听力与言语-语言病理学

行为科学

医学伦理学

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  • Predicting Drug Interactions with Human Equilibrative Nucleoside Transporters 1 and 2 Using Functional Knockout Cell Lines and Bayesian Modeling.

    abstract::Equilibrative nucleoside transporters (ENTs) 1 and 2 facilitate nucleoside transport across the blood-testis barrier (BTB). Improving drug entry into the testes with drugs that use endogenous transport pathways may lead to more effective treatments for diseases within the reproductive tract. In this study, CRISPR/CRIS...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/molpharm.120.000169

    authors: Miller SR,Zhang X,Hau RK,Jilek JL,Jennings EQ,Galligan JJ,Foil DH,Zorn KM,Ekins S,Wright SH,Cherrington NJ

    更新日期:2021-02-01 00:00:00

  • Mechanism-based Inactivation of Cytochrome P450 3A4 by Benzbromarone.

    abstract::Benzbromarone (BBR), a potent uricosuric agent for the management of gout, is known to cause fatal fulminant hepatitis. While the mechanism of BBR-induced idiosyncratic hepatotoxicity remains unelucidated, cytochrome P450 enzyme (CYP450)-mediated bioactivation of BBR to electrophilic reactive metabolites is commonly r...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/molpharm.120.000086

    authors: Tang LWT,Verma RK,Fan H,Chan ECY

    更新日期:2021-01-12 00:00:00

  • Characterization of Vixotrigine, a Broad-Spectrum Voltage-Gated Sodium Channel Blocker.

    abstract::Voltage-gated sodium channels (Navs) are promising targets for analgesic and antiepileptic therapies. Although specificity between Nav subtypes may be desirable to target specific neural types, such as nociceptors in pain, many broadly acting Nav inhibitors are clinically beneficial in neuropathic pain and epilepsy. H...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/molpharm.120.000079

    authors: Hinckley CA,Kuryshev Y,Sers A,Barre A,Buisson B,Naik H,Hajos M

    更新日期:2021-01-01 00:00:00

  • Proteomic approaches to investigate regulated trafficking and signaling of GPCRs.

    abstract::Advances in proteomic methodologies based on quantitative mass spectrometry are now transforming pharmacology and experimental biology more broadly. The present review will discuss several examples, based on work in the author's laboratory that focuses on delineating relationships between GPCR signaling and traffickin...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/molpharm.120.000178

    authors: von Zastrow M

    更新日期:2020-12-22 00:00:00

  • N-Terminal Targeting of Regulator of G Protein Signaling Protein 2 for F-Box Only Protein 44-Mediated Proteasomal Degradation.

    abstract::Regulator of G protein signaling (RGS) proteins are negative modulators of G protein signaling that have emerged as promising drug targets to improve specificity and reduce side effects of G protein-coupled receptor-related therapies. Several small molecule RGS protein inhibitors have been identified; however, enhanci...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/molpharm.120.000061

    authors: McNabb HJ,Gonzalez S,Muli CS,Sjögren B

    更新日期:2020-12-01 00:00:00

  • Notch1 in Cancer Therapy: Possible Clinical Implications and Challenges.

    abstract::The Notch family consists of four highly conserved transmembrane receptors. The release of the active intracellular domain requires the enzymatic activity of γ-secretase. Notch is involved in embryonic development and in many physiologic processes of normal cells, in which it regulates growth, apoptosis, and different...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1124/molpharm.120.000006

    authors: Gharaibeh L,Elmadany N,Alwosaibai K,Alshaer W

    更新日期:2020-11-01 00:00:00

  • Structure of Cytochrome P450 2C9*2 in Complex with Losartan: Insights into the Effect of Genetic Polymorphism.

    abstract::The human CYP2C9 plays a crucial role in the metabolic clearance of a wide range of clinical therapeutics. The *2 allele is a prevalent genetic variation in CYP2C9 that is found in various populations. A marked reduction of catalytic activity toward many important drug substrates has been demonstrated by CYP2C9*2, whi...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/molpharm.120.000042

    authors: Parikh SJ,Evans CM,Obi JO,Zhang Q,Maekawa K,Glass KC,Shah MB

    更新日期:2020-11-01 00:00:00

  • A Truncated Six Transmembrane Splice Variant MOR-1G Enhances Expression of the Full-Length Seven Transmembrane μ-Opioid Receptor through Heterodimerization.

