Search results for "Amide"

showing 10 items of 3119 documents

CCDC 1433602: Experimental Crystal Structure Determination

2017

Related Article: H. Purandara, S. Foro, B. Thimme Gowda|2017|Acta Crystallogr.,Sect.E:Cryst.Commun.|73|1683|doi:10.1107/S2056989017014669

4-methyl-N-{2-[2-(4-nitrobenzylidene)hydrazinyl]-2-oxoethyl}benzenesulfonamide NN-dimethylformamide solvateSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 1998476: Experimental Crystal Structure Determination

2021

Related Article: Lars J. Wesenberg, Erika Diehl, Till J. B. Zähringer, Carolin Dörr, Dieter Schollmeyer, Akihiro Shimizu, Jun‐ichi Yoshida, Ute A. Hellmich, Siegfried R. Waldvogel|2020|Chem.-Eur.J.|26|17574|doi:10.1002/chem.202003852

5-bromo-2-methoxy-N-(6-methoxy-22-dimethyl-3-oxo-34-dihydro-2H-14-benzoxazin-7-yl)benzene-1-sulfonamideSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 907245: Experimental Crystal Structure Determination

2014

Related Article: A.Valkonen,M.Chucklieb,K.Rissanen|2013|Cryst.Growth Des.|13|4769|doi:10.1021/cg400924n

5-iodopyrimidine-24(1H3H)-dione formamide solvateSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 1561793: Experimental Crystal Structure Determination

2017

Related Article: Tile Gieshoff, Anton Kehl, Dieter Schollmeyer, Kevin D. Moeller, Siegfried R. Waldvogel|2017|J.Am.Chem.Soc.|139|12317|doi:10.1021/jacs.7b07488

6-chloro-2-(N-(4-chlorophenyl)-11-dimethyl)propanamide-13-benzoxazoleSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 1993374: Experimental Crystal Structure Determination

2020

Related Article: Felix Brosge, Johannes Florian Kochs, Mariela Bregu, Khai-Nghi Truong, Kari Rissanen, Carsten Bolm|2020|Org.Lett.|22|6667|doi:10.1021/acs.orglett.0c02504

6-methyl-N-[methyl(oxo)phenylsulfanylidene]-24-dioxo-34-dihydro-2H-13-oxazine-5-carboxamideSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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CCDC 633848: Experimental Crystal Structure Determination

2007

Related Article: M.Albrecht, Triyanti, S.Schiffers, O.Osetska, G.Raabe, T.Wieland, L.Russo, K.Rissanen|2007|Eur.J.Org.Chem.|2007|2850|doi:10.1002/ejoc.200700130

8-(3-n-Butylureido)-4-isobutoxyquinoline-2-carboxylic acid phenyl amide acetonitrile solvateSpace GroupCrystallographyCrystal SystemCrystal StructureCell ParametersExperimental 3D Coordinates
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A subset of flavaglines inhibits KRAS nanoclustering and activation.

2020

The RAS oncogenes are frequently mutated in human cancers and among the three isoforms (KRAS, HRAS and NRAS), KRAS is the most frequently mutated oncogene. Here, we demonstrate that a subset of flavaglines, a class of natural anti-tumour drugs and chemical ligands of prohibitins, inhibit RAS GTP loading and oncogene activation in cells at nanomolar concentrations. Treatment with rocaglamide, the first discovered flavagline, inhibited the nanoclustering of KRAS, but not HRAS and NRAS, at specific phospholipid-enriched plasma membrane domains. We further demonstrate that plasma membrane-associated prohibitins directly interact with KRAS, phosphatidylserine and phosphatidic acid, and these int…

:Bioengineering [Engineering]Neuroblastoma RAS viral oncogene homologGene isoformLung NeoplasmsGTP'[SDV]Life Sciences [q-bio]AucunBiology: Biochemistry biophysics & molecular biology [F05] [Life sciences]medicine.disease_causeProto-Oncogene Proteins p21(ras)03 medical and health scienceschemistry.chemical_compound0302 clinical medicineRocaglamideCarcinoma Non-Small-Cell LungmedicineKRASHumansdrug therapy;geneticsgeneticsHRASProhibitin: Biochimie biophysique & biologie moléculaire [F05] [Sciences du vivant]neoplasmsComputingMilieux_MISCELLANEOUS030304 developmental biology0303 health sciencesOncogeneLipid nanoclusterOncogenesCell Biologydigestive system diseases3. Good healthrespiratory tract diseasesPhospholipidchemistry030220 oncology & carcinogenesisMutationCancer researchKRASFlavaglineRocaglamideProhibitinSignal Transduction
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Antidepressive-like Behavior-Related Metabolomic Signatures of Sigma-1 Receptor Knockout Mice

