kool, Marcel and Kogner, Per and Baryawno, Ninib and Johnsen, John Inge and Neurosurgery and Neurokirurgi and Lund University and BioCARE: Biomarkers in Cancer Medicine improving Health Care, Education and Innovation and Lunds universitet
Nature Communications, ISSN 2041-1723, 11/2015, Volume 6, Issue 1, pp. 8904 - 8904
The DNA repair enzyme O6-methylguanine- DNA methyltransferase (MGMT) is commonly overexpressed in cancers and is implicated in the development of... 
MALIGNANT GLIOMA | CELLS | GLIOBLASTOMA | METHYLTRANSFERASE | MULTIDISCIPLINARY SCIENCES | RESISTANCE | THERAPEUTIC TARGETS | FAMILIAL ADENOMATOUS POLYPOSIS | MECHANISMS | TUMOR-GROWTH | TEMOZOLOMIDE | Index Medicus | VDP | Klinisk medisinske fag: 750 | Onkologi: 762 | Oncology: 762 | Medisinske Fag: 700 | Clinical medical disciplines: 750 | Medical disciplines: 700 | Cell and Molecular Biology | Basic Medicine | Medical and Health Sciences | Medicin och hälsovetenskap | Cell- och molekylärbiologi | Medicinska och farmaceutiska grundvetenskaper
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2. Full Text WNT signaling drives cholangiocarcinoma growth and can be pharmacologically inhibited
by Boulter, Luke and Guest, Rachel V and Kendall, Timothy J and Wilson, David H and Wojtacha, Davina and Robson, Andrew J and Ridgway, Rachel A and Samuel, Kay and Van Rooijen, Nico and Barry, Simon T and Wigmore, Stephen J and Sansom, Owen J and Forbes, Stuart J
Journal of Clinical Investigation, ISSN 0021-9738, 03/2015, Volume 125, Issue 3, pp. 1269 - 1285
Cholangiocarcinoma (CC) is typically diagnosed at an advanced stage and is refractory to surgical intervention and chemotherapy. Despite a global increase in... 
BREAST-CANCER | MEDICINE, RESEARCH & EXPERIMENTAL | INTRAHEPATIC CHOLANGIOCARCINOMA | THIOACETAMIDE | PORCUPINE | LIVER | BILIARY | BETA-CATENIN | RAT CHOLANGIOCARCINOMA | PROGRESSION | CANCER STEM-CELLS | Anisoles - pharmacology | Humans | Male | Cholangiocarcinoma - metabolism | Bile Ducts, Intrahepatic - metabolism | Keratins - metabolism | Pyrimidinones - pharmacology | Antineoplastic Agents - pharmacology | Benzeneacetamides - pharmacology | Wnt Signaling Pathway | Bile Duct Neoplasms - drug therapy | Cell Survival - drug effects | Aniline Compounds - pharmacology | Bile Duct Neoplasms - metabolism | Pyrimidines - pharmacology | Rats, Sprague-Dawley | beta Catenin - metabolism | Heterocyclic Compounds, 2-Ring - pharmacology | Xenograft Model Antitumor Assays | Bridged Bicyclo Compounds, Heterocyclic - pharmacology | Macrophages - metabolism | Animals | Cholangiocarcinoma - drug therapy | Mice, Nude | Tamoxifen - pharmacology | Cell Line, Tumor | Macrophages - drug effects | Cell Proliferation - drug effects | Clodronic Acid - administration & dosage | Pyridines - pharmacology | Liposomes | Physiological aspects | Research | Tumor proteins | Wnt proteins | Oncology, Experimental | Cancer | Heparan sulfate | Medical research | Liver | Gene expression | Cancer therapies | Studies | Councils | Medical prognosis | Cell cycle | Ligands | Mutation | Tumors
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3. Full Text Combined treatment with morphine and Δ9-tetrahydrocannabinol in rhesus monkeys: Antinociceptive tolerance and withdrawal
by Gerak, L.R and France, C.P
Journal of Pharmacology and Experimental Therapeutics, ISSN 0022-3565, 05/2016, Volume 357, Issue 2, pp. 357 - 366
Opioid receptor agonists are effective for treating pain; however, tolerance and dependence can develop with repeated use. Combining opioids with cannabinoids... 
