Control of transmitter release from the motor nerve by presynaptic nicotinic and muscarinic autoreceptors.

abstract：:Hypertension is prevalent and affects approximately 1 in every 4 adults in the Western world. Although many drugs are effective in treating hypertension, an individual's response to treatment is unpredictable. Pharmacogenetics holds the promise of becoming a tool to predict this response but obstacles and shortcomings...

journal_title：Trends in pharmacological sciences

authors： Kurland L,Lind L,Melhus H

更新日期：2005-09-01 00:00:00

abstract：:The GABAA receptor belongs, along with the nicotinic acetylcholine receptor, the glycine receptor and the 5-HT3 receptor, to a family of homologous transmitter-gated ion channels mediating fast synaptic transmission. Many classes of drug interact with the GABAA receptor, which is the major inhibitory ion channel in th...

journal_title：Trends in pharmacological sciences

authors： Sigel E,Buhr A

更新日期：1997-11-01 00:00:00

abstract：:Chronic obstructive pulmonary disease (COPD) is caused mostly by cigarette smoking but its specific molecular mechanisms are obscure. Current theories suggest that the inflammation and oxidative stress induced by smoking lead to proteolytic imbalance and progressive lung structural derangement, with disease susceptibi...

journal_title：Trends in pharmacological sciences

authors： Anderson GP,Bozinovski S

更新日期：2003-02-01 00:00:00

abstract：:Degradation of heme requires its conversion to biliverdin (BV) by heme oxygenase, followed by reduction of BV to the free-radical quencher bilirubin (BR) by biliverdin reductase (BVR). It is now recognized that human BVR (hBVR) is a dual-specificity kinase (Ser/Thr and Tyr) upstream activator of the insulin/insulin gr...

journal_title：Trends in pharmacological sciences

authors： Kapitulnik J,Maines MD

更新日期：2009-03-01 00:00:00

abstract：:The characterization of P2 gamma purinoceptors on vascular endothelial cells has progressed rapidly since their existence was first demonstrated in 1983. They transduce the actions of extracellular ATP and ADP--endothelium-dependent relaxation, prostacyclin synthesis, endothelial cell mitogenesis--which play a vital r...

journal_title：Trends in pharmacological sciences

authors： Boeynaems JM,Pearson JD

更新日期：1990-01-01 00:00:00

abstract：:In drug development, major resources are invested into the development of cellular delivery systems to increase the effectiveness of a large array of potential therapeutics, such as proteins and oligonucleotides. These carriers comprise cell-penetrating peptides (CPPs), cationic lipids and cationic polymers. In recent...

journal_title：Trends in pharmacological sciences

authors： Verdurmen WP,Brock R

更新日期：2011-02-01 00:00:00

abstract：:Clodronate is a first-generation bisphosphonate used worldwide for antiresorptive therapy for osteoporosis. Although clodronate is analgesic in nature, its mechanism and efficacy were unknown for some time. Recently, clodronate was identified as a selective and potent inhibitor for vesicular nucleotide transporter (VN...

journal_title：Trends in pharmacological sciences

authors： Moriyama Y,Nomura M

更新日期：2018-01-01 00:00:00

abstract：:Over the past few decades, mortality resulting from cardiovascular disease (CVD) steadily decreased in western countries; however, in recent years, the decline has become offset by the increase in obesity. Obesity is strongly associated with the metabolic syndrome and its atherogenic dyslipidemia resulting from insuli...

journal_title：Trends in pharmacological sciences

authors： Soyal SM,Nofziger C,Dossena S,Paulmichl M,Patsch W

更新日期：2015-06-01 00:00:00

abstract：:It has been over 50years since Sir James Black developed the first beta adrenergic receptor (βAR) blocker to treat heart disease. At that time, the concept of cell surface receptors was relatively new and not widely accepted, and most of the tools currently used to characterize plasma membrane receptors had not been d...

journal_title：Trends in pharmacological sciences

authors： Kobilka BK

更新日期：2011-04-01 00:00:00

abstract：:Mitogen-activated protein kinases [MAPKs, also called extracellular signal-regulated kinases (ERKs)] are constituents of numerous signal transduction pathways, and are activated by protein kinase cascades. Intense efforts are under way to develop and evaluate compounds that target components of MAPK pathways. In this ...

