Clinical Implications of Folate Transport in the Central Nervous System.

abstract：:The importance of the inhibitory neurotransmitter, GABA, within higher centres of the mammalian brain is unquestionable. However, its role within the spinal cord is of equal significance. There have been numerous studies over the past two decades that have established GABA as a neurotransmitter at both post- and presy...

journal_title：Trends in pharmacological sciences

authors： Malcangio M,Bowery NG

更新日期：1996-12-01 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：:The metabotropic glutamate (mGlu) receptors are a family of G-protein-coupled receptors (GPCRs) that regulate cell physiology throughout the nervous system. The potential of mGlu receptors as therapeutic targets has been bolstered by current research that has provided insight into the diverse modes of mGlu activation ...

journal_title：Trends in pharmacological sciences

authors： Stansley BJ,Conn PJ

更新日期：2019-04-01 00:00:00

abstract：:Clodronate is a first-generation bisphosphonate used worldwide for antiresorptive therapy for osteoporosis. Although clodronate is analgesic in nature, its mechanism and efficacy were unknown for some time. Recently, clodronate was identified as a selective and potent inhibitor for vesicular nucleotide transporter (VN...

journal_title：Trends in pharmacological sciences

authors： Moriyama Y,Nomura M

更新日期：2018-01-01 00:00:00

abstract：:Insect nicotinic acetylcholine (nACh) receptors are molecular targets of insecticides such as neonicotinoids that are used to control disease-carrying insects and agricultural pests. To date, several insect nACh receptor subunits have been identified, indicating different nACh receptor subtypes and pharmacological pro...

journal_title：Trends in pharmacological sciences

authors： Thany SH,Lenaers G,Raymond-Delpech V,Sattelle DB,Lapied B

更新日期：2007-01-01 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：:Loss of function of the phosphatase and tensin homolog (PTEN) tumour suppressor contributes to the development of many cancers. However, in contrast to classical models of tumour suppression, partial loss of PTEN function appears to be frequently observed in the clinic. In addition, studies of both humans and mice wit...

journal_title：Trends in pharmacological sciences

authors： Leslie NR,Foti M

更新日期：2011-03-01 00:00:00

abstract：:The 5-hydroxytryptamine (5-HT)(2C) receptor has received considerable attention as a target for treating drug addiction. 5-HT(2C)-receptor agonism, however, also induces side-effects. In this article, we review recent findings regarding the involvement of 5-HT(2C) receptors in behaviours related to drug addiction in a...

journal_title：Trends in pharmacological sciences

authors： Müller CP,Carey RJ

更新日期：2006-09-01 00:00:00

abstract：:Centrally acting drugs interfere with the function of central neurotransmitter systems. This often requires intact neuronal connections and is therefore best studied in vivo. Here, Gaetano Di Chiara describes the technique of brain dialysis, which permits direct in-vivo sampling of neurotransmitters and their metaboli...

journal_title：Trends in pharmacological sciences

authors： Di Chiara G

更新日期：1990-03-01 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：:Ubiquitination is a highly conserved post-translational modification that regulates protein trafficking, function, and turnover. Ubiquitin ligases (E3s) conjugate ubiquitin polypeptides on substrates, whereas deubiquitnases (DUBs) reverse ubiquitination. Engineering of chemical antagonists and inhibitors of ubiquitin ...

journal_title：Trends in pharmacological sciences

authors： Lill JR,Wertz IE

更新日期：2014-04-01 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：:The pursuit for drugs that inhibit cyclin-dependent kinases (CDKs) has been an intense area of research for more than 15 years. The first-generation inhibitors, Flavopiridol and CY-202, are in late-stage clinical trials, but so far have demonstrated only modest activity. Several second-generation inhibitors are now in...

journal_title：Trends in pharmacological sciences

authors： Malumbres M,Pevarello P,Barbacid M,Bischoff JR

更新日期：2008-01-01 00:00:00

abstract：:Snake venom neurotoxins and lymphocyte antigen 6 (Ly6) proteins, most of the latter being membrane tethered by a glycosylphosphatidylinositol (GPI) anchor, have a variety of biological activities, but their three-finger (3F) folding combines them in one Ly6/neurotoxin family. Subsets of two groups, represented by α-ne...

