Allosteric modulation of muscarinic acetylcholine receptors.

abstract：:Sulfoconjugation of drugs and small xenobiotic and endogenous compounds in human tissues is primarily catalysed by cytosolic forms of sulfotransferase. In most instances, sulfate conjugation is associated with a decrease in the biological activity and an increase in the excretion of the sulfated compounds. However, su...

journal_title：Trends in pharmacological sciences

authors： Falany CN

更新日期：1991-07-01 00:00:00

abstract：:Muscarinic agonists open potassium-selective K(ACh) channels in cardiac myocytes of pacemaker or atrial origin. Receptor activation is coupled to channel opening by a membrane bound guanine nucleotide-binding protein (GK) through a process that does not require cytoplasmic intermediates. We have used the muscarinic po...

journal_title：Trends in pharmacological sciences

authors： Szabo G,Otero AS

更新日期：1989-12-01 00:00:00

abstract：:Recent developments in genetic research using Saccharomyces cerevisiae have provided rapid new methods for identifying the genes that control cellular responses to treatment with a wide variety of agents, including chemicals and radiation. This significantly increases the power of yeast as a model system for studying ...

journal_title：Trends in pharmacological sciences

authors： Game JC

更新日期：2002-10-01 00:00:00

abstract：:Efforts to model and reengineer the putative binding sites of G-protein-coupled receptors (GPCRs) have led to an approach that combines small-molecule 'classical' medicinal chemistry and gene therapy. In this approach, complementary structural changes (e.g. based on novel ionic or H-bonds) are made in the receptor and...

journal_title：Trends in pharmacological sciences

authors： Jacobson KA,Gao ZG,Liang BT

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：: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：:Antipsychotic drugs (APDs), and the 'atypical' APDs in particular, are commonly associated with metabolic side effects in humans. These include glucose dysregulation, insulin resistance, hyperlipidemia, weight gain and hypertension, which put patients at increased risk of cardiometabolic disorders. The underlying biol...

journal_title：Trends in pharmacological sciences

authors： Boyda HN,Tse L,Procyshyn RM,Honer WG,Barr AM

更新日期：2010-10-01 00:00:00

abstract：:The pursuit for drugs that inhibit cyclin-dependent kinases (CDKs) has been an intense area of research for more than 15 years. The first-generation inhibitors, Flavopiridol and CY-202, are in late-stage clinical trials, but so far have demonstrated only modest activity. Several second-generation inhibitors are now in...

journal_title：Trends in pharmacological sciences

authors： Malumbres M,Pevarello P,Barbacid M,Bischoff JR

更新日期：2008-01-01 00:00:00

abstract：:The histamine H3 receptor was discovered 15 years ago, and many potent and selective H3 receptor agonists and antagonists have since been developed. Currently, much attention is being focused on the therapeutic potential of H3 receptor ligands. In this review, Rob Leurs, Patrizio Blandina, Clark Tedford and Henk Timme...

journal_title：Trends in pharmacological sciences

authors： Leurs R,Blandina P,Tedford C,Timmerman H

更新日期：1998-05-01 00:00:00

abstract：:Regulators of G-protein signaling (RGS proteins) comprise a large family of signal transduction molecules that modulate G-protein-coupled-receptor (GPCR) function. Among the RGS proteins expressed in the brain, RGS9-2 is very abundant in the striatum, a brain region involved in movement, motivation, mood and addiction...

journal_title：Trends in pharmacological sciences

authors： Traynor JR,Terzi D,Caldarone BJ,Zachariou V

更新日期：2009-03-01 00:00:00

abstract：:Kinin B1 and B2 receptors are central to the aetiology of pain and inflammation. Constitutive B2 receptors are commonly associated with the acute phase of inflammation and nociception, whereas the inducible B1 receptors are mostly linked to the chronic or persistent phase (or both). Therefore, selective, orally active...

journal_title：Trends in pharmacological sciences

authors： Campos MM,Leal PC,Yunes RA,Calixto JB

更新日期：2006-12-01 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：:Exposure of cells to agonists of receptors linked to G proteins can result in downregulation of cellular levels or redistribution of G proteins from membranes to the cytosol. Agonist-induced reductions in G protein levels have been observed for members of each of the Gs, Gi and Gq families of G proteins, are likely to...

journal_title：Trends in pharmacological sciences

authors： Milligan G

更新日期：1993-11-01 00:00:00

abstract：:It is generally accepted that muscle wasting is caused by an increase in protein breakdown which seems to be associated with an ATP-dependent, non-lysosomal proteolytic system based on conjugation of proteins to the small polypeptide ubiquitin. Increases in ubiquitin conjugates and in ubiquitin mRNAs are found in the ...