    abstract::The μ-opioid receptor gene undergoes extensive alternative splicing to generate an array of splice variants. One group of splice variants excludes the first transmembrane (TM) domain and contains six TM domains. These 6TM variants are essential for the action of a novel class of analgesic drugs, including 3-iodobenzoy...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.120.119453

    authors: Zhang T,Xu J,Pan YX

    更新日期:2020-10-01 00:00:00

  • Opioid Pharmacology under the Microscope.

    abstract::The powerful analgesic effects of opioid drugs have captivated the interest of physicians and scientists for millennia, and the ability of opioid drugs to produce serious undesired effects has been recognized for a similar period of time (Kieffer and Evans, 2009). Many of these develop progressively with prolonged or ...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1124/mol.119.119321

    authors: Jullié D,Gondin AB,von Zastrow M,Canals M

    更新日期:2020-10-01 00:00:00

  • Inhibition of Brain Epidermal Growth Factor Receptor Activation: A Novel Target in Neurodegenerative Diseases and Brain Injuries.

    abstract::Several reports have been published recently demonstrating a beneficial effect of epidermal growth factor receptor (EGFR) inhibitors in improving pathologic and behavioral conditions in neurodegenerative diseases (NDDs) such as Alzheimer's disease and Amyotrophic Lateral Sclerosis (ALS) as well as the brain and spinal...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1124/mol.120.119909

    authors: Tavassoly O,Sato T,Tavassoly I

    更新日期:2020-07-01 00:00:00

  • Tubulin-Binding 3,5-Bis(styryl)pyrazoles as Lead Compounds for the Treatment of Castration-Resistant Prostate Cancer.

    abstract::The microtubule-binding taxanes, docetaxel and cabazitaxel, are administered intravenously for the treatment of castration-resistant prostate cancer (CRPC) as the oral administration of these drugs is largely hampered by their low and highly variable bioavailabilities. Using a simple, rapid, and environmentally friend...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.119.118539

    authors: Liao VWY,Kumari A,Narlawar R,Vignarajan S,Hibbs DE,Panda D,Groundwater PW

    更新日期:2020-06-01 00:00:00

  • A New Paroxetine-Based GRK2 Inhibitor Reduces Internalization of the μ-Opioid Receptor.

    abstract::G protein-coupled receptor (GPCR) kinases (GRKs) play a key role in terminating signals initiated by agonist-bound GPCRs. However, chronic stimulation of GPCRs, such as that which occurs during heart failure, leads to the overexpression of GRKs and maladaptive downregulation of GPCRs on the cell surface. We previously...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.119.118661

    authors: Bouley RA,Weinberg ZY,Waldschmidt HV,Yen YC,Larsen SD,Puthenveedu MA,Tesmer JJG

    更新日期:2020-06-01 00:00:00

  • Cisplatin in Combination with MDM2 Inhibition Downregulates Rad51 Recombinase in a Bimodal Manner to Inhibit Homologous Recombination and Augment Tumor Cell Kill.

    abstract::Dysfunction of p53 and resistance to cancer drugs can arise through mutually exclusive overexpression of MDM2 or MDM4. Cisplatin-resistant cells, however, can demonstrate increased binding of both MDM2 and MDM4 to p53 but in absence of cellular overexpression. Whether MDM2 inhibitors alone can activate p53 in these re...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.119.117564

    authors: Xie X,He G,Siddik ZH

    更新日期:2020-04-01 00:00:00

  • Defining a cellular map of cAMP nanodomains.

    abstract::By limiting unrestricted activation of intracellular effectors, compartmentalised signalling of cyclic nucleotides confers specificity to extracellular stimuli and is critical for the development and health of cells and organisms. Dissecting the molecular mechanisms that allow local control of cyclic nucleotide signal...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.119.118869

    authors: Schleicher K,Zaccolo M

    更新日期:2020-02-28 00:00:00

  • Molecular Pharmacology of Class F Receptor Activation.

