Protein kinase Calpha: disease regulator and therapeutic target.

abstract：:The imbalance theory proposes that arterial thrombosis is dependent on a ratio or balance between the cyclooxygenase (COX)-1-dependent generation of thromboxane in platelets and the COX-2-dependent generation of prostacyclin in the endothelium. Accordingly, by reducing endothelium-derived prostacyclin levels, selectiv...

journal_title：Trends in pharmacological sciences

authors： Flavahan NA

更新日期：2007-03-01 00:00:00

abstract：:Since conformational flexibility, which is required for the function of a protein, comes at the expense of structural stability, many proteins, including G-protein-coupled receptors (GPCRs), are under constant risk of misfolding and aggregation. In this regard GPR37 (also named PAEL-R and ETBR-LP-1) takes a prominent ...

journal_title：Trends in pharmacological sciences

authors： Leinartaité L,Svenningsson P

更新日期：2017-08-01 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：: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 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：:As we have learnt from earlier articles in our series on the pharmacology of excitatory amino acids, neurons and glia express several subtypes of excitatory amino acid receptor, the activation of which increases intracellular free calcium ion concentration. In this sixth article, Mark Mayer and Richard Miller detail t...

journal_title：Trends in pharmacological sciences

authors： Mayer ML,Miller RJ

更新日期：1990-06-01 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：: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：:Cannabinoids have emerged as powerful drug candidates for the treatment of inflammatory and autoimmune diseases due to their immunosuppressive properties. Significant clinical and experimental data on the use of cannabinoids as anti-inflammatory agents exist in many autoimmune disease settings, but virtually no studie...

journal_title：Trends in pharmacological sciences

authors： Nagarkatti M,Rieder SA,Hegde VL,Kanada S,Nagarkatti P

更新日期：2010-08-01 00:00:00

abstract：:N-Methyl-D-aspartate (NMDA) receptors are tetrameric ion channels containing two of four possible GluN2 subunits. These receptors have been implicated for decades in neurological diseases such as stroke, traumatic brain injury, dementia and schizophrenia. The GluN2 subunits substantially contribute to functional diver...

journal_title：Trends in pharmacological sciences

authors： Ogden KK,Traynelis SF

更新日期：2011-12-01 00:00:00

abstract：:It is generally accepted that seven-transmembrane receptors have the capacity to regulate cellular signaling systems in the absence of occupancy by a ligand (i.e. the receptors display constitutive activity). Drugs can increase (agonists), decrease (inverse agonists) or not change (antagonists) receptor activity towar...

journal_title：Trends in pharmacological sciences

authors： Berg KA,Harvey JA,Spampinato U,Clarke WP

更新日期：2005-12-01 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：:Traditional African medicine (TAM) is a shorthand reference to indigenous forms of healing that are practiced all over Africa. Although TAM is based on the accumulated experience of ancient Africans, its mode of transmission by word-of-mouth has hindered emergence of a generally accepted theory and hence of the system...

journal_title：Trends in pharmacological sciences

authors： Okpako DT

更新日期：1999-12-01 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：: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：: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：:Several clinical studies document a greater discrimination between asthmatic and healthy subjects in bronchial responsiveness to a range of stimuli such as cold air, distilled water and sodium metabisulphite, than to conventional bronchoconstrictor agonists including histamine and methacholine. One of the mechanisms t...

journal_title：Trends in pharmacological sciences

authors： Spina D,Shah S,Harrison S

更新日期：1998-11-01 00:00:00

abstract：:Histamine-containing neurons and histamine H1 receptors are distributed within the brain and peripheral tissues. The results of physiological and pharmacological studies have revealed that brain histamine and H1 receptors are involved in the regulation of feeding and obesity in rodents. The adipocytokine leptin regula...

journal_title：Trends in pharmacological sciences

authors： Masaki T,Yoshimatsu H

更新日期：2006-05-01 00:00:00

abstract：:Recruitment of leukocytes either during development or to the site of injury is crucial. The molecular regulation of cell trafficking is complex but well orchestrated by the temporal and spatial expression of a multitude of chemokines (chemoattractant cytokines) and chemokine receptors. The chemokines, classified prim...

journal_title：Trends in pharmacological sciences

authors： Devalaraja MN,Richmond A

更新日期：1999-04-01 00:00:00

abstract：:Heat shock proteins (HSPs) constitute a large family of proteins involved in protein folding and maturation whose expression is induced by heat shock or other stressors. The major groups are classified based on their molecular weights and include HSP27, HSP40, HSP60, HSP70, HSP90, and large HSPs. HSPs play a significa...

journal_title：Trends in pharmacological sciences

authors： Wu J,Liu T,Rios Z,Mei Q,Lin X,Cao S

更新日期：2017-03-01 00:00:00

abstract：:Molecular forms of acetylcholinesterase exhibit tissue-specific distribution, and each form is anchored to the cell surface via a particular post-translational modification of the catalytic subunit. Nibaldo Inestrosa and Alejandra Perelman review evidence that heparan sulphate proteoglycans are the extracellular matri...

journal_title：Trends in pharmacological sciences

authors： Inestrosa NC,Perelman A

更新日期：1989-08-01 00:00:00

abstract：:Ischaemia-reperfusion (I/R) injury is a common feature of several diseases associated with high morbidity and mortality, such as stroke and myocardial infarction. The damaged tissue displays cardinal signs of inflammation and microvascular injury that, unless resolved, lead to long-term tissue damage with associated d...

journal_title：Trends in pharmacological sciences

authors： Gavins FN

更新日期：2010-06-01 00:00:00

abstract：:Within the past six months, isolation of cDNA or genomic clones has been reported for three 5-HT receptors, the 5-HT1C, 5-HT1A and 5-HT2 subtypes. As members of the G protein receptor superfamily, all three 5-HT receptor clones encode single-subunit proteins containing approximately 450 amino acids arrayed as seven in...

journal_title：Trends in pharmacological sciences

authors： Hartig PR

更新日期：1989-02-01 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

abstract：:Carbonic anhydrase isoform IX (CA IX) is highly overexpressed in many types of cancer. Its expression, which is regulated by the HIF-1 transcription factor, is strongly induced by hypoxia and correlates with a poor response to classical chemo- and radiotherapies. CA IX contributes to acidification of the tumor environ...

journal_title：Trends in pharmacological sciences

authors： Thiry A,Dogné JM,Masereel B,Supuran CT

更新日期：2006-11-01 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：:Therapeutic targeting of the processes that regulate histone modification is a growing area of scientific exploration. Although most interest has concentrated on the various families of enzymes that contribute to these processes, this review focuses on emerging data demonstrating the chemical tractability and therapeu...

journal_title：Trends in pharmacological sciences

authors： Prinjha RK,Witherington J,Lee K

更新日期：2012-03-01 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：:The GPR119 receptor is expressed predominantly in pancreatic β cells and in enteroendocrine cells. It is a major target for the development of anti-diabetic drugs that through GPR119 activation may stimulate both insulin and GLP-1 release. GPR119 can be activated by oleoylethanolamide and several other endogenous lipi...

journal_title：Trends in pharmacological sciences

authors： Hansen HS,Rosenkilde MM,Holst JJ,Schwartz TW

更新日期：2012-07-01 00:00:00

abstract：:HIV-1 integrase (IN) executes the insertion of proviral DNA into the host cell genome, an essential step in the retroviral life cycle. This is a multi-step process that starts in the cytosol and culminates in the nucleus of the infected cell. It is becoming increasingly clear that IN interacts with a wide range of dif...

journal_title：Trends in pharmacological sciences

authors： Al-Mawsawi LQ,Neamati N

更新日期：2007-10-01 00:00:00