Therapeutic potential of histamine H3 receptor agonists and antagonists.

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：:During the past decade, translocator protein 18 kDa (TSPO), previously named peripheral benzodiazepine receptor, has gained a great deal of attention based on its use as a clinical biomarker of neuroinflammation with therapeutic potential. However, there is a paucity of knowledge on the function(s) of TSPO in glial ce...

journal_title：Trends in pharmacological sciences

authors： Guilarte TR,Loth MK,Guariglia SR

更新日期：2016-05-01 00:00:00

abstract：:The NLRP3 inflammasome is an intracellular multimeric protein complex which plays an important role in the pathogenesis of various human inflammatory diseases, such as diabetes, Alzheimer's disease and atherosclerosis. Recently, various G protein-coupled receptors (GPCRs) have been reported to be involved in the activ...

journal_title：Trends in pharmacological sciences

authors： Tang T,Gong T,Jiang W,Zhou R

更新日期：2018-09-01 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：:K(+) channels are macromolecules embedded in biological membranes, where they play a key role in cellular excitability and signal transduction pathways. Knowledge of their structure should help improve our understanding of their function and lead to the design of therapeutic compounds. Most pharmacological and structu...

journal_title：Trends in pharmacological sciences

authors： Rodríguez de la Vega RC,Merino E,Becerril B,Possani LD

更新日期：2003-05-01 00:00:00

abstract：:The affinity of a drug candidate for a biological membrane (its lipophilicity) is closely related to the pharmacologically crucial events of absorption, biodistribution, metabolization and excretion. The evolution of knowledge of biological membranes during the past two decades contrasts with the rudimentary parameter...

journal_title：Trends in pharmacological sciences

authors： Ribeiro MM,Melo MN,Serrano ID,Santos NC,Castanho MA

更新日期：2010-10-01 00:00:00

abstract：:Discoidin (DS) domains are found in eukaryotic and prokaryotic extracellular and transmembrane multidomain proteins. These small domains play different functional roles and can interact with phospholipids, glycans, and proteins, including collagens. DS domain-containing proteins are often involved in cellular adhesion...

journal_title：Trends in pharmacological sciences

authors： Villoutreix BO,Miteva MA

更新日期：2016-08-01 00:00:00

abstract：:Erythropoietin (EPO) has emerged as a versatile growth factor that has transcended its traditional role as a mediator of erythroid maturation to one that modulates stem cell development, cellular protection and angiogenesis in the brain. As a possible candidate for nervous system disorders, it becomes crucial to under...

journal_title：Trends in pharmacological sciences

authors： Maiese K,Li F,Chong ZZ

更新日期：2004-11-01 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：:Conus venoms from marine cone snails continue to provide novel bioactive components. Two new classes of conopeptide specifically block alpha(1)-adrenoceptors (rho-conopeptide) and noradrenaline transporters (chi-conopeptides). Both classes are small peptides with two disulfide bonds. Rho-conopeptide is structurally si...

journal_title：Trends in pharmacological sciences

authors： Harvey AL

更新日期：2002-05-01 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：:Addiction biology has focused on the mechanisms of the positive and negative reinforcing actions of addictive drugs but neglected potential benefits. Two new studies provide the first insights into a neurobiology of psychoactive drug instrumentalization. This may help us design better models for addiction neuroscience...

journal_title：Trends in pharmacological sciences

authors： Müller CP,Kornhuber J

更新日期：2017-06-01 00:00:00

abstract：:The broad importance of receptor-activated phosphoinositide hydrolysis in the physiological action of hormones, neurotransmitters and growth factors has sparked interest in the study of transmembrane signalling events responsible for activation of phospholipase C. As with receptors involved in regulation of adenylyl c...

journal_title：Trends in pharmacological sciences

authors： Boyer JL,Hepler JR,Harden TK

更新日期：1989-09-01 00:00:00

abstract：:From the deep part of the main ligand-binding crevice, a minor, often shallower pocket extends between the extracellular ends of transmembrane domains (TM)-I, II, III and VII of 7TM receptors. This minor binding pocket is defined by a highly conserved kink in TM-II that is induced by a proline residue located in one o...