    abstract::The class Frizzled (FZD) or class F of G protein-coupled receptors consists of 10 FZD paralogues and Smoothened (SMO). FZDs coordinate wingless/Int-1 signaling and SMO mediates Hedgehog signaling. Class F receptor signaling is intrinsically important for embryonic development and its dysregulation leads to diseases, i...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1124/mol.119.117986

    authors: Kozielewicz P,Turku A,Schulte G

    更新日期:2020-02-01 00:00:00

  • The Role of ACKR3 in Breast, Lung, and Brain Cancer.

    abstract::Recent reports regarding the significance of chemokine receptors in disease have put a spotlight on atypical chemokine receptor 3 (ACKR3). This atypical chemokine receptor is overexpressed in numerous cancer types and has been involved in the modulation of tumor cell proliferation and migration, tumor angiogenesis, or...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1124/mol.118.115279

    authors: Neves M,Fumagalli A,van den Bor J,Marin P,Smit MJ,Mayor F

    更新日期:2019-12-01 00:00:00

  • Chemokine Receptor Crystal Structures: What Can Be Learned from Them?

    abstract::Chemokine receptors belong to the class A of G protein-coupled receptors (GPCRs) and are implicated in a wide variety of physiologic functions, mostly related to the homeostasis of the immune system. Chemokine receptors are also involved in multiple pathologic processes, including immune and autoimmune diseases, as we...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1124/mol.119.117168

    authors: Arimont M,Hoffmann C,de Graaf C,Leurs R

    更新日期:2019-12-01 00:00:00

  • Antibodies Targeting Chemokine Receptors CXCR4 and ACKR3.

    abstract::Dysregulation of the chemokine system is implicated in a number of autoimmune and inflammatory diseases, as well as cancer. Modulation of chemokine receptor function is a very promising approach for therapeutic intervention. Despite interest from academic groups and pharmaceutical companies, there are currently few ap...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1124/mol.119.116954

    authors: Bobkov V,Arimont M,Zarca A,De Groof TWM,van der Woning B,de Haard H,Smit MJ

    更新日期:2019-12-01 00:00:00

  • Modulators of CXCR4 and CXCR7/ACKR3 Function.

    abstract::The two G protein-coupled receptors (GPCRs) C-X-C chemokine receptor type 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3) are part of the class A chemokine GPCR family and represent important drug targets for human immunodeficiency virus (HIV) infection, cancer, and inflammation diseases. CXCR4 is one of only thre...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1124/mol.119.117663

    authors: Adlere I,Caspar B,Arimont M,Dekkers S,Visser K,Stuijt J,de Graaf C,Stocks M,Kellam B,Briddon S,Wijtmans M,de Esch I,Hill S,Leurs R

    更新日期:2019-12-01 00:00:00

  • N-Terminal Modification of the Tetrapeptide Arg-Leu-Tyr-Glu, a Vascular Endothelial Growth Factor Receptor-2 (VEGFR-2) Antagonist, Improves Antitumor Activity by Increasing its Stability against Serum Peptidases.

    abstract::The tetrapeptide Arg-Leu-Tyr-Glu (RLYE), a vascular endothelial growth factor (VEGF) receptor-2 antagonist, has been used previously either alone or in combination with chemotherapeutic drugs for treating colorectal cancer in a mouse model. We analyzed the half-life of the peptide and found that because of degradation...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.119.117234

    authors: Yun JA,Kim J,Baek YY,Park W,Park M,Kim S,Kim T,Choi S,Jeoung D,Lee H,Won MH,Kim JY,Ha KS,Kwon YG,Kim YM

    更新日期:2019-12-01 00:00:00

  • The Basis for Strain-Dependent Rat Aldehyde Dehydrogenase 1A7 (ALDH1A7) Gene Expression.

    abstract::Aldehyde hydrogenases (ALDHs) belong to a large gene family involved in oxidation of both endogenous and exogenous compounds in mammalian tissues. Among ALDHs, the rat ALDH1A7 gene displays a curious strain dependence in phenobarbital (PB)-induced hepatic expression: the responsive RR ...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.119.117424

    authors: Touloupi K,Küblbeck J,Magklara A,Molnár F,Reinisalo M,Konstandi M,Honkakoski P,Pappas P

    更新日期:2019-11-01 00:00:00

  • Does the Lipid Bilayer Orchestrate Access and Binding of Ligands to Transmembrane Orthosteric/Allosteric Sites of G Protein-Coupled Receptors?

