Targeting the Type Three Secretion System in Pseudomonas aeruginosa.

abstract：:Carbonic anhydrase isoform IX (CA IX) is highly overexpressed in many types of cancer. Its expression, which is regulated by the HIF-1 transcription factor, is strongly induced by hypoxia and correlates with a poor response to classical chemo- and radiotherapies. CA IX contributes to acidification of the tumor environ...

journal_title：Trends in pharmacological sciences

authors： Thiry A,Dogné JM,Masereel B,Supuran CT

更新日期：2006-11-01 00:00:00

abstract：:cGMP inhibits hypertrophy, decreases fibrosis, and protects against cardiac ischemia-reperfusion (I/R) injury. Gene-targeting studies have not defined a clear role for its major downstream effector, cGMP-dependent protein kinase I (cGKI), in cardiac hypertrophy, but do implicate cGMP-cGKI signaling in fibrosis and I/R...

journal_title：Trends in pharmacological sciences

authors： Lukowski R,Krieg T,Rybalkin SD,Beavo J,Hofmann F

更新日期：2014-08-01 00:00:00

abstract：:The NLRP3 inflammasome is an intracellular multimeric protein complex which plays an important role in the pathogenesis of various human inflammatory diseases, such as diabetes, Alzheimer's disease and atherosclerosis. Recently, various G protein-coupled receptors (GPCRs) have been reported to be involved in the activ...

journal_title：Trends in pharmacological sciences

authors： Tang T,Gong T,Jiang W,Zhou R

更新日期：2018-09-01 00:00:00

abstract：:Cys loop, glutamate, and P2X receptors are ligand-gated ion channels (LGICs) with 5, 4, and 3 protomers, respectively. There is now growing atomic level understanding of their gating mechanisms. Although each family is unique in the architecture of the ligand-binding pocket, the pathway for motions to propagate from l...

journal_title：Trends in pharmacological sciences

authors： Du J,Dong H,Zhou HX

更新日期：2012-09-01 00:00:00

abstract：:An unlikely animal model is gaining popularity in neuropharmacological research: the 2-mm fruit fly (Drosophila melanogaster). Drugs have been administered to adult flies in their food and, more recently, via gasses and injections. Pharmacological tools have introduced behavioral alterations in Drosophila reminiscent ...

journal_title：Trends in pharmacological sciences

authors： Manev H,Dimitrijevic N,Dzitoyeva S

更新日期：2003-01-01 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：:New classes of drugs modifying Ca2+ channel activity have become available, this may enlarge the clinical utilities that have been associated with established Ca2+ channel antagonists such as the dihydropyridines (for example, nifedipine). Two such classes are reviewed by Michael Spedding, Barry Kenny and Pierre Chate...

journal_title：Trends in pharmacological sciences

authors： Spedding M,Kenny B,Chatelain P

更新日期：1995-04-01 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：: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：:Since conformational flexibility, which is required for the function of a protein, comes at the expense of structural stability, many proteins, including G-protein-coupled receptors (GPCRs), are under constant risk of misfolding and aggregation. In this regard GPR37 (also named PAEL-R and ETBR-LP-1) takes a prominent ...

journal_title：Trends in pharmacological sciences

authors： Leinartaité L,Svenningsson P

更新日期：2017-08-01 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：: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：:Neonatal Fc receptors (FcRns) recycle IgGs by preventing their lysosome degradation. As this process also enhances half-life of pathogenic auto-IgG, inspired from the mechanisms of intravenous immunoglobulin, several inhibitors of IgG-FcRn interface have been conceived for treating autoimmune diseases. Among them, the...

journal_title：Trends in pharmacological sciences

authors： Bayry J,Kaveri SV

更新日期：2018-11-01 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：:Classical targeted drug discovery is based on targeting druggable targets, typically kinases and receptors of which the function can be agonized or antagonized. This strategy meets difficulties in cases such as Huntington's disease (HD) and similar neurodegenerative disorders, where the pathological function of the pr...