journal_title：Trends in pharmacological sciences

authors： Argilés JM,López-Soriano FJ

更新日期：1996-06-01 00:00:00

abstract：:Cannabis (marijuana) is not only a frequently abused drug but also has the potential for the development of useful agents for the treatment of emesis, anorexia and multiple sclerosis. In this article, the effects of modulation of transmitter release by cannabinoids in both the CNS and the PNS of various species, inclu...

journal_title：Trends in pharmacological sciences

authors： Schlicker E,Kathmann M

更新日期：2001-11-01 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：:Glucocorticosteroids are highly effective in controlling inflammation and the molecular mechanisms involved are now becoming clear. Activation of glucocorticoid receptors results in increased or decreased transcription of a number of genes involved in the inflammatory process. Of particular importance is the repressio...

journal_title：Trends in pharmacological sciences

authors： Barnes PJ,Adcock I

更新日期：1993-12-01 00:00:00

abstract：:G protein-coupled receptors (GPCRs) are involved in almost every (patho)physiological process, which explains their importance as drug targets. GPCRs have long been regarded as on/off-switches, which is reflected by direct activation or blockade of these receptors through the majority of marketed GPCR drugs. In recent...

journal_title：Trends in pharmacological sciences

authors： Bock A,Kostenis E,Tränkle C,Lohse MJ,Mohr K

更新日期：2014-12-01 00:00:00

abstract：:Non-steroidal anti-inflammatory drugs (NSAIDs) have been considered for treatment and prevention of Alzheimer's disease (AD) for more than two decades. Biochemical markers in the brains of individuals with AD suggest that inflammation might be a driving cause of the disease that can be suppressed by drug treatment. In...

journal_title：Trends in pharmacological sciences

authors： Weggen S,Rogers M,Eriksen J

更新日期：2007-10-01 00:00:00

abstract：:All currently available general anesthetics produce potentially deadly side effects. Unfortunately, few approaches have been developed to design safer ones, despite important advances in anesthetic mechanisms research. Cayla and colleagues recently showed that computational methods can be used to identify anesthetic l...

journal_title：Trends in pharmacological sciences

authors： McGrath M,Pence A,Raines DE

更新日期：2019-11-01 00:00:00

abstract：:Humans are exposed to mixtures of chemicals, rather than to individual chemicals. From a public health point of view, it is most relevant to answer the question of whether or not the components in a mixture interact in a way that results in an increase in their overall effect compared with the sum of the effects of th...

journal_title：Trends in pharmacological sciences

authors： Groten JP,Feron VJ,Sühnel J

更新日期：2001-06-01 00:00:00

abstract：:Classical targeted drug discovery is based on targeting druggable targets, typically kinases and receptors of which the function can be agonized or antagonized. This strategy meets difficulties in cases such as Huntington's disease (HD) and similar neurodegenerative disorders, where the pathological function of the pr...

journal_title：Trends in pharmacological sciences

authors： Yu S,Liang Y,Palacino J,Difiglia M,Lu B

更新日期：2014-02-01 00:00:00

abstract：:An unlikely animal model is gaining popularity in neuropharmacological research: the 2-mm fruit fly (Drosophila melanogaster). Drugs have been administered to adult flies in their food and, more recently, via gasses and injections. Pharmacological tools have introduced behavioral alterations in Drosophila reminiscent ...

journal_title：Trends in pharmacological sciences

authors： Manev H,Dimitrijevic N,Dzitoyeva S

更新日期：2003-01-01 00:00:00

abstract：:There is a variety of pressures on pharmacology teachers to replace real laboratory practicals with simulations but do they help students achieve the required learning objectives? In this article, the marks obtained by students in a variety of assessments using 'wet' or simulated practicals are analysed. Poorer perfor...

journal_title：Trends in pharmacological sciences

authors： Hughes IE

更新日期：2001-02-01 00:00:00

abstract：:The United States is experiencing an epidemic of opioid overdose deaths. Many of the recent fatalities are associated with illicitly manufactured fentanyl, which is being added to heroin and counterfeit pain pills. The crisis is further exacerbated by the emergence of an increasing number of novel synthetic opioids (N...

journal_title：Trends in pharmacological sciences

authors： Baumann MH,Kopajtic TA,Madras BK

更新日期：2018-12-01 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：: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：: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：:Recently, nicotinic acid adenine dinucleotide phosphate (NAADP) has been shown, using different techniques, to mobilize intracellular Ca2+ stores in invertebrate, lower vertebrate, plant and mammalian cells. This endogenous molecule might play an atypical role in Ca2+ signalling by coordinating the responses of other ...

journal_title：Trends in pharmacological sciences

authors： Genazzani AA,Billington RA

更新日期：2002-04-01 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