    abstract::The ligand-binding sites of many G protein-coupled receptors (GPCRs) are situated around and deeply embedded within the central pocket formed by their seven transmembrane-spanning α-helical domains. Generally, these binding sites are assumed accessible to endogenous ligands from the aqueous phase. Recent advances in t...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1124/mol.118.115113

    authors: Szlenk CT,Gc JB,Natesan S

    更新日期:2019-11-01 00:00:00

  • ORKAMBI-Mediated Rescue of Mucociliary Clearance in Cystic Fibrosis Primary Respiratory Cultures Is Enhanced by Arginine Uptake, Arginase Inhibition, and Promotion of Nitric Oxide Signaling to the Cystic Fibrosis Transmembrane Conductance Regulator Channe

    abstract::ORKAMBI, a combination of the corrector, lumacaftor, and the potentiator, ivacaftor, partially rescues the defective processing and anion channel activity conferred by the major cystic fibrosis-causing mutation, F508del, in in vitro studies. Clinically, the improvement in lung function after ORKAMBI treatment is modes...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.119.117143

    authors: Wu YS,Jiang J,Ahmadi S,Lew A,Laselva O,Xia S,Bartlett C,Ip W,Wellhauser L,Ouyang H,Gonska T,Moraes TJ,Bear CE

    更新日期:2019-10-01 00:00:00

  • Structural Basis for Diltiazem Block of a Voltage-Gated Ca2+ Channel.

    abstract::Diltiazem is a widely prescribed Ca2+ antagonist drug for cardiac arrhythmia, hypertension, and angina pectoris. Using the ancestral CaV channel construct CaVAb as a molecular model for X-ray crystallographic analysis, we show here that diltiazem targets the central cavity of the voltage-gated Ca2+ channel underneath ...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.119.117531

    authors: Tang L,Gamal El-Din TM,Lenaeus MJ,Zheng N,Catterall WA

    更新日期:2019-10-01 00:00:00

  • Inhibition of Heat Shock Protein 90 suppresses TWIST1 Transcription.

    abstract::Molecular chaperone heat shock protein 90 (HSP90) is involved in oncogenic signaling pathways including epithelial-mesenchymal transition (EMT), a key process in tumor initiation, progression, metastasis, and chemoresistance. The molecular mechanisms underlying the involvement of HSP90 in EMT are still under investiga...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.119.116137

    authors: Chong KY,Kang M,Garofalo F,Ueno D,Liang H,Cady S,Madarikan O,Pitruzzello N,Tsai CH,Hartwich TMP,Shuch BM,Yang-Hartwich Y

    更新日期:2019-08-01 00:00:00

  • Identification of Abundant and Evolutionarily Conserved Opioid Receptor Circular RNAs in the Nervous System Modulated by Morphine.

    abstract::Circular RNAs (circRNAs) are a distinct category of single-stranded, covalently closed RNAs formed by backsplicing. The functions of circRNAs are incompletely known and are under active investigation. Here, we report that in addition to traditional linear mRNAs (linRNA), mouse, rat, and human opioid receptor genes gen...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.118.113977

    authors: Irie T,Shum R,Deni I,Hunkele A,Le Rouzic V,Xu J,Wilson R,Fischer GW,Pasternak GW,Pan YX

    更新日期:2019-08-01 00:00:00

  • Identification of MRP4/ABCC4 as a Target for Reducing the Proliferation of Pancreatic Ductal Adenocarcinoma Cells by Modulating the cAMP Efflux.

    abstract::Pancreatic cancer is one of the most lethal types of tumors with no effective therapy available; is currently the third leading cause of cancer in developed countries; and is predicted to become the second deadliest cancer in the United States by 2030. Due to the marginal benefits of current standard chemotherapy, the...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.118.115444

    authors: Carozzo A,Yaneff A,Gómez N,Di Siervi N,Sahores A,Diez F,Attorresi AI,Rodríguez-González Á,Monczor F,Fernández N,Abba M,Shayo C,Davio C

    更新日期:2019-07-01 00:00:00

  • Hepatic Expression of Niemann-Pick C1-Like 1, a Cholesterol Reabsorber from Bile, Exacerbates Western Diet-Induced Atherosclerosis in LDL Receptor Mutant Mice.

    abstract::Westernization of dietary habits increases lipid intake and is responsible for increased numbers of patients with atherosclerotic diseases. Niemann-Pick C1-Like 1 (NPC1L1)-a cholesterol importer-plays a crucial role in dietary cholesterol absorption in the intestine and is closely associated with several lipid-related...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.119.115840

    authors: Yamamoto H,Yamanashi Y,Takada T,Mu S,Tanaka Y,Komine T,Suzuki H

    更新日期:2019-07-01 00:00:00

  • Monod-Wyman-Changeux Allosteric Shift Analysis in Mutant α1β3γ2L GABAA Receptors Indicates Selectivity and Crosstalk among Intersubunit Transmembrane Anesthetic Sites.

    abstract::Propofol, etomidate, and barbiturate anesthetics are allosteric coagonists at pentameric α1β3γ2 GABAA receptors, modulating channel activation via four biochemically established intersubunit transmembrane pockets. Etomidate selectively occupies the two β+/α- pockets, the barbiturate photolabel R-5-allyl-1-methyl-5-(m-...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.118.115048

    authors: Szabo A,Nourmahnad A,Halpin E,Forman SA

    更新日期:2019-04-01 00:00:00

  • Cannabinoid CB2 Agonist AM1710 Differentially Suppresses Distinct Pathological Pain States and Attenuates Morphine Tolerance and Withdrawal.

    abstract::AM1710 (3-(1,1-dimethyl-heptyl)-1-hydroxy-9-methoxy-benzo(c) chromen-6-one), a cannabilactone cannabinoid receptor 2 (CB2) agonist, suppresses chemotherapy-induced neuropathic pain in rodents without producing tolerance or unwanted side effects associated with CB1 receptors; however, the signaling profile of AM1710 re...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.118.113233

    authors: Li AL,Lin X,Dhopeshwarkar AS,Thomaz AC,Carey LM,Liu Y,Nikas SP,Makriyannis A,Mackie K,Hohmann AG

    更新日期:2019-02-01 00:00:00

  • Identification of Peracetylated Quercetin as a Selective 12-Lipoxygenase Pathway Inhibitor in Human Platelets.

    abstract::The inflammatory response is necessary for the host's defense against pathogens; however, uncontrolled or unregulated production of eicosanoids has been associated with several types of chronic inflammatory diseases. Thus, it is not surprising that enzymes implicated in the production of eicosanoids have been strategi...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.118.113480

    authors: Doucet MS,Jougleux JL,Poirier SJ,Cormier M,Léger JL,Surette ME,Pichaud N,Touaibia M,Boudreau LH

    更新日期:2019-01-01 00:00:00

  • Lysosome Membrane Permeabilization and Disruption of the Molecular Target of Rapamycin (mTOR)-Lysosome Interaction Are Associated with the Inhibition of Lung Cancer Cell Proliferation by a Chloroquinoline Analog.

    abstract::Lysosomes degrade cellular proteins and organelles and regulate cell signaling by providing a surface for the formation of critical protein complexes, notably molecular target of rapamycin (mTOR) complex 1 (mTORC1). Striking differences in the lysosomes of cancer versus normal cells suggest that they could be targets ...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.118.113118

    authors: Sironi J,Aranda E,Nordstrøm LU,Schwartz EL

    更新日期:2019-01-01 00:00:00

  • N-Phthalyl-l-Tryptophan (RG108), like Clozapine (CLO), Induces Chromatin Remodeling in Brains of Prenatally Stressed Mice.

    abstract::Schizophrenia (SZ), schizoaffective (SZA), and bipolar (BP) disorder are neurodevelopmental psychopathological conditions related, in part, to genetic load and, in part, to environmentally induced epigenetic dysregulation of chromatin structure and function in neocortical GABAergic, glutamatergic, and monoaminergic ne...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.118.113415

    authors: Dong E,Locci V,Gatta E,Grayson DR,Guidotti A

    更新日期:2019-01-01 00:00:00

  • Modeling and Mutational Analysis of the Binding Mode for the Multimodal Antidepressant Drug Vortioxetine to the Human 5-HT3A Receptor.