Analgesics - pharmacology | Opioid-Related Disorders - psychology | Morphine - pharmacology | Drug Tolerance | Analgesics, Opioid - pharmacology | Morpholines - pharmacology | Pain Measurement - drug effects | Macaca mulatta | Cannabinoid Receptor Agonists - pharmacology | 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer - pharmacology | Naphthalenes - pharmacology | Dose-Response Relationship, Drug | Heart Rate - drug effects | Animals | Benzoxazines - pharmacology | Cyclohexanols - pharmacology | Dronabinol - pharmacology | Substance Withdrawal Syndrome - psychology | Behavioral Pharmacology
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4. Full Text Neurokinin B Activates Arcuate Kisspeptin Neurons Through Multiple Tachykinin Receptors in the Male Mouse
by de Croft, Simon and Boehm, Ulrich and Herbison, Allan E
Endocrinology, ISSN 0013-7227, 08/2013, Volume 154, Issue 8, pp. 2750 - 2760
Kisspeptin neurons located in the arcuate nucleus (ARN) coexpress dynorphin and neurokinin B (NKB) and may interact to influence gonadotropin secretion. Using... 
GNRH PULSE-GENERATOR | HORMONE SECRETION | MORPHOLOGIC EVIDENCE | FEMALE MOUSE | IN-VITRO | MESSENGER-RNA EXPRESSION | PHARMACOLOGICAL CHARACTERIZATION | ENDOCRINOLOGY & METABOLISM | MEDIAN-EMINENCE | KAPPA-OPIOID RECEPTOR | SUBSTANCE-P | Receptors, Neurokinin-2 - antagonists & inhibitors | Receptors, Tachykinin - metabolism | Analgesics, Non-Narcotic - pharmacology | Arcuate Nucleus of Hypothalamus - cytology | Male | Peptide Fragments - pharmacology | Substance P - pharmacology | Green Fluorescent Proteins - genetics | Neurokinin B - pharmacology | Quinolines - pharmacology | Kisspeptins - genetics | Piperidines - pharmacology | Neurons - physiology | Receptors, Neurokinin-3 - metabolism | Neurons - metabolism | Receptors, Neurokinin-2 - metabolism | Dynorphins - metabolism | Neurons - drug effects | Substance P - analogs & derivatives | Receptors, Neurokinin-3 - antagonists & inhibitors | Membrane Potentials - drug effects | Green Fluorescent Proteins - metabolism | Arcuate Nucleus of Hypothalamus - metabolism | Receptors, Opioid, kappa - agonists | Receptors, Neurokinin-3 - agonists | Receptors, Opioid, kappa - metabolism | Mice, Transgenic | Kisspeptins - metabolism | 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer - pharmacology | Neurokinin B - metabolism | Patch-Clamp Techniques | Animals | Dynorphins - pharmacology | Kisspeptins - pharmacology | Mice | Oligopeptides - pharmacology
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5. Full Text Role of 5-HT2C receptors in effects of monoamine releasers on intracranial self-stimulation in rats
by Bauer, Clayton T and Banks, Matthew L and Blough, Bruce E and Negus, S Stevens
Psychopharmacology, ISSN 0033-3158, 9/2015, Volume 232, Issue 17, pp. 3249 - 3258
Many monoamine releasers are abused by humans and produce abuse-related facilitation of intracranial self-stimulation (ICSS) in rats. Facilitation of ICSS in... 
Neurosciences | Biomedicine | Dopamine | Amphetamine | Serotonin | Methylenedioxymethamphetamine | Fenfluramine | Intracranial self-stimulation | Pharmacology/Toxicology | Psychiatry | 5-HT 2C receptors | receptors | 5-HT | SQUIRREL-MONKEYS | PSYCHIATRY | DOPAMINERGIC FUNCTION | BEHAVIOR | LOCOMOTOR-ACTIVITY | SEROTONIN RELEASE | NEUROSCIENCES | ABUSE | AMPHETAMINE ANALOGS | PHARMACOLOGY & PHARMACY | METHCATHINONE ANALOGS | 5-HT2C receptors | MODULATION | Receptor, Serotonin, 5-HT2C - drug effects | Receptors, Opioid, kappa - agonists | Rats | Male | Serotonin 5-HT2 Receptor Agonists - pharmacology | Electrodes, Implanted | Serotonin 5-HT2 Receptor Antagonists - pharmacology | Fenfluramine - pharmacology | Rats, Sprague-Dawley | Pyrrolidines - pharmacology | Self Stimulation - drug effects | Animals | Conditioning, Operant - drug effects | N-Methyl-3,4-methylenedioxyamphetamine - pharmacology | Aminopyridines - pharmacology | Adrenergic Uptake Inhibitors - pharmacology | Indoles - pharmacology | Biogenic Monoamines - metabolism | Serotonin Uptake Inhibitors - pharmacology | Benzeneacetamides - pharmacology | Index Medicus | serotonin | amphetamine | methylenedioxymethamphetamine | dopamine | fenfluramine | intracranial self-stimulation
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6. Full Text Locus coeruleus kappa-opioid receptors modulate reinstatement of cocaine place preference through a noradrenergic mechanism
by Al-Hasani, Ream and McCall, Jordan G and Foshage, Audra M and Bruchas, Michael R
Neuropsychopharmacology, ISSN 0893-133X, 11/2013, Volume 38, Issue 12, pp. 2484 - 2497
Activation of kappa-opioid receptors (KORs) in monoamine circuits results in dysphoria-like behaviors and stress-induced reinstatement of drug seeking in both... 
norepinephrine | kappa-opioid receptor | cocaine | reinstatement | locus coeruleus | b-adrenergic receptors | AGONIST SALVINORIN | PRESYNAPTIC INHIBITION | PSYCHIATRY | P38 MAPK | NEUROSCIENCES | BED NUCLEUS | PREFRONTAL CORTEX | CORTICOTROPIN-RELEASING-FACTOR | STRIA TERMINALIS | STRESS-INDUCED REINSTATEMENT | AXON TERMINALS | beta-adrenergic receptors | PHARMACOLOGY & PHARMACY | SALVINORIN-A | Naltrexone - analogs & derivatives | Adrenergic beta-1 Receptor Antagonists - pharmacology | Locus Coeruleus - drug effects | Male | Adrenergic alpha-2 Receptor Agonists - pharmacology | Adrenergic beta-Antagonists - pharmacology | Drug-Seeking Behavior | Naltrexone - pharmacology | Propranolol - pharmacology | Clonidine - pharmacology | Receptors, Adrenergic, beta - metabolism | Receptors, Adrenergic, alpha - metabolism | Receptors, Opioid, kappa - antagonists & inhibitors | Conditioning (Psychology) - drug effects | Mice, Inbred C57BL | Receptors, Opioid, kappa - agonists | Receptors, Opioid, kappa - metabolism | 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer - pharmacology | Cocaine - administration & dosage | Cocaine - pharmacology | Animals | Mice | Betaxolol - pharmacology | Propanolamines - pharmacology | Locus Coeruleus - metabolism | Adrenergic receptors | beta adrenergic receptors | kappa opioid receptor | Catecholamines | Neuropharmacology | behavioral Science | Original | β-adrenergic receptors | opioids
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7. Full Text Differential expression and sensitivity of presynaptic and postsynaptic opioid receptors regulating hypothalamic proopiomelanocortin neurons
by Pennock, Reagan L and Hentges, Shane T
Journal of Neuroscience, ISSN 0270-6474, 01/2011, Volume 31, Issue 1, pp. 281 - 288
Hypothalamic proopiomelanocortin (POMC) neurons release the endogenous opioid beta-endorphin and POMC neuron activity is inhibited by opioids, leading to the... 
LEPTIN | IN-SITU HYBRIDIZATION | GABA | KNOCKOUT | MICE | ARCUATE NUCLEUS | NEUROSCIENCES | Naltrexone - analogs & derivatives | Analgesics - pharmacology | Receptors, Opioid - agonists | Analgesics, Opioid - pharmacology | Neurons - cytology | Peptide Fragments - pharmacology | Patch-Clamp Techniques - methods | Somatostatin - pharmacology | Pyrrolidines - pharmacology | Dose-Response Relationship, Drug | Quinoxalines - pharmacology | Naltrexone - pharmacology | Synapses - metabolism | Gene Expression - physiology | Neurons - physiology | Neurons - drug effects | Benzeneacetamides - pharmacology | Receptors, Opioid - metabolism | Membrane Potentials - drug effects | Synapses - drug effects | Enkephalin, Ala-MePhe-Gly- - pharmacology | Mice, Inbred C57BL | Mice, Transgenic | Pro-Opiomelanocortin - metabolism | Animals | Analysis of Variance | Hypothalamus - cytology | Narcotic Antagonists - pharmacology | Luminescent Proteins - genetics | Mice | Dizocilpine Maleate - pharmacology | In Vitro Techniques | Neural Inhibition - drug effects | Inhibitory Postsynaptic Potentials - drug effects
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8. Full Text Pain-related depression of the mesolimbic dopamine system in rats: Expression, blockade by analgesics, and role of endogenous κ-opioids
by Leitl, Michael D and Onvani, Sara and Bowers, M Scott and Cheng, Kejun and Rice, Kenner C and Carlezon, William A and Banks, Matthew L and Negus, S Stevens
Neuropsychopharmacology, ISSN 0893-133X, 02/2014, Volume 39, Issue 3, pp. 614 - 624
Pain is often associated with depression of behavior and mood, and relief of pain-related depression is a common goal of treatment. This study tested the... 
dynorphin | depression | nucleus accumbens | pain/analgesics | dopamine | intracranial self-stimulation | PRECLINICAL ASSAYS | ACTIVATION | SHELL | PSYCHIATRY | RECEPTOR AGONISTS | BEHAVIOR | NEUROSCIENCES | NUCLEUS-ACCUMBENS | PHARMACOLOGY & PHARMACY | SALVINORIN-A | STRESS | Naltrexone - analogs & derivatives | Self Stimulation | Depression - pathology | Ketoprofen - pharmacology | Nucleus Accumbens - metabolism | Analgesics, Opioid - pharmacology | Male | Medial Forebrain Bundle - drug effects | Pyrrolidines - pharmacology | Depression - etiology | Depression - metabolism | Naltrexone - pharmacology | Pain - complications | Time Factors | Pain - drug therapy | Lactic Acid - pharmacology | Benzeneacetamides - pharmacology | Dopamine - metabolism | Receptors, Opioid, kappa - genetics | Disease Models, Animal | Morphine - pharmacology | Receptors, Opioid, kappa - metabolism | Rats | Rats, Sprague-Dawley | Gene Expression Regulation - drug effects | Medial Forebrain Bundle - physiology | Animals | Narcotic Antagonists - pharmacology | Nucleus Accumbens - drug effects | Index Medicus | Analgesics | pain | analgesics | Original
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9. Full Text Prefrontal cortical kappa-opioid receptor modulation of local neurotransmission and conditioned place aversion
by Tejeda, Hugo A and Counotte, Danielle S and Oh, Eric and Ramamoorthy, Sammanda and Schultz-Kuszak, Kristin N and Bäckman, Cristina M and Chefer, Vladmir and O'Donnell, Patricio and Shippenberg, Toni S
Neuropsychopharmacology, ISSN 0893-133X, 08/2013, Volume 38, Issue 9, pp. 1770 - 1779
Kappa-opioid receptors (KORs) are important for motivation and other medial prefrontal cortex (mPFC)-dependent behaviors. Although KORs are present in the... 
