Molecular biology of 5-HT receptors.

abstract：:Since the cloning and expression of many of the G protein-coupled receptors during the 1980s, there has been a massive increase in our understanding of many aspects of their function. The use of molecular biology to engineer and express mutant receptors has made it possible to determine key amino acids involved in rec...

journal_title：Trends in pharmacological sciences

authors： Haddad el-B,Rousell J

更新日期：1998-08-01 00:00:00

abstract：:Signal transducer and activator of transcription 3 (STAT3) plays crucial roles in several cellular processes such as cell proliferation and survival, and has been found to be aberrantly activated in many cancers. Much research has explored the leading mechanisms for regulating the STAT3 pathway and its role in promoti...

journal_title：Trends in pharmacological sciences

authors： Zhao C,Li H,Lin HJ,Yang S,Lin J,Liang G

更新日期：2016-01-01 00:00:00

abstract：:Recent advances in schizophrenia (SZ) research indicate that the telencephalic gamma-aminobutyric acid (GABA)ergic neurotransmission deficit associated with this psychiatric disorder probably is mediated by the hypermethylation of the glutamic acid decarboxylase 67 (GAD(67)), reelin and other GABAergic promoters. A ph...

journal_title：Trends in pharmacological sciences

authors： Guidotti A,Dong E,Kundakovic M,Satta R,Grayson DR,Costa E

更新日期：2009-02-01 00:00:00

abstract：:Chronic inflammation is the basis of various chronic illnesses including cancer and vascular diseases. However, much has yet to be learned how inflammation becomes chronic. Prostaglandins (PGs) are well established as mediators of acute inflammation, and recent studies in experimental animals have provided evidence th...

journal_title：Trends in pharmacological sciences

authors： Aoki T,Narumiya S

更新日期：2012-06-01 00:00:00

abstract：:It has been over 50years since Sir James Black developed the first beta adrenergic receptor (βAR) blocker to treat heart disease. At that time, the concept of cell surface receptors was relatively new and not widely accepted, and most of the tools currently used to characterize plasma membrane receptors had not been d...

journal_title：Trends in pharmacological sciences

authors： Kobilka BK

更新日期：2011-04-01 00:00:00

abstract：:Seven-transmembrane receptors are prototypic allosteric proteins with the ability to adopt numerous conformations, many of which interact with cellular partners to initiate cellular biochemical processes. Defining efficacy as the ability of ligands to stabilize some of these conformations (which, in turn, possess phys...

journal_title：Trends in pharmacological sciences

authors： Kenakin T

更新日期：2007-08-01 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：:Adenosine is an endogenous nucleoside that modulates many physiological processes. Its actions are mediated by interaction with specific cell membrane receptors. Four subtypes of adenosine receptor have been cloned: A1, A2A, A2B and A3. Significant advancement has been made in our understanding of the molecular pharma...

journal_title：Trends in pharmacological sciences

authors： Feoktistov I,Polosa R,Holgate ST,Biaggioni I

更新日期：1998-04-01 00:00:00

abstract：:Hypertension is prevalent and affects approximately 1 in every 4 adults in the Western world. Although many drugs are effective in treating hypertension, an individual's response to treatment is unpredictable. Pharmacogenetics holds the promise of becoming a tool to predict this response but obstacles and shortcomings...

journal_title：Trends in pharmacological sciences

authors： Kurland L,Lind L,Melhus H

更新日期：2005-09-01 00:00:00

abstract：:Nearly all molecules known to signal cells via G proteins have been assigned a cloned G-protein-coupled-receptor (GPCR) gene. This has been the result of a decade-long genetic search that has also identified some receptors for which ligands are unknown; these receptors are described as orphans (oGPCRs). More than 80 o...

journal_title：Trends in pharmacological sciences

authors： Marchese A,George SR,Kolakowski LF Jr,Lynch KR,O'Dowd BF

更新日期：1999-09-01 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：: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：: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：: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：:Biogenic amines and amino acids have been implicated in central cardiovascular homeostasis. Initially, drugs were injected into the brain and their effects on blood pressure were investigated. Other approaches allowed endogenous neurotransmitters released in the extracellular space of brain structures involved in card...

journal_title：Trends in pharmacological sciences

authors： Singewald N,Philippu A

更新日期：1996-10-01 00:00:00

abstract：:For almost 70 years, children have received stimulants for the treatment of attention deficit hyperactivity disorder [ADHD (initially called hyperkinetic syndrome)], with little understanding of the long-term effects of these drugs on brain development. The maturation and refinement of the brain during childhood and a...