journal_title：Trends in pharmacological sciences

authors： English JM,Cobb MH

更新日期：2002-01-01 00:00:00

abstract：:Ca2+ channels in the plasma membrane of T cells vitally influence Ca2+-dependent signals that lead ultimately to cytokine secretion, cellular proliferation and apoptosis. Conventional models depict the Ca2+ inrush across the T-cell membrane following T-cell receptor engagement as being due to Ca2+-release-activated Ca...

journal_title：Trends in pharmacological sciences

authors： Kotturi MF,Hunt SV,Jefferies WA

更新日期：2006-07-01 00:00:00

abstract：:Neonatal Fc receptors (FcRns) recycle IgGs by preventing their lysosome degradation. As this process also enhances half-life of pathogenic auto-IgG, inspired from the mechanisms of intravenous immunoglobulin, several inhibitors of IgG-FcRn interface have been conceived for treating autoimmune diseases. Among them, the...

journal_title：Trends in pharmacological sciences

authors： Bayry J,Kaveri SV

更新日期：2018-11-01 00:00:00

abstract：:Our growing understanding of the immunopathogenesis of inflammatory bowel disease (IBD) has opened new avenues for developing targeted therapies. These advances in treatment options targeting different mechanisms of action offer new hope for personalized management. In this review we highlight emerging novel and easil...

journal_title：Trends in pharmacological sciences

authors： Coskun M,Vermeire S,Nielsen OH

更新日期：2017-02-01 00:00:00

abstract：:Protease-activated receptors (PARs) are a ubiquitously expressed class of G-protein-coupled receptors (GPCRs) that enable cells to respond to proteases in the extracellular environment in a nuanced and dynamic manner. PAR1 is the archetypal family member and has been the object of large-scale drug development programs...

journal_title：Trends in pharmacological sciences

authors： Flaumenhaft R,De Ceunynck K

更新日期：2017-08-01 00:00:00

abstract：:Seven-transmembrane receptors are prototypic allosteric proteins with the ability to adopt numerous conformations, many of which interact with cellular partners to initiate cellular biochemical processes. Defining efficacy as the ability of ligands to stabilize some of these conformations (which, in turn, possess phys...

journal_title：Trends in pharmacological sciences

authors： Kenakin T

更新日期：2007-08-01 00:00:00

abstract：:It has been suggested that G protein-coupled receptors can act as proton transporters, with the activated G protein-coupled receptor transporting H+ across the membrane from the extracellular side to the cytoplasm. In this article, Paul Nederkoorn, Henk Timmerman and Gabriëlle Donné-Op den Kelder summarize the various...

journal_title：Trends in pharmacological sciences

authors： Nederkoorn PH,Timmerman H,Donné-Op den Kelder GM

更新日期：1995-05-01 00:00:00

abstract：:Endothelial-dependent relaxation of vascular smooth muscle cells evoked by a number of agonists, including cholinomimetics and substance P, is often accompanied by an increase (repolarization and/or hyperpolarization) in the membrane potential. This change in membrane potential appears predominantly to reflect the act...

journal_title：Trends in pharmacological sciences

authors： Garland CJ,Plane F,Kemp BK,Cocks TM

更新日期：1995-01-01 00:00:00

abstract：:Docking is now routine in virtual screening or lead optimization for drug screening and design. The number of papers related to docking has dramatically increased over the past decade. However, there are many issues to consider when undertaking a docking study. Frequent problems or issues arise, such as the wrong bind...

journal_title：Trends in pharmacological sciences

authors： Chen YC

更新日期：2015-02-01 00:00:00

abstract：:Elucidating plant-specialized biosynthetic pathways has always constituted a laborious task, notably for natural products with high pharmaceutical values. Here, we discuss emerging omics-based strategies that facilitate the identification of genes from these complex metabolic pathways, paving the way to engineered sup...

journal_title：Trends in pharmacological sciences

authors： Dugé de Bernonville T,Papon N,Clastre M,O'Connor SE,Courdavault V

更新日期：2020-03-01 00:00:00

abstract：:Clinical experience with muscarinic agonists in the symptomatic treatment of Alzheimer's disease includes studies of the effects of pilocarpine, arecoline, bethanechol, oxotremorine and RS 86. Although the results are somewhat conflicting, there is evidence that a subgroup of patients may respond with an improvement o...