journal_title：Trends in pharmacological sciences

authors： Tsetlin VI

更新日期：2015-02-01 00:00:00

abstract：:Spinal and bulbar muscular atrophy is a hereditary motor neuron disease caused by trinucleotide repeat expansion in the androgen receptor gene. The disease mechanism probably involves a toxic gain of function in the mutant protein, because other mutations that cause a loss of androgen receptor function result in a dif...

journal_title：Trends in pharmacological sciences

authors： Ranganathan S,Fischbeck KH

更新日期：2010-11-01 00:00:00

abstract：:G protein-coupled receptors (GPCRs) comprise a large and diverse class of signal-transducing receptors that undergo dynamic and isoform-specific membrane trafficking. GPCRs thus have an inherent potential to initiate or regulate signaling reactions from multiple membrane locations. This review discusses emerging insig...

journal_title：Trends in pharmacological sciences

authors： Eichel K,von Zastrow M

更新日期：2018-02-01 00:00:00

abstract：:Three 'alpha 1-adrenoceptors' and three 'alpha 2-adrenoceptors' have now been cloned. How closely do these receptors match the native receptors that have been identified pharmacologically? What are the properties of these receptors, and how do they relate to other members of the cationic amine receptor family? Kevin L...

journal_title：Trends in pharmacological sciences

authors： Harrison JK,Pearson WR,Lynch KR

更新日期：1991-02-01 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：: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：: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：:Nuclear receptors represent a large class of ligand-activated transcriptional regulators; about 70 members of this protein family have been cloned from mammalian or insect species. Thus, it came as a great surprise when the recent completion of the Caenorhabditis elegans genome revealed at least 228 genes for nuclear ...

journal_title：Trends in pharmacological sciences

authors： Enmark E,Gustafsson JA

更新日期：2000-03-01 00:00:00

abstract：:Antipsychotic drugs (APDs), and the 'atypical' APDs in particular, are commonly associated with metabolic side effects in humans. These include glucose dysregulation, insulin resistance, hyperlipidemia, weight gain and hypertension, which put patients at increased risk of cardiometabolic disorders. The underlying biol...

journal_title：Trends in pharmacological sciences

authors： Boyda HN,Tse L,Procyshyn RM,Honer WG,Barr AM

更新日期：2010-10-01 00:00:00

abstract：:Many diseases result from defects in cell signaling. Achieving an in-depth understanding of the complex mechanisms by which cells transduce extracellular signals into cellular responses in both normal and diseased systems is a crucial step in the discovery of more effective drugs to treat human diseases. Traditional a...

journal_title：Trends in pharmacological sciences

authors： Koller E,Gaarde WA,Monia BP

更新日期：2000-04-01 00:00:00

abstract：:Central nervous system (CNS) drug development has been plagued by a failure to translate effective therapies from the lab to the clinic. There are many potential reasons for this, including poor understanding of brain pharmacokinetic (PK) and pharmacodynamic (PD) factors, preclinical study flaws, clinical trial design...

journal_title：Trends in pharmacological sciences

authors： Dragunow M

更新日期：2020-11-01 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：:Disorders of the central nervous system (CNS) have many etiologies compounded by limited options for treatment. The lack of successful treatments for these disorders stems from the difficulty of gaining effective access to the CNS through the blood-brain barrier, and the irreplaceable nature of neurons. Here, we revie...

journal_title：Trends in pharmacological sciences

authors： Valente LA,Begg LR,Filiano AJ

更新日期：2019-07-01 00:00:00

abstract：:Lithium is the simplest therapeutic agent available for the treatment of depression and has been used for over 100 years, yet no definitive mechanism for its effect has been established. Among the proposed mechanisms, two lithium-sensitive signal transduction pathways are active in the brain; these are mediated by gly...

journal_title：Trends in pharmacological sciences

authors： Williams RS,Harwood AJ

更新日期：2000-02-01 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：:Drug development consumes huge amounts of time and money and the search for novel analgesics, which are urgently required, is particularly difficult, having resulted in many setbacks in the past. Drug repurposing - the identification of new uses for existing drugs - is an alternative approach, which bypasses most of t...

journal_title：Trends in pharmacological sciences

authors： Sisignano M,Parnham MJ,Geisslinger G

更新日期：2016-03-01 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