journal_title：Trends in pharmacological sciences

authors： Yu S,Liang Y,Palacino J,Difiglia M,Lu B

更新日期：2014-02-01 00:00:00

abstract：:Our growing understanding of the immunopathogenesis of inflammatory bowel disease (IBD) has opened new avenues for developing targeted therapies. These advances in treatment options targeting different mechanisms of action offer new hope for personalized management. In this review we highlight emerging novel and easil...

journal_title：Trends in pharmacological sciences

authors： Coskun M,Vermeire S,Nielsen OH

更新日期：2017-02-01 00:00:00

abstract：:For many years the prevailing view of how steroid hormone receptors exert their effects on gene transcription has been that these intracellular receptor proteins, upon association with their specific cognate ligands, undergo a transformation to a state where they are capable of interacting with chromatin and regulatin...

journal_title：Trends in pharmacological sciences

authors： Power RF,Conneely OM,O'Malley BW

更新日期：1992-08-01 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：: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：: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：:Parkinson's disease (PD) is the second most common neurodegenerative disorder after Alzheimer's disease and is an important cause of chronic disability. Numerous important advances have been made in our understanding of the aetiopathogenesis, pathology and clinical phenomenology of this disease, and these have underpi...

journal_title：Trends in pharmacological sciences

authors： Schapira AH

更新日期：2009-01-01 00:00:00

abstract：:Bioluminescence resonance energy transfer has developed in recent years as a new technique to study protein-protein interactions. Protein partners of interest are tagged with either luciferase or green fluorescent protein (GFP). Non-radiative energy transfer between the excited luciferase and the GFP permits the study...

journal_title：Trends in pharmacological sciences

authors： Boute N,Jockers R,Issad T

更新日期：2002-08-01 00:00:00

abstract：:Cardiovascular disease remains the leading cause of death worldwide. Among many potential targets for pharmacological intervention, a promising strategy involves epoxyeicosatrienoic acid (EET) and soluble epoxide hydroxylase (sEH) inhibition. sEH is the enzyme that converts EET to its less potent metabolite; therefore...

journal_title：Trends in pharmacological sciences

authors： Romashko M,Schragenheim J,Abraham NG,McClung JA

更新日期：2016-11-01 00:00:00

abstract：:In drug development, major resources are invested into the development of cellular delivery systems to increase the effectiveness of a large array of potential therapeutics, such as proteins and oligonucleotides. These carriers comprise cell-penetrating peptides (CPPs), cationic lipids and cationic polymers. In recent...

journal_title：Trends in pharmacological sciences

authors： Verdurmen WP,Brock R

更新日期：2011-02-01 00:00:00

abstract：:Glucocorticosteroids are highly effective in controlling inflammation and the molecular mechanisms involved are now becoming clear. Activation of glucocorticoid receptors results in increased or decreased transcription of a number of genes involved in the inflammatory process. Of particular importance is the repressio...

journal_title：Trends in pharmacological sciences

authors： Barnes PJ,Adcock I

更新日期：1993-12-01 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：:Cancer initiates at one site (primary tumor) and, in most cases, spreads to other distant organs (metastasis). During the multistep process of metastasis, primary tumor cells acquire cellular and phenotypic plasticity to survive and thrive in different environments. Moreover, cancer cells also utilize and educate micr...

journal_title：Trends in pharmacological sciences

authors： Zhuang X,Zhang H,Hu G

更新日期：2019-06-01 00:00:00

abstract：:In 1964, the psychoactive ingredient of Cannabis sativa, Δ(9)-tetrahydrocannabinol (THC), was isolated. Nearly 30 years later the endogenous counterparts of THC, collectively termed endocannabinoids (eCBs), were discovered: N-arachidonoylethanolamine (anandamide) (AEA) in 1992 and 2-arachidonoylglycerol (2-AG) in 1995...

journal_title：Trends in pharmacological sciences

authors： Maccarrone M,Bