Chemokines, chemokine receptors and small-molecule antagonists: recent developments.

abstract：:This year marks the 90th anniversary of the publication of Hans Horst Meyer's classic paper in which he proposed that the ability of a substance to produce narcosis or anesthesia is governed by its partition coefficient. In this article, Robert Lipnick describes the experiments carried out by Meyer and his colleagues ...

journal_title：Trends in pharmacological sciences

authors： Lipnick RL

更新日期：1989-07-01 00:00:00

abstract：:The melanocortin receptors are a subfamily of G-protein-coupled, rhodopsin-like receptors that are rapidly being acknowledged as an extremely promising target for pharmacological intervention in a variety of different inflammatory pathologies, including stroke. Stroke continues to be a leading cause of death worldwide...

journal_title：Trends in pharmacological sciences

authors： Holloway PM,Smith HK,Renshaw D,Flower RJ,Getting SJ,Gavins FN

更新日期：2011-02-01 00:00:00

abstract：:Elucidating plant-specialized biosynthetic pathways has always constituted a laborious task, notably for natural products with high pharmaceutical values. Here, we discuss emerging omics-based strategies that facilitate the identification of genes from these complex metabolic pathways, paving the way to engineered sup...

journal_title：Trends in pharmacological sciences

authors： Dugé de Bernonville T,Papon N,Clastre M,O'Connor SE,Courdavault V

更新日期：2020-03-01 00:00:00

abstract：:The disruption of large protein-protein (PP) interfaces remains a challenge in targeted therapy. Designing drugs that compete with binding partners is daunting, especially when the structure of the protein complex is unknown. To address the problem we propose a deep protein databank (PDB) learning platform to discover...

journal_title：Trends in pharmacological sciences

authors： Fernández A

更新日期：2019-08-01 00:00:00

abstract：:The discovery of neuropeptides as signaling molecules with paracrine or hormonal regulatory functions has led to trailblazing advances in physiology and fostered the characterization of numerous neuropeptide-binding G protein-coupled receptors (GPCRs) as potential drug targets. The impact on human health has been trem...

journal_title：Trends in pharmacological sciences

authors： Romanova EV,Sweedler JV

更新日期：2015-09-01 00:00:00

abstract：:Steroid hormones are recognized as producing their major long-term effects on cell structure and function via intracellular receptors acting on the expression of genes. There is now increasing evidence that steroids also affect the surface of cells and alter ion permeability, as well as release of neurohormones and ne...

journal_title：Trends in pharmacological sciences

authors： McEwen BS

更新日期：1991-04-01 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：:It has been hypothesized that anxiety disorders play an important role in the initiation and maintenance of alcohol drinking behaviors. However, the molecular mechanisms for the association between anxiety and alcohol abuse are not well understood. Structures of the extended amygdala, particularly the central nucleus ...

journal_title：Trends in pharmacological sciences

authors： Pandey SC

更新日期：2003-09-01 00:00:00

abstract：:NMDA and non-NMDA (AMPA/kainate) antagonists have potential in the treatment of a diverse group of neurological disorders associated with excessive activation of excitatory amino acid receptors. Here Michael Rogawski reviews recent progress in the development of therapeutically useful NMDA receptor channel blockers an...

journal_title：Trends in pharmacological sciences

authors： Rogawski MA

更新日期：1993-09-01 00:00:00

abstract：:For more than 30 years, WNT/β-catenin and planar cell polarity signaling has formed the basis for what we understand to be the primary output of the interaction between WNTs and their cognate receptors known as Frizzleds (FZDs). In the shadow of these pathways, evidence for the involvement of heterotrimeric G proteins...

journal_title：Trends in pharmacological sciences

authors： Schulte G,Wright SC

更新日期：2018-09-01 00:00:00

abstract：:Tissue factor (TF) is the cellular receptor and cofactor for blood coagulation factor VII (FVII). Exposure of flowing blood to cells that express TF leads to the initiation of blood coagulation. A recent study of mice expressing low levels of TF has demonstrated the importance of TF and FVII in maintaining adequate ha...

journal_title：Trends in pharmacological sciences

authors： McVey JH

更新日期：2003-06-01 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：:Successful biologics must satisfy multiple properties including activity and particular physicochemical features that are globally defined as developability. These multiple properties must be simultaneously optimized in a very broad design space of protein sequences and buffer compositions. In this context, artificial...

journal_title：Trends in pharmacological sciences

authors： Narayanan H,Dingfelder F,Butté A,Lorenzen N,Sokolov M,Arosio P

更新日期：2021-01-23 00:00:00

abstract：:Recruitment of leukocytes either during development or to the site of injury is crucial. The molecular regulation of cell trafficking is complex but well orchestrated by the temporal and spatial expression of a multitude of chemokines (chemoattractant cytokines) and chemokine receptors. The chemokines, classified prim...

journal_title：Trends in pharmacological sciences

authors： Devalaraja MN,Richmond A

更新日期：1999-04-01 00:00:00

abstract：:Ca2+ channels in the plasma membrane of T cells vitally influence Ca2+-dependent signals that lead ultimately to cytokine secretion, cellular proliferation and apoptosis. Conventional models depict the Ca2+ inrush across the T-cell membrane following T-cell receptor engagement as being due to Ca2+-release-activated Ca...

journal_title：Trends in pharmacological sciences

authors： Kotturi MF,Hunt SV,Jefferies WA

更新日期：2006-07-01 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：: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：: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：: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：:The efficacy of the powerful CRISPR-Cas9 genome-editing platform depends on DNA repair activities in the cells being targeted. Two new papers show that the low efficiency of targeting in some primary human cell lines is the result of p53-dependent cell arrest in response to the Cas9-induced break. This limitation must...

journal_title：Trends in pharmacological sciences

authors： Carroll D

更新日期：2018-09-01 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：: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：:G-protein-coupled receptors (GPCRs) are dynamically regulated by various mechanisms that tune their response to external stimuli. Modulation of their plasma membrane density, via trafficking between subcellular compartments, constitutes an important process in this context. Substantial information has been accumulated...

journal_title：Trends in pharmacological sciences

authors： Achour L,Labbé-Jullié C,Scott MG,Marullo S

更新日期：2008-10-01 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

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：:Changes in the structure and function of the small airways (<2mm diameter) are now recognized to play a major role in airflow limitation in both chronic obstructive pulmonary disease (COPD) and severe asthma. Increased thickness of the small airway wall causes lumenal narrowing, which can be further occluded by mucus ...

journal_title：Trends in pharmacological sciences

authors： Sturton G,Persson C,Barnes PJ

更新日期：2008-07-01 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：: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：:Hormesis is a generalizable dose-response relationship characterized by low-dose stimulation and high-dose inhibition. Despite debate over this biphasic dose-response curve, hormesis is challenging central beliefs in the evaluation of chemicals or drugs and has influenced biological model selection, concentration rang...

journal_title：Trends in pharmacological sciences

authors： Sun H,Calabrese EJ,Lin Z,Lian B,Zhang X

更新日期：2020-08-01 00:00:00

abstract：:Gastroesophageal reflux disease (GERD) is very common and advances in drug development over recent years have markedly improved GERD management. A wide range of medications are currently used in GERD treatment, including antacids, Gaviscon, sucralfate, histamine-2 receptor antagonists and prokinetics. However, proton ...

journal_title：Trends in pharmacological sciences

authors： Hershcovici T,Fass R

更新日期：2011-04-01 00:00:00