    abstract::5-Hydroxytryptamine3 (5-HT3) receptors are ligand-gated ion channels that mediate neurotransmission by serotonin in the central nervous system. Pharmacological inhibition of 5-HT3 receptor activity has therapeutic potential in several psychiatric diseases, including depression and anxiety. The recently approved multim...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.118.113530

    authors: Ladefoged LK,Munro L,Pedersen AJ,Lummis SCR,Bang-Andersen B,Balle T,Schiøtt B,Kristensen AS

    更新日期:2018-12-01 00:00:00

  • Application of Mixture Design Response Surface Methodology for Combination Chemotherapy in PC-3 Human Prostate Cancer Cells.

    abstract::Combining chemotherapeutics to treat malignant tumors has been shown to be effective in preventing drug resistance, tumor recurrence, and reducing tumor size. We modeled combination drug therapy in PC-3 human prostate cancer cells using mixture design response surface methodology (MDRSM), a statistical technique desig...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.117.111450

    authors: Oblad R,Doughty H,Lawson J,Christensen M,Kenealey J

    更新日期:2018-08-01 00:00:00

  • Cysteine Scanning Mutagenesis of TM4b-4c Loop of Glutamate Transporter EAAT1 Reveals Three Conformationally Sensitive Residues.

    abstract::Glutamatergic synaptic transmitters are cleared from the synaptic cleft through excitatory amino acid transporters (EAATs) that are responsible for recycling glutamate and transporting it into neurons and glial cells. To probe the structural role of the TM4b-4c loop of EAAT1 (Rattus norvegicus), each of the 57 amino a...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.117.111245

    authors: Zhang W,Zhang X,Qu S

    更新日期:2018-07-01 00:00:00

  • A Transcriptional Regulatory Network Containing Nuclear Receptors and Long Noncoding RNAs Controls Basal and Drug-Induced Expression of Cytochrome P450s in HepaRG Cells.

    abstract::Cytochrome P450 (P450) enzymes are responsible for metabolizing drugs. Expression of P450s can directly affect drug metabolism, resulting in various outcomes in therapeutic efficacy and adverse effects. Several nuclear receptors are transcription factors that can regulate expression of P450s at both basal and drug-ind...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.118.112235

    authors: Chen L,Bao Y,Piekos SC,Zhu K,Zhang L,Zhong XB

    更新日期:2018-07-01 00:00:00

  • Retinal-chitosan Conjugates Effectively Deliver Active Chromophores to Retinal Photoreceptor Cells in Blind Mice and Dogs.

    abstract::The retinoid (visual) cycle consists of a series of biochemical reactions needed to regenerate the visual chromophore 11-cis-retinal and sustain vision. Genetic or environmental factors affecting chromophore production can lead to blindness. Using animal models that mimic human retinal diseases, we previously demonstr...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.117.111294

    authors: Gao S,Kahremany S,Zhang J,Jastrzebska B,Querubin J,Petersen-Jones SM,Palczewski K

    更新日期:2018-05-01 00:00:00

  • Hemodynamic Effects of Glutathione-Liganded Binuclear Dinitrosyl Iron Complex: Evidence for Nitroxyl Generation and Modulation by Plasma Albumin.

    abstract::Glutathione-liganded binuclear dinitrosyl iron complex (glut-BDNIC) has been proposed to be a donor of nitric oxide (NO). This study was undertaken to investigate the mechanisms of vasoactivity, systemic hemodynamic effects, and pharmacokinetics of glut-BDNIC. To test the hypothesis that glut-BDNICs vasodilate by rele...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章

    doi:10.1124/mol.117.110957

    authors: Liu T,Zhang M,Terry MH,Schroeder H,Wilson SM,Power GG,Li Q,Tipple TE,Borchardt D,Blood AB

    更新日期:2018-05-01 00:00:00

  • Caveolins as Regulators of Stress Adaptation.

    abstract::Caveolins have been recognized over the past few decades as key regulators of cell physiology. They are ubiquitously expressed and regulate a number of processes that ultimately impact efficiency of cellular processes. Though not critical to life, they are central to stress adaptation in a number of organs. The follow...

    journal_title:Molecular pharmacology

    pub_type: 杂志文章,评审

    doi:10.1124/mol.117.111237

    authors: Schilling JM,Head BP,Patel HH

    更新日期:2018-04-01 00:00:00

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