The use of resonance energy transfer in high-throughput screening: BRET versus FRET.

abstract：:The therapeutic advantage of reducing the activity of interleukin 1 (IL-1) resides in preventing its deleterious biological effects without interfering with homeostasis. As such, methods attempting to block the production or activity of IL-1 have now entered clinical trials. For example, IL-1 induction of prostaglandi...

journal_title：Trends in pharmacological sciences

authors： Dinarello CA

更新日期：1993-05-01 00:00:00

abstract：:Receptors that are coupled to the production of inositol (1,4,5)-trisphosphate cause an increase in cytosolic free Ca2+ concentration as a consequence of both Ca2+ mobilization from intracellular stores and Ca2+ influx through the plasma membrane. Although this latter phenomenon appears attributable to the activation ...

journal_title：Trends in pharmacological sciences

authors： Fasolato C,Innocenti B,Pozzan T

更新日期：1994-03-01 00:00:00

abstract：:Pairing orphan G-protein-coupled receptors (GPCRs) to potential ligands found in tissue extracts or in libraries of synthetic compounds has identified an ever-increasing number of transmitters, some of which are novel, some of which were previously known and, more recently, some of which are unexpected. These discover...

journal_title：Trends in pharmacological sciences

authors： Civelli O

更新日期：2005-01-01 00:00:00

abstract：:The melanocortin receptors are a subfamily of G-protein-coupled, rhodopsin-like receptors that are rapidly being acknowledged as an extremely promising target for pharmacological intervention in a variety of different inflammatory pathologies, including stroke. Stroke continues to be a leading cause of death worldwide...

journal_title：Trends in pharmacological sciences

authors： Holloway PM,Smith HK,Renshaw D,Flower RJ,Getting SJ,Gavins FN

更新日期：2011-02-01 00:00:00

abstract：:This year marks the 90th anniversary of the publication of Hans Horst Meyer's classic paper in which he proposed that the ability of a substance to produce narcosis or anesthesia is governed by its partition coefficient. In this article, Robert Lipnick describes the experiments carried out by Meyer and his colleagues ...

journal_title：Trends in pharmacological sciences

authors： Lipnick RL

更新日期：1989-07-01 00:00:00

abstract：:Salvinorin A, a neoclerodane diterpene, is the most potent naturally occurring hallucinogen known and rivals the synthetic hallucinogen lysergic acid diethylamide in potency. Recently, the molecular target of salvinorin A was identified as the kappa opioid receptor (KOR). Salvinorin A represents the only known non-nit...

journal_title：Trends in pharmacological sciences

authors： Sheffler DJ,Roth BL

更新日期：2003-03-01 00:00:00

abstract：:Attempts to develop neuroprotective treatments for neurodegenerative disorders have not yet been clinically successful. Axonal degeneration has been recognized as a predominant driver of disability and disease progression in central nervous system (CNS) diseases such as amyotrophic lateral sclerosis (ALS), multiple sc...

journal_title：Trends in pharmacological sciences

authors： Krauss R,Bosanac T,Devraj R,Engber T,Hughes RO

更新日期：2020-04-01 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：:Oxycodone is a semisynthetic opioid analgesic that is increasingly used for the treatment of acute, cancer, and chronic non-malignant pain. Oxycodone was synthesized in 1917 but its pharmacological properties were not thoroughly studied until recently. Oxycodone is a fairly selective μ-opioid receptor agonist, but the...

journal_title：Trends in pharmacological sciences

authors： Olkkola KT,Kontinen VK,Saari TI,Kalso EA

更新日期：2013-04-01 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 physiological roles of chemokine receptors have expanded beyond host defense and now represent important targets for intervention in several disease indications. Chemokine receptors have joined the ranks of other members of the G-protein-coupled receptor (GPCR) family in therapeutic potential as small-molecule che...

journal_title：Trends in pharmacological sciences

authors： Onuffer JJ,Horuk R

更新日期：2002-10-01 00:00:00

abstract：:Parkinson's disease (PD) is a progressive neurodegenerative disorder. Although therapies that treat the symptoms of the disease have proven efficacy, strategies that slow or stop the neurodegenerative process are currently not available. Recently, the National Institute of Neurological Disorders and Stroke (NINDS) con...

journal_title：Trends in pharmacological sciences

authors： Meissner W,Hill MP,Tison F,Gross CE,Bezard E

更新日期：2004-05-01 00:00:00

abstract：:It is now established that most of the approximately 800 G-protein-coupled receptors (GPCRs) are regulated by phosphorylation in a process that results in the recruitment of arrestins, leading to receptor desensitization and the activation of arrestin-dependent processes. This generalized view of GPCR regulation, howe...

journal_title：Trends in pharmacological sciences

authors： Tobin AB,Butcher AJ,Kong KC

更新日期：2008-08-01 00:00:00

abstract：:The fruit fly Drosophila melanogaster has been used for modeling cancer and as an in vivo tool for the validation and/or development of cancer therapeutics. The impetus for the use of Drosophila in cancer research stems from the high conservation of its signaling pathways, lower genetic redundancy, short life cycle, g...