journal_title：Trends in pharmacological sciences

authors： Andersen SL

更新日期：2005-05-01 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：:Leukotrienes have physiological roles in innate immune responses and pathological roles in inflammatory diseases, such as asthma, allergic rhinitis and atherosclerosis. Anti-leukotriene therapy has proven benefits in the treatment of respiratory disease, either through the inhibition of leukotriene synthesis or the se...

journal_title：Trends in pharmacological sciences

authors： Evans JF,Ferguson AD,Mosley RT,Hutchinson JH

更新日期：2008-02-01 00:00:00

abstract：:Chronic obstructive pulmonary disease (COPD) is a pulmonary inflammatory disease that is caused by cigarette smoke. The main characteristic of COPD is the continued inflammation caused by the sustained influx of macrophages and neutrophils into the lung. Recent studies have shed light on how these cells are attracted ...

journal_title：Trends in pharmacological sciences

authors： Smit JJ,Lukacs NW

更新日期：2006-11-01 00:00:00

abstract：:Recent studies in mice have identified single molecules that can delay multiple diseases of aging and extend lifespan. In theory, such molecules could prevent dozens of diseases simultaneously, potentially extending healthy years of life. In this review, we discuss recent advances, controversies, opportunities, and ch...

journal_title：Trends in pharmacological sciences

authors： Hubbard BP,Sinclair DA

更新日期：2014-03-01 00:00:00

abstract：:Fatty acid amide hydrolase (FAAH) is a hydrolytic enzyme that recognizes as substrates and inactivates the two most studied endocannabinoids, anandamide and 2-arachidonoylglycerol (2-AG). Following the observation that endocannabinoids produced by tissues during pathological conditions often have protective roles, FAA...

journal_title：Trends in pharmacological sciences

authors： Di Marzo V,Maccarrone M

更新日期：2008-05-01 00:00:00

abstract：:The genotoxicity of the most potent carcinogen in cigarette smoke [4-(methylnitrosamino)-1-(3-pyridyl)-1-butanone (NNK)] is dependent on the relationship between its activation by cytochrome P450 enzymes and its detoxification by carbonyl reduction to NNK alcohol (NNAL) followed by glucuronidation. Recently, '11 beta-...

journal_title：Trends in pharmacological sciences

authors： Maser E

更新日期：1997-08-01 00:00:00

abstract：:Hedgehog (Hh) signaling has emerged in recent years as an attractive target for anticancer therapy because its aberrant activation is implicated in several cancers. Major progress has been made in the development of SMOOTHENED (SMO) antagonists, although they have shown several limitations due to downstream SMO pathwa...

journal_title：Trends in pharmacological sciences

authors： Infante P,Alfonsi R,Botta B,Mori M,Di Marcotullio L

更新日期：2015-08-01 00:00:00

abstract：:Complete nucleotide sequences are now available for different species of the animal kingdom: Caenorhabditis elegans - a nematode, Drosophila - an insect, and humans - a mammal. Such information makes it possible to compare the set of nuclear receptors found in these organisms, and to discuss the possible reasons for t...

journal_title：Trends in pharmacological sciences

authors： Enmark E,Gustafsson JA

更新日期：2001-12-01 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：:Cytochromes P450 are a superfamily of haem-containing monooxygenases. In mammals, two general classes of P450s exist: six families involved in steroid and bile acid biosynthetic pathways of metabolism; four families containing numerous individual P450s, mainly responsible for metabolism of foreign compounds. Many of t...

journal_title：Trends in pharmacological sciences

authors： Gonzalez FJ

更新日期：1992-09-01 00:00:00

abstract：:Much regarding the engagement of the G(12) family of heterotrimeric G proteins (G(12) and G(13)) by agonist-activated receptors remains unclear. For example, the identity of receptors that couple unequivocally to G(12) and G(13) and how signals are allocated among these and other G proteins remain open questions. Part...

journal_title：Trends in pharmacological sciences

authors： Riobo NA,Manning DR

更新日期：2005-03-01 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：:Mechanisms of opioid tolerance have focused on adaptive modifications within cells containing opioid receptors, defined here as cellular allostasis, emphasizing regulation of the opioid receptor signalosome. We review additional regulatory and opponent processes involved in behavioral tolerance, and include mechanisti...

journal_title：Trends in pharmacological sciences

authors： Cahill CM,Walwyn W,Taylor AMW,Pradhan AAA,Evans CJ

更新日期：2016-11-01 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