2022

Sigma-1 receptor (Sig1R) has been proposed as a therapeutic target for neurological, neu-rodegenerative, and psychiatric disorders, including depression and anxiety. Identifying metabolites that are affected by Sig1R absence and cross-referencing them with specific mood-related behaviors would be helpful for the development of new therapies for Sig1R-associated disorders. Here, we examined metabolic profiles in the blood and brains of male CD-1 background Sig1R knockout (KO) mice in adulthood and old age and correlated them with the assessment of depression-and anxiety-related behaviors. The most pronounced changes in the metabolic profile were observed in the plasma of adult Sig1R KO mice.…

:PHARMACY::Biopharmacy [Research Subject Categories]sigma-1 receptorMedicine (miscellaneous)metabolomic signaturesceramidedespair behaviorGeneral Biochemistry Genetics and Molecular Biologyserotonin
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Pharmacological activation of CB2 receptors counteracts the deleterious effect of ethanol on cell proliferation in the main neurogenic zones of the a…

2015

Chronic alcohol exposure reduces endocannabinoid activity and disrupts adult neurogenesis in rodents, which results in structural and functional alterations. Cannabinoid receptor agonists promote adult neural progenitor cell (NPC) proliferation. We evaluated the protective effects of the selective CB1 receptor agonist ACEA, the selective CB2 receptor agonist JWH133 and the fatty-acid amide-hydrolase (FAAH) inhibitor URB597, which enhances endocannabinoid receptor activity, on NPC proliferation in rats with forced consumption of ethanol (10%) or sucrose liquid diets for 2 weeks. We performed immunohistochemical and stereological analyses of cells expressing the mitotic phosphorylation of his…

:Phenomena and Processes::Physiological Phenomena::Physiological Processes::Growth and Development::Morphogenesis::Embryonic and Fetal Development::Organogenesis::Neurogenesis [Medical Subject Headings]CB1 receptorTubulina (proteína)Cannabinoid receptorCarbamatosEtanol:Chemicals and Drugs::Amino Acids Peptides and Proteins::Proteins::Nuclear Proteins::Histones [Medical Subject Headings]Ventrículos lateralesSacarosaNeuronasSubgranular zone0302 clinical medicine:Chemicals and Drugs::Amino Acids Peptides and Proteins::Proteins::Membrane Proteins::Receptors Cell Surface::Receptors G-Protein-Coupled::Receptors Cannabinoid::Receptor Cannabinoid CB1 [Medical Subject Headings]Histonas:Chemicals and Drugs::Organic Chemicals::Carboxylic Acids::Acids Acyclic::Carbamates [Medical Subject Headings]Receptor cannabinoide CB1Cannabinoid receptor type 2:Organisms::Eukaryota::Animals [Medical Subject Headings]:Phenomena and Processes::Metabolic Phenomena::Metabolism::Phosphorylation [Medical Subject Headings]:Anatomy::Cells::Stem Cells::Neural Stem Cells [Medical Subject Headings]:Anatomy::Nervous System::Neurons [Medical Subject Headings]health care economics and organizations:Anatomy::Nervous System::Central Nervous System::Brain::Cerebral Ventricles::Lateral Ventricles [Medical Subject Headings]Original Research:Chemicals and Drugs::Nucleic Acids Nucleotides and Nucleosides::Nucleosides::Deoxyribonucleosides::Deoxyuridine::Bromodeoxyuridine [Medical Subject Headings]0303 health sciencesAlcoholismoalcoholConsumo de alcoholNeurogenesis:Phenomena and Processes::Genetic Phenomena::Phenotype::Genetic Markers [Medical Subject Headings]:Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Molecular Mechanisms of Pharmacological Action::Neurotransmitter Agents::Cannabinoid Receptor Modulators::Cannabinoid Receptor Agonists [Medical Subject Headings]Benzamidas:Chemicals and Drugs::Amino Acids Peptides and Proteins::Proteins::Membrane Proteins::Receptors Cell Surface::Receptors G-Protein-Coupled::Receptors Cannabinoid::Receptor Cannabinoid CB2 [Medical Subject Headings]Endocannabinoid system3. Good healthbromodesoxiuridinaneurogenesisEndocannabinoidesmedicine.anatomical_structure:Chemicals and Drugs::Enzymes and Coenzymes::Enzymes::Hydrolases [Medical Subject Headings]ACEADietaAlcoholFosforilaciónAgonistmedicine.medical_specialtyHidrolasasmedicine.drug_classNeurogenesiseducation:Psychiatry and Psychology::Mental Disorders::Substance-Related Disorders::Alcohol-Related Disorders::Alcoholism [Medical Subject Headings]Subventricular zoneBiology:Phenomena and Processes::Physiological Phenomena::Nutritional Physiological Phenomena::Diet [Medical Subject Headings]:Anatomy::Nervous System::Central Nervous System::Brain::Prosencephalon::Telencephalon::Cerebrum::Cerebral Cortex::Hippocampus::Dentate Gyrus [Medical Subject Headings]lcsh:RC321-57103 medical and health sciencesCellular and Molecular NeuroscienceRatasInternal medicine:Chemicals and Drugs::Amino Acids Peptides and Proteins::Proteins::Nerve Tissue Proteins::Tubulin [Medical Subject Headings]JWH133medicineGiro dentadolcsh:Neurosciences. Biological psychiatry. Neuropsychiatry030304 developmental biologyCélulas madre nerviosas:Chemicals and Drugs::Chemical Actions and Uses::Pharmacologic Actions::Molecular Mechanisms of Pharmacological Action::Neurotransmitter Agents::Endocannabinoids [Medical Subject Headings]Dentate gyrusmarcadores genéticosCB2 receptor:Chemicals and Drugs::Carbohydrates::Polysaccharides::Oligosaccharides::Disaccharides::Sucrose [Medical Subject Headings]:Anatomy::Nervous System::Central Nervous System::Brain::Prosencephalon::Diencephalon::Hypothalamus [Medical Subject Headings]:Chemicals and Drugs::Organic Chemicals::Alcohols::Ethanol [Medical Subject Headings]Endocrinology:Organisms::Eukaryota::Animals::Chordata::Vertebrates::Mammals::Rodentia::Muridae::Murinae::Rats [Medical Subject Headings]nervous system:Psychiatry and Psychology::Behavior and Behavior Mechanisms::Behavior::Drinking Behavior::Alcohol Drinking [Medical Subject Headings]:Chemicals and Drugs::Organic Chemicals::Amides::Benzamides [Medical Subject Headings]030217 neurology & neurosurgeryHipotálamoNeuroscience
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Polyoxypregnanes as safe, potent, and specific ABCB1-inhibitory pro-drugs to overcome multidrug resistance in cancer chemotherapy in vitro and in vivo