journal_title：Trends in pharmacological sciences

authors： Yadav AK,Srikrishna S,Gupta SC

更新日期：2016-09-01 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：:Since the cloning and expression of many of the G protein-coupled receptors during the 1980s, there has been a massive increase in our understanding of many aspects of their function. The use of molecular biology to engineer and express mutant receptors has made it possible to determine key amino acids involved in rec...

journal_title：Trends in pharmacological sciences

authors： Haddad el-B,Rousell J

更新日期：1998-08-01 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：:Data sets from recent large-scale projects can be integrated into one unified puzzle that can provide new insights into how drugs and genetic perturbations applied to human cells are linked to whole-organism phenotypes. Data that report how drugs affect the phenotype of human cell lines and how drugs induce changes in...

journal_title：Trends in pharmacological sciences

authors： Ma'ayan A,Rouillard AD,Clark NR,Wang Z,Duan Q,Kou Y

更新日期：2014-09-01 00:00:00

abstract：:Current medicines for the clinical management of inflammatory diseases act by inhibiting specific enzymes or antagonising specific receptors or blocking their ligands. In the past decade, a new paradigm in our understanding of the inflammatory process has emerged with the appreciation of genetic, molecular, and cellul...

journal_title：Trends in pharmacological sciences

authors： Perretti M,Leroy X,Bland EJ,Montero-Melendez T

更新日期：2015-11-01 00:00:00

abstract：:In the past 20 years we have learned a great deal about GABAA receptor (GABAAR) subtypes, and which behaviors are regulated or which drug effects are mediated by each subtype. However, the question of where GABAARs involved in specific drug effects and behaviors are located in the brain remains largely unanswered. We ...

journal_title：Trends in pharmacological sciences

authors： Engin E,Benham RS,Rudolph U

更新日期：2018-08-01 00:00:00

abstract：:A family of peptides that shares a common C-terminal sequence (Phe-X-Gly-Leu-MetNH2) exists in mammalian and non-mammalian species. In mammals, three of these peptides (substance P, neurokinin A and neurokinin B) satisfy the criteria to be considered as neurotransmitters either in the central, peripheral or enteric ne...

journal_title：Trends in pharmacological sciences

authors： Maggi CA

更新日期：2000-05-01 00:00:00

abstract：:Enveloped viruses pose an important health threat because most of the persistent and many emerging viruses are enveloped. In particular, newly emerging viruses create a need to develop broad-spectrum antivirals, which usually are obtained by targeting host cell factors. Persistent viruses have developed efficient stra...

journal_title：Trends in pharmacological sciences

authors： Wisskirchen K,Lucifora J,Michler T,Protzer U

更新日期：2014-09-01 00:00:00

abstract：:Genes encoding glutamate receptor channel subunits were identified in genomes from Drosophila melanogaster and Caenorhabditis elegans by homology search with amino acid sequences that participate in the conserved channel pore. The predicted sequences of the putative glutamate receptor subunits revealed a distinct chan...

journal_title：Trends in pharmacological sciences

authors： Sprengel R,Aronoff R,Völkner M,Schmitt B,Mosbach R,Kuner T

更新日期：2001-01-01 00:00:00

abstract：:Behavioural pharmacology is an interdisciplinary field at the intersection of several research areas that ultimately lead to the development of drugs for clinical use and build understanding of how brain functions enable cognition and behaviour. In this article, the development of behavioural pharmacology in the UK is...

journal_title：Trends in pharmacological sciences

authors： Robbins TW,Murphy ER

更新日期：2006-03-01 00:00:00

abstract：:Inter-organelle signaling plays important roles in many physiological functions. Endoplasmic reticulum (ER)-mitochondrion signaling affects intramitochondrial calcium (Ca(2+)) homeostasis and cellular bioenergetics. ER-nucleus signaling attenuates ER stress. ER-plasma membrane signaling regulates cytosolic Ca(2+) home...

journal_title：Trends in pharmacological sciences

authors： Su TP,Hayashi T,Maurice T,Buch S,Ruoho AE

更新日期：2010-12-01 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：:Pharmacology training in Canada was initiated at McGill University in Montréal in 1824, and there are now 17 pharmacology departments in Canada offering graduate training to more than 500 students. In this article, Gerald Marks reviews the growth of pharmacology in Canada since the early 19th century in both academic ...

journal_title：Trends in pharmacological sciences

authors： Marks GS

更新日期：1994-07-01 00:00:00

abstract：:5-Hydroxytryptamine (5-HT), dopamine and norepinephrine are important monoamine neurotransmitters implicated in multiple brain mechanisms and regulated by high-affinity transmembrane monoamine transporters. Although knockout mice lacking 5-HT, dopamine or norepinephrine transporters are widely used to assess brain mon...

journal_title：Trends in pharmacological sciences

authors： Kalueff AV,Ren-Patterson RF,Murphy DL

更新日期：2007-03-01 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：:Inappropriate production of the iron-regulatory hormone hepcidin contributes to the pathogenesis of common iron disorders. Absolute or relative deficiency of hepcidin causes iron overload in hereditary hemochromatosis and iron-loading anemias. Elevated hepcidin causes iron restriction in inflammatory conditions includ...

journal_title：Trends in pharmacological sciences

authors： Ruchala P,Nemeth E

更新日期：2014-03-01 00:00:00