Your bleeding heart: lessons from low tissue factor expression in mice.

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：:Schizophrenia is a grave psychiatric disorder with psychotic symptoms and an enigmatic etiology. Family studies have strongly indicated that genetic risk factors have a role in this disease. Recent findings, together with previously established evidence, highlight the PDZ-domain-containing protein interacting with C-k...

journal_title：Trends in pharmacological sciences

authors： Dev KK,Henley JM

更新日期：2006-11-01 00:00:00

abstract：:Progress in understanding the genetic changes that drive tumorigenesis has enabled the development of molecularly targeted anticancer therapy. The first small molecule targeted to a specific protein was imatinib mesylate (Gleevec, STI571), which is used to treat chronic myeloid leukemia (CML). A recent article present...

journal_title：Trends in pharmacological sciences

authors： Michor F

更新日期：2007-05-01 00:00:00

abstract：:Due to its negative chronotropic and inotropic effects, adenosine has to date been considered as a cardiodepressant agent. However, adenosine increases ventricular automaticity. This review by Jesus Hernández and Alexandre Ribeiro discusses the experimental and clinical evidence for the excitatory effects of adenosine...

journal_title：Trends in pharmacological sciences

authors： Hernández J,Ribeiro JA

更新日期：1996-04-01 00:00:00

abstract：:Amyotrophic lateral sclerosis (ALS) is an incurable disease that arises from the progressive loss of motoneurons. Even when caused by a single gene defect, as in the case of mutations in the enzyme Cu-Zn superoxide dismutase (SOD1), ALS is the result of a complex cascade that involves crosstalk among motoneurons, glia...

journal_title：Trends in pharmacological sciences

authors： Carrì MT,Grignaschi G,Bendotti C

更新日期：2006-05-01 00:00:00

abstract：:The translocator protein (TSPO), an 18-kDa transmembrane protein primarily found in the outer mitochondrial membrane, is evolutionarily conserved and widely distributed across species. In mammals, TSPO has been described as a key member of a multiprotein complex involved in many putative functions and, over the years,...

journal_title：Trends in pharmacological sciences

authors： Lacapere JJ,Duma L,Finet S,Kassiou M,Papadopoulos V

更新日期：2020-02-01 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：:The British Pharmacological Society (BPS) is currently celebrating its 75th anniversary. It is therefore a young society compared with some other biomedical societies and particularly when compared with the origins of the oldest learned societies. In this article, I briefly review the origins of learned societies and ...

journal_title：Trends in pharmacological sciences

authors： Green AR

更新日期：2006-03-01 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：: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：:Drugs that cause liver injury often 'stress' mitochondria and activate signal transduction pathways important in determining cell survival or death. In most cases, hepatocytes adapt to the drug-induced stress by activating adaptive signaling pathways, such as mitochondrial adaptive responses and nuclear factor erythro...

journal_title：Trends in pharmacological sciences

authors： Han D,Dara L,Win S,Than TA,Yuan L,Abbasi SQ,Liu ZX,Kaplowitz N

更新日期：2013-04-01 00:00:00

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：:The injectisome type three secretion system (T3SS) is a major virulence factor in Pseudomonas aeruginosa. This bacterium is responsible for severe infections in immunosuppressed or cystic fibrosis patients and has become resistant to many antibiotics. Inhibitors of T3SS may therefore constitute an innovative therapeut...

journal_title：Trends in pharmacological sciences

authors： Anantharajah A,Mingeot-Leclercq MP,Van Bambeke F

更新日期：2016-09-01 00:00:00

abstract：:Pharmacology as a modern science was introduced in China approximately 150 years ago, and has been used since then to study traditional Chinese medicine (TCM). Pharmacology has experienced its own development over this time and continues to provide new tools for the study of TCM. In the present review, three models fo...

journal_title：Trends in pharmacological sciences

authors： Liu X,Wu WY,Jiang BH,Yang M,Guo DA

更新日期：2013-11-01 00:00:00

abstract：:Muscarinic acetylcholine receptor subtypes m1, m3 and m5 couple strongly to phosphatidylinositol turnover and hence to intracellular Ca2+ concentration via pertussis toxin (PTX) sensitive and insensitive G proteins. The m2 and m4 muscarinic receptor subtypes strongly inhibit adenylyl cyclase production via PTX sensiti...

journal_title：Trends in pharmacological sciences

authors： Lechleiter J,Peralta E,Clapham D

更新日期：1989-12-01 00:00:00

abstract：:Dimerization is fairly common in the G-protein-coupled receptor (GPCR) superfamily. First attempts to rationalize this phenomenon gave rise to an idea that two receptors in a dimer could be necessary to bind a single molecule of G protein or arrestin. Although GPCRs, G proteins and arrestins were crystallized only in ...

journal_title：Trends in pharmacological sciences

authors： Gurevich VV,Gurevich EV

更新日期：2008-05-01 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：:Upregulation of binding to nicotinic acetylcholine receptors (nAChRs) is observed in the brains of both smokers and animals chronically exposed to nicotine, although whether this in vivo change is accompanied by an increase in receptor function is unknown. In vitro recordings indicate that alpha4beta2- and alpha7-subt...

journal_title：Trends in pharmacological sciences

authors： Buisson B,Bertrand D

更新日期：2002-03-01 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：:Drugs of abuse are very powerful reinforcers, and even in conditions of limited access (where the organism is not dependent) these drugs will motivate high rates of operant responding. This presumed hedonic property and the drugs' neuropharmacological specificity provide a means of studying the neuropharmacology and n...

journal_title：Trends in pharmacological sciences

authors： Koob GF

更新日期：1992-05-01 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：:Urinary incontinence and other urinary storage symptoms are frequent in the general population but available treatments have limited efficacy and tolerability. Rho kinase (ROCK) has a central role in the regulation of smooth muscle contraction, including that of the urinary bladder. Recent experimental evidence indica...

journal_title：Trends in pharmacological sciences

authors： Peters SL,Schmidt M,Michel MC

更新日期：2006-09-01 00:00:00

abstract：:The vascular endothelium is a remarkably heterogeneous organ. In addition to well-characterized anatomical diversity in situ, specific differences are increasingly being recognized between surface antigens on endothelial cells from different tissues, including absence of the classic endothelial marker factor VIII-rela...

journal_title：Trends in pharmacological sciences

authors： McCarthy SA,Kuzu I,Gatter KC,Bicknell R

更新日期：1991-12-01 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：: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：:Cytochrome P450 3A (CYP3A) enzymes metabolize a wide variety of xenobiotics including many drugs. Because CYP3A is localized in both the liver and intestine, it can make a major contribution to the presystemic elimination of substrate drugs after oral administration ('first-pass metabolism'). However, assessments of t...

journal_title：Trends in pharmacological sciences

authors： van Herwaarden AE,van Waterschoot RA,Schinkel AH

更新日期：2009-05-01 00:00:00

abstract：:Prospecting the full biodiversity of nature to find leads for new drugs is not necessary. Because finding leads is aimed at identifying biological activity, structure is of secondary importance. Furthermore, although natural chemical diversity might be unrivalled, functional diversity is bound to be considerably less....

journal_title：Trends in pharmacological sciences

authors： Tulp M,Bohlin L

更新日期：2002-05-01 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：: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 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