2021

Multidrug resistance (MDR) mediated by ATP binding cassette subfamily B member 1 (ABCB1) is significantly hindering effective cancer chemotherapy. However, currently, no ABCB1-inhibitory drugs have been approved to treat MDR cancer clinically, mainly due to the inhibitor specificity, toxicity, and drug interactions. Here, we reported that three polyoxypregnanes (POPs) as the most abundant constituents of Marsdenia tenacissima (M. tenacissima) were novel ABCB1-modulatory pro-drugs, which underwent intestinal microbiota-mediated biotransformation in vivo to generate active metabolites. The metabolites at non-toxic concentrations restored chemosensitivity in ABCB1-overexpressing cancer cells v…

ABCC1 ATP binding cassette subfamily C member 1IC50 half maximal inhibitory concentrationMultidrug resistancePharmacologyNADPH reduced nicotinamide adenine dinucleotide phosphateF bioavailabilitychemistry.chemical_compoundPCR polymerase chain reaction0302 clinical medicineMDR multidrug resistanceECL electrochemiluminescencet1/2 elimination half-lifeLC–MS liquid chromatography coupled with mass spectrometryN.D. not detectedGeneral Pharmacology Toxicology and PharmaceuticsBBB blood–brain barriermedia_commonATF3 activating transcription factor 30303 health sciencesChemistryABC ATP-binding cassetteNMPA National Medical Products AdministrationPXR pregnane X receptorSDS-PAGE sodium dodecyl sulfate-polyacrylamide gel electrophoresisHBSS Hankʹs balanced salt solutionABCB1Combination chemotherapyProdrugMarsdenia tenacissimaCmax peak concentrationPaclitaxelGAPDH glyceraldehyde-3-phosphate dehydrogenase030220 oncology & carcinogenesisBHI brain heart infusionOriginal ArticleAUC0–∞ area under plasma concentration vs. time curveMRT mean residence timeDrugmedia_common.quotation_subjectRM1-950Vd volume of distributionABCB1 ATP binding cassette subfamily B member 1UIC-2 mouse monoclonal ABCB1 antibodyABCG2 ATP binding cassette subfamily G member 2Combination chemotherapyCYP cytochrome P450 isozymePI propidium iodideTEER transepithelial electrical resistance03 medical and health sciencesPBS phosphate buffer salineFBS fetal bovine serumDox doxorubicinIn vivoPOP polyoxypregnanemedicine030304 developmental biologyEVOM epithelial tissue voltohmmeterTmax time for peak concentrationCancerLBE lowest binding energyPE phycoerythrinmedicine.diseaseMultiple drug resistancePolyoxypregnanePapp apparent permeabilityN.A. not applicableCancer cellH&E hematoxylin and eosinMDR1a multidrug resistance protein 1aTherapeutics. PharmacologyqPCR quantitative PCRM. tenacissima Marsdenia tenacissimaCL clearanceSD standard derivationActa Pharmaceutica Sinica B
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