Non-peptide antagonists for kinin B1 receptors: new insights into their therapeutic potential for the management of inflammation and pain.

abstract：:The breast cancer resistance protein [BCRP (also known as ABCG2)] belongs to the ATP binding cassette (ABC) family of transmembrane drug transporters. BCRP has a broad substrate specificity and actively extrudes a wide variety of drugs, carcinogens and dietary toxins from cells. Situated in the apical plasma membrane ...

journal_title：Trends in pharmacological sciences

authors： van Herwaarden AE,Schinkel AH

更新日期：2006-01-01 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：:Stem cells derived from pre-implantation human embryos or from somatic cells by reprogramming are pluripotent and self-renew indefinitely in culture. Pluripotent stem cells are unique in being able to differentiate to any cell type of the human body. Differentiation towards the cardiac lineage has attracted significan...

journal_title：Trends in pharmacological sciences

authors： Braam SR,Passier R,Mummery CL

更新日期：2009-10-01 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：:Mitogen-activated protein kinases [MAPKs, also called extracellular signal-regulated kinases (ERKs)] are constituents of numerous signal transduction pathways, and are activated by protein kinase cascades. Intense efforts are under way to develop and evaluate compounds that target components of MAPK pathways. In this ...

journal_title：Trends in pharmacological sciences

authors： English JM,Cobb MH

更新日期：2002-01-01 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：:Apoptosis is an area of intense scientific interest, which encompasses the study of and triggers mechanisms involved in mediating the cell biology of programmed cell death. A number of low molecular weight compounds have been used to inhibit or enhance this fundamental cellular process and so apoptosis has now become ...

journal_title：Trends in pharmacological sciences

authors： Kinloch RA,Treherne JM,Furness LM,Hajimohamadreza I

更新日期：1999-01-01 00:00:00

abstract：:The rise of multidrug-resistant pathogens and the dearth of new antibiotic development place an existential strain on successful infectious disease therapy. Breakthrough strategies that go beyond classical antibiotic mechanisms are needed to combat this looming public health catastrophe. Reconceptualizing antibiotic t...

journal_title：Trends in pharmacological sciences

authors： Munguia J,Nizet V

更新日期：2017-05-01 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：: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：: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：:Annexin A1 (ANXA1) is an endogenous protein known to have potent anti-inflammatory properties in the peripheral system. It has also been detected in the brain, but its function there is still ambiguous. In this review, we have, for the first time, collated the evidence currently available on the function of ANXA1 in t...

journal_title：Trends in pharmacological sciences

authors： Solito E,McArthur S,Christian H,Gavins F,Buckingham JC,Gillies GE

更新日期：2008-03-01 00:00:00

abstract：:Several lines of evidence suggest that adenosine may be an endogenous protective agent in cerebral ischaemia. Adenosine is normally present in the extracellular fluid in most tissues of the body, including the brain, and its level increases dramatically following hypoxia or ischaemia. The rate of adenosine production ...

journal_title：Trends in pharmacological sciences

authors： Rudolphi KA,Schubert P,Parkinson FE,Fredholm BB

更新日期：1992-12-01 00:00:00

abstract：:The current classification for 5-HT2 receptors accommodates three subtypes. In addition to the originally defined 5-HT2 receptor, sanctuary is now provided for the structurally related 5-HT1c receptor (now 5-HT2c) and at least one atypical 5-HT receptor subtype. The strong functional union of this family is reflected ...

journal_title：Trends in pharmacological sciences

authors： Baxter G,Kennett G,Blaney F,Blackburn T

更新日期：1995-03-01 00:00:00

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：: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：:Pharmacological studies as well as molecular cloning of 5-HT receptors have revealed a multiplicity of receptor subtypes, not only in mammals but, as discussed in this review by René Hen, also in molluscs and arthropods. Most of these receptors belong to the G protein-coupled receptor family, and their mechanism of ac...

journal_title：Trends in pharmacological sciences

authors： Hen R

更新日期：1992-04-01 00:00:00

abstract：:Clinical implementation of two recently approved antisense RNA therapeutics - Exondys51® to treat Duchenne muscular dystrophy (Duchenne MD) and Spinraza® as a treatment for spinal muscular atrophy (SMA) - highlights the therapeutic potential of antisense oligonucleotides (ASOs). As shown in the Duchenne and Becker cas...

journal_title：Trends in pharmacological sciences

authors： Li D,Mastaglia FL,Fletcher S,Wilton SD

更新日期：2018-11-01 00:00:00

abstract：:Thiol-based drugs are considered as mucolytics because they decrease the viscosity and mostly decrease the elasticity of bronchial secretions by reducing disulfide bonds in proteins. However, they can also act as antioxidant drugs directly through free sulfhydryl groups that serve as a source of reducing equivalents, ...

journal_title：Trends in pharmacological sciences

authors： Cazzola M,Calzetta L,Page C,Rogliani P,Matera MG

更新日期：2019-07-01 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：: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：: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：: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：: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：:It has taken 17 years from the first identification of a voltage-gated Ca2+ channel (CaV) beta-subunit as a band on a gel following purification of skeletal muscle dihydropyridine (DHP) receptors in 1987 to the publication of key information on the structures of Ca2+ channel beta-subunits. Three recent X-ray crystallo...

journal_title：Trends in pharmacological sciences

authors： Richards MW,Butcher AJ,Dolphin AC

更新日期：2004-12-01 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：:The potent pro-inflammatory cytokines tumour necrosis factor alpha (TNF-alpha) and interleukin 1 (IL-1) are capable of triggering biologically similar effects through activation of the same set of transcription factors. Based on recent findings it is now becoming evident that certain members of the mitogen-activated p...

journal_title：Trends in pharmacological sciences

authors： Eder J

更新日期：1997-09-01 00:00:00

abstract：:5-HT(3) receptors are widely distributed in the CNS and PNS where they participate in a variety of physiological processes. Native 5-HT(3) receptors in the CNS display functional and pharmacological heterogeneity, suggesting the existence of multiple receptor subunits. However, recent evidence suggests that of the two...

journal_title：Trends in pharmacological sciences

authors： van Hooft JA,Yakel JL

更新日期：2003-04-01 00:00:00

abstract：:Folates are essential for key biosynthetic processes in mammalian cells and play a crucial role in the maintenance of central nervous system homeostasis. Mammals lack the metabolic capacity for folate biosynthesis; hence, folate requirements are largely met through dietary sources. To date, three major folate transpor...

journal_title：Trends in pharmacological sciences

authors： Alam C,Kondo M,O'Connor DL,Bendayan R

更新日期：2020-05-01 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