journal_title：Trends in pharmacological sciences

authors： Gray JA,Enz A,Spiegel R

更新日期：1989-12-01 00:00:00

abstract：:Lithium is the simplest therapeutic agent available for the treatment of depression and has been used for over 100 years, yet no definitive mechanism for its effect has been established. Among the proposed mechanisms, two lithium-sensitive signal transduction pathways are active in the brain; these are mediated by gly...

journal_title：Trends in pharmacological sciences

authors： Williams RS,Harwood AJ

更新日期：2000-02-01 00:00:00

abstract：:Exposing the heart to brief episodes of ischaemia protects the myocardium and vascular endothelial cells against functional damage and cell death caused by subsequent prolonged ischaemia. Elucidation of the mechanisms that are involved in this phenomenon known as 'ischaemic preconditioning' and identification of drugs...

journal_title：Trends in pharmacological sciences

authors： Rubino A,Yellon DM

更新日期：2000-06-01 00:00:00

abstract：:Alanine-glyoxylate aminotransferase 2 (AGXT2) is a multifunctional mitochondrial aminotransferase that was first identified in 1978. The physiological importance of AGXT2 was largely overlooked for three decades because AGXT2 is less active in glyoxylate metabolism than AGXT1, the enzyme that is deficient in primary h...

journal_title：Trends in pharmacological sciences

authors： Rodionov RN,Jarzebska N,Weiss N,Lentz SR

更新日期：2014-11-01 00:00:00

abstract：:Recent studies in mice have identified single molecules that can delay multiple diseases of aging and extend lifespan. In theory, such molecules could prevent dozens of diseases simultaneously, potentially extending healthy years of life. In this review, we discuss recent advances, controversies, opportunities, and ch...

journal_title：Trends in pharmacological sciences

authors： Hubbard BP,Sinclair DA

更新日期：2014-03-01 00:00:00

abstract：:The tachykinin family has recently been extended by the discovery of a third tachykinin gene encoding previously unknown mammalian tachykinins (hemokinin 1, endokinin A and endokinin B) that have a widespread peripheral distribution and a tachykinin NK(1) receptor selectivity. This and the identification of other tach...

journal_title：Trends in pharmacological sciences

authors： Patacchini R,Lecci A,Holzer P,Maggi CA

更新日期：2004-01-01 00:00:00

abstract：:Cytochromes P450 are a superfamily of haem-containing monooxygenases. In mammals, two general classes of P450s exist: six families involved in steroid and bile acid biosynthetic pathways of metabolism; four families containing numerous individual P450s, mainly responsible for metabolism of foreign compounds. Many of t...

journal_title：Trends in pharmacological sciences

authors： Gonzalez FJ

更新日期：1992-09-01 00:00:00

abstract：:Advances in the understanding of the sense of smell have increased awareness of the role of olfaction in human life. Odors are perceived via specific G protein-coupled receptors (GPCRs) with cAMP as the second messenger. Drugs that interact with this signaling cascade, such as opioids, cannabinoids and sildenafil, are...

journal_title：Trends in pharmacological sciences

authors： Lötsch J,Geisslinger G,Hummel T

更新日期：2012-04-01 00:00:00

abstract：:Transcription factors comprise just over 7% of the human proteome and serve as gatekeepers of cellular function, integrating external signal information into gene expression programs that reconfigure cellular physiology at the most basic levels. Surface-initiated cell signaling pathways converge on transcription facto...

journal_title：Trends in pharmacological sciences

authors： Filtz TM,Vogel WK,Leid M

更新日期：2014-02-01 00:00:00

abstract：:The sialic-acid-binding immunoglobulin-like lectins (siglecs) comprise a family of receptors that are differentially expressed on leukocytes and other immune cells. The restricted expression of several siglecs to one or a few cell types makes them attractive targets for cell-directed therapies. The anti-CD33 (also kno...

journal_title：Trends in pharmacological sciences

authors： O'Reilly MK,Paulson JC

更新日期：2009-05-01 00:00:00

abstract：:The metabotropic glutamate (mGlu) receptors are a family of G-protein-coupled receptors (GPCRs) that regulate cell physiology throughout the nervous system. The potential of mGlu receptors as therapeutic targets has been bolstered by current research that has provided insight into the diverse modes of mGlu activation ...

journal_title：Trends in pharmacological sciences

authors： Stansley BJ,Conn PJ

更新日期：2019-04-01 00:00:00