aversion | GABA | kappa-opioid receptors | dopamine | prefrontal cortex | glutamate | IN-VIVO MICRODIALYSIS | RAT | PSYCHIATRY | COCAINE | DYNORPHIN | DOPAMINERGIC-NEURONS | NEUROSCIENCES | EXTRACELLULAR GLUTAMATE | NUCLEUS-ACCUMBENS | CORTEX | PHARMACOLOGY & PHARMACY | GLUTAMATE LEVELS | Naltrexone - analogs & derivatives | Analgesics - pharmacology | Narcotic Antagonists - administration & dosage | Synaptic Transmission - physiology | Neurotransmitter Uptake Inhibitors - antagonists & inhibitors | gamma-Aminobutyric Acid - metabolism | Pyrrolidines - antagonists & inhibitors | Neurotransmitter Uptake Inhibitors - pharmacology | Pyrrolidines - administration & dosage | Male | Dicarboxylic Acids - pharmacology | Miniature Postsynaptic Potentials - drug effects | Excitatory Postsynaptic Potentials - drug effects | Pyrrolidines - pharmacology | Excitatory Postsynaptic Potentials - physiology | Naltrexone - pharmacology | Drug Interactions | Prefrontal Cortex - drug effects | Pyramidal Cells - physiology | Synaptic Transmission - drug effects | Dicarboxylic Acids - antagonists & inhibitors | Pyramidal Cells - drug effects | Benzeneacetamides - pharmacology | Naltrexone - administration & dosage | Dopamine - metabolism | Receptors, Opioid, kappa - genetics | Receptors, Opioid, kappa - antagonists & inhibitors | Glutamic Acid - pharmacology | Microinjections | Receptors, Opioid, kappa - agonists | Analgesics - administration & dosage | Rats | Avoidance Learning - physiology | Benzeneacetamides - administration & dosage | Mice, Knockout | Receptors, Opioid, kappa - physiology | Animals | Narcotic Antagonists - pharmacology | Prefrontal Cortex - metabolism | Avoidance Learning - drug effects | Glutamic Acid - metabolism | Mice | Prefrontal Cortex - physiology | Original | opioids
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10. Full Text Targeting glutaminolysis has antileukemic activity in acute myeloid leukemia and synergizes with BCL-2 inhibition
by Jacque, Nathalie and Ronchetti, Anne Marie and Larrue, Clément and Meunier, Godelieve and Birsen, Rudy and Willems, Lise and Saland, Estelle and Decroocq, Justine and Maciel, Thiago Trovati and Lambert, Mireille and Poulain, Laury and Hospital, Marie Anne and Sujobert, Pierre and Joseph, Laure and Chapuis, Nicolas and Lacombe, Catherine and Moura, Ivan Cruz and Demo, Susan and Sarry, Jean Emmanuel and Recher, Christian and Mayeux, Patrick and Tamburini, Jérôme and Bouscary, Didier and Marie Anne Hosp
Blood, ISSN 0006-4971, 09/2015, Volume 126, Issue 11, pp. 1346 - 1356
Cancer cells require glutamine to adapt to increased biosynthetic activity. The limiting step in intracellular glutamine catabolism involves its conversion to... 
GLYCOLYSIS | STEM-CELLS | DEPENDENCY | MECHANISM | PHOSPHATE-ACTIVATED GLUTAMINASE | AMINO-ACIDS | GROWTH | ENERGY-METABOLISM | HEMATOLOGY | CANCER | EXPRESSION | Apoptosis - drug effects | Humans | Leukemia, Myeloid, Acute - metabolism | Glutamine - metabolism | Gene Knockdown Techniques | Oxidative Phosphorylation - drug effects | Leukemia, Myeloid, Acute - drug therapy | Antineoplastic Agents - pharmacology | Benzeneacetamides - pharmacology | Thiadiazoles - pharmacology | Citric Acid Cycle - drug effects | Enzyme Inhibitors - pharmacology | Glutaminase - metabolism | Mitochondria - metabolism | Sulfonamides - pharmacology | Glutaminase - antagonists & inhibitors | Xenograft Model Antitumor Assays | Bridged Bicyclo Compounds, Heterocyclic - pharmacology | Animals | Oxygen Consumption - drug effects | Cell Line, Tumor | Proto-Oncogene Proteins c-bcl-2 - antagonists & inhibitors | Cell Proliferation - drug effects | Mice | Glutaminase - genetics | Leukemia, Myeloid, Acute - genetics | Myeloid Neoplasia
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11. Full Text Phosphorylation- and stimulus-dependent inhibition of cellular 5-lipoxygenase activity by nonredox-type inhibitors
by Fischer, Lutz and Szellas, Dagmar and RÃ¥dmark, Olof and Steinhilber, Dieter and Werz, Oliver
The FASEB journal : official publication of the Federation of American Societies for Experimental Biology, ISSN 0892-6638, 2003, Volume 17, Issue 8, pp. 949 - 951
Nonredox-type 5-lipoxygenase (5-LO) inhibitors such as ZM230487 or L-739.010 potently suppress leukotriene biosynthesis at low cellular peroxide tone. Here, we... 