journal_title：Trends in pharmacological sciences

authors： Rosenkilde MM,Benned-Jensen T,Frimurer TM,Schwartz TW

更新日期：2010-12-01 00:00:00

abstract：:Platelet activating factor (PAF) is a phospholipid mediator of inflammation and stimulates anion secretion in animals and in isolated preparations of human colon. Nitric oxide (NO), synthesized from the amino acid L-arginine, is an important enteric inhibitory neurotransmitter. In addition, NO-donating compounds stimu...

journal_title：Trends in pharmacological sciences

authors： Izzo AA,Gaginella TS,Mascolo N,Capasso F

更新日期：1998-10-01 00:00:00

abstract：:Cyclic AMP (cAMP) steers the generation of basal heart beat in the sinoatrial node. It also induces sinoatrial tachycardia and increased cardiac force, elicited through activation of Gs-protein-coupled receptors (GsPCRs). Phosphodiesterases (PDEs) hydrolyse cAMP. In the heart mainly PDE3 and PDE4 would be expected to ...

journal_title：Trends in pharmacological sciences

authors： Kaumann AJ

更新日期：2011-07-01 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 myeloid-derived suppressor cell (MDSC) is the 'queen bee' of the tumor microenvironment. MDSCs protect the cancer from the patient's immune system, make the tumor resistant to immunotherapy, and allow the tumor to thrive while the patient withers away. Eliminating MDSCs should improve response rates to cancer ther...

journal_title：Trends in pharmacological sciences

authors： Tesi RJ

更新日期：2019-01-01 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：:Since G protein-coupled receptors (GPCRs) belong to a very large superfamily of evolutionarily related receptors (>800 members in humans), and due to the rapid progress on their structural biology, they are ideal candidates for polypharmacology studies. Broad screening and bioinformatics/chemoinformatics have been app...

journal_title：Trends in pharmacological sciences

authors： Jacobson KA,Costanzi S,Paoletta S

更新日期：2014-12-01 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：: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：: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：: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：:In 1964, the psychoactive ingredient of Cannabis sativa, Δ(9)-tetrahydrocannabinol (THC), was isolated. Nearly 30 years later the endogenous counterparts of THC, collectively termed endocannabinoids (eCBs), were discovered: N-arachidonoylethanolamine (anandamide) (AEA) in 1992 and 2-arachidonoylglycerol (2-AG) in 1995...

journal_title：Trends in pharmacological sciences

authors： Maccarrone M,Bab I,Bíró T,Cabral GA,Dey SK,Di Marzo V,Konje JC,Kunos G,Mechoulam R,Pacher P,Sharkey KA,Zimmer A

更新日期：2015-05-01 00:00:00

abstract：:Gene therapy is a new field of medical research that has great potential to influence the course of treatment of human disease. The lung has been a particularly attractive target organ for gene therapy due to its accessibility and the identification of genetic deficits for a number of lung diseases. Several clinical t...

journal_title：Trends in pharmacological sciences

authors： Ennist DL

更新日期：1999-06-01 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 concept that receptors can exist in multiple conformational states is becoming a physical reality. A fundamental question is how many active states need to be proposed in order to account for pharmacological observations, in particular, the finding that the same receptor type can exhibit a different agonist pharma...

journal_title：Trends in pharmacological sciences

authors： Leff P,Scaramellini C,Law C,McKechnie K

更新日期：1997-10-01 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：:During the past decade remarkable progress in molecular genetics and the possibility of manipulating cells so that the expression of genes can directly 'report' on drug activity has produced major changes in drug development strategies. The recent description and pharmacological validation of reporter mice for in vivo...

journal_title：Trends in pharmacological sciences

authors： Maggi A,Ottobrini L,Biserni A,Lucignani G,Ciana P

更新日期：2004-06-01 00:00:00