polymorphonuclear leukocytes | calcium | MONO-MAC-6 CELLS | CANCER CELLS | leukotriene | BIOCHEMISTRY & MOLECULAR BIOLOGY | MAPK | HUMAN POLYMORPHONUCLEAR LEUKOCYTES | MONOSODIUM URATE | CELL BIOLOGY | IN-VITRO | HUMAN-NEUTROPHILS | LEUKOTRIENE SYNTHESIS | GENE | inflammation | BIOLOGY | GROWTH-FACTOR | Arsenites - pharmacology | Neutrophils - cytology | Phosphorylation | Arachidonate 5-Lipoxygenase - genetics | Calcium - metabolism | Sodium Chloride - pharmacology | Humans | Quinolones - pharmacology | Mutation, Missense | Quinolines - pharmacology | Dose-Response Relationship, Drug | Terpenes - pharmacology | Peroxides - metabolism | Hydroxamic Acids - pharmacology | Neutrophils - metabolism | Pyrans - pharmacology | Arachidonate 5-Lipoxygenase - metabolism | Bridged Bicyclo Compounds - pharmacology | Neutrophils - drug effects | Enzyme Inhibitors - pharmacology | Enzyme Activation - drug effects | Sodium Compounds - pharmacology | Benzeneacetamides | Calcimycin - pharmacology | HeLa Cells | Lipoxygenase Inhibitors - pharmacology | Phloroglucinol - analogs & derivatives | Mitogen-Activated Protein Kinases - metabolism
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12. Full Text Hits of a high-throughput screen identify the hydrophobic pocket of autotaxin/lysophospholipase D as an inhibitory surface
by Fells, James I and Lee, Sue Chin and Fujiwara, Yuko and Norman, Derek D and Lim, Keng Gat and Tsukahara, Ryoko and Liu, Jianxiong and Patil, Renukadevi and Miller, Duane D and Kirby, R. Jason and Nelson, Sandra and Seibel, William and Papoian, Ruben and Parrill, Abby L and Baker, Daniel L and Bittman, Robert and Tigyi, Gabor
Molecular Pharmacology, ISSN 0026-895X, 09/2013, Volume 84, Issue 3, pp. 415 - 424
Autotaxin (ATX), a lysophospholipase D, plays an important role in cancer invasion, metastasis, tumor progression, tumorigenesis, neuropathic pain, fibrotic... 
SITE | LYSOPHOSPHATIDIC ACID | INTESTINAL ALKALINE SPHINGOMYELINASE | DRUG DISCOVERY | PHARMACOLOGY & PHARMACY | AUTOTAXIN EXPRESSION | NUCLEOTIDE PHOSPHODIESTERASE | IDENTIFICATION | CANCER | FAMILY | AXIS | Lung Neoplasms - drug therapy | Tetrazoles - pharmacology | Humans | Melanoma, Experimental - drug therapy | Lung Neoplasms - pathology | Structure-Activity Relationship | Hydrazines - chemistry | Lung Neoplasms - secondary | Tetrazoles - chemistry | Melanoma, Experimental - secondary | Indoles - pharmacology | Antineoplastic Agents - pharmacology | Benzamides - pharmacology | Benzeneacetamides - chemistry | Phosphodiesterase Inhibitors - chemistry | Benzeneacetamides - pharmacology | Benzamides - chemistry | Hydrazines - pharmacology | Phosphoric Diester Hydrolases - metabolism | Sulfonamides - chemistry | Neoplasm Invasiveness | Mice, Inbred C57BL | Phosphodiesterase Inhibitors - pharmacology | Phosphoric Diester Hydrolases - genetics | Antineoplastic Agents - chemistry | Sulfonamides - pharmacology | Phosphoric Diester Hydrolases - chemistry | Animals | High-Throughput Screening Assays | Cell Line, Tumor | Hydrophobic and Hydrophilic Interactions | Mice | Molecular Docking Simulation | Mutation | Indoles - chemistry | Drug Screening Assays, Antitumor | Index Medicus
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13. Full Text Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors
by Jia, Yong and Yun, Cai-Hong and Park, Eunyoung and Ercan, Dalia and Manuia, Mari and Juarez, Jose and Xu, Chunxiao and Rhee, Kevin and Chen, Ting and Zhang, Haikuo and Palakurthi, Sangeetha and Jang, Jaebong and Lelais, Gerald and DiDonato, Michael and Bursulaya, Badry and Michellys, Pierre-Yves and Epple, Robert and Marsilje, Thomas H and McNeill, Matthew and Lu, Wenshuo and Harris, Jennifer and Bender, Steven and Wong, Kwok-Kin and Jänne, Pasi A and Eck, Michael J
Nature, ISSN 0028-0836, 05/2016, Volume 534, Issue 7605, pp. 129 - 132
The epidermal growth factor receptor (EGFR)-directed tyrosine kinase inhibitors (TKIs) gefitinib, erlotinib and afatinib are approved treatments for non-small... 
CELL LUNG-CANCER | EGFR KINASE | GROWTH-FACTOR RECEPTOR | TARGETED THERAPIES | GEFITINIB | ACTIVATION | MECHANISM | MULTIDISCIPLINARY SCIENCES | MUTATIONS | AZD9291 | Lung Neoplasms - drug therapy | Drug Resistance, Multiple - drug effects | Protein Conformation - drug effects | ErbB Receptors - genetics | Lung Neoplasms - pathology | Antineoplastic Agents - pharmacology | Benzeneacetamides - pharmacology | Mutant Proteins - antagonists & inhibitors | Disease Models, Animal | Allosteric Regulation - drug effects | Carcinoma, Non-Small-Cell Lung - pathology | Drug Resistance, Multiple - genetics | ErbB Receptors - antagonists & inhibitors | ErbB Receptors - metabolism | Lung Neoplasms - enzymology | Allosteric Site - drug effects | Mutant Proteins - genetics | Cetuximab - pharmacology | Mutant Proteins - metabolism | Drug Synergism | Drug Resistance, Neoplasm - genetics | Animals | ErbB Receptors - chemistry | Mutant Proteins - chemistry | Cell Line, Tumor | Cell Proliferation - drug effects | Mice | Protein Kinase Inhibitors - pharmacology | Thiazoles - pharmacology | Carcinoma, Non-Small-Cell Lung - drug therapy | Carcinoma, Non-Small-Cell Lung - enzymology | Protein Multimerization - drug effects | Drug Resistance, Neoplasm - drug effects | Studies | Phosphorylation | Nuclear magnetic resonance--NMR | Epidermal growth factor | Mutation | Kinases | Enzyme kinetics | Tumors
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14. Full Text Exploratory effects of a strong CYP3A inhibitor (ketoconazole), a strong CYP3A inducer (rifampicin), and concomitant ethanol on piragliatin pharmacokinetics and pharmacodynamics in type 2 diabetic patients
by Zhi, Jianguo and Zhai, Suoping and Georgy, Angela and Liang, Zhenming and Boldrin, Mark
The Journal of Clinical Pharmacology, ISSN 0091-2700, 05/2016, Volume 56, Issue 5, pp. 548 - 554
Piragliatin is a CYP3A substrate; its inactive metabolite M4, formed through cytosolic reductase, is reversibly metabolized back to piragliatin through CYP3A.... 
pharmacokinetics | interaction | glucokinase activator | pharmacodynamics | DRUG | PHARMACOLOGY & PHARMACY | MELLITUS | Hypoglycemic Agents - pharmacokinetics | Blood Glucose - analysis | Cytochrome P-450 CYP3A Inhibitors - pharmacology | Double-Blind Method | Benzeneacetamides - pharmacokinetics | Humans | Middle Aged | Benzeneacetamides - urine | Male | Diabetes Mellitus, Type 2 - metabolism | Diabetes Mellitus, Type 2 - urine | Ketoconazole - pharmacology | Benzeneacetamides - blood | Hypoglycemic Agents - pharmacology | Cross-Over Studies | Diabetes Mellitus, Type 2 - blood | Ethanol - pharmacology | Cytochrome P-450 CYP3A Inducers - pharmacology | Adult | Female | Aged | Rifampin - pharmacology | Benzeneacetamides - pharmacology | Type 2 diabetes | Care and treatment | Ketoconazole | Analysis | Dosage and administration | Pharmacokinetics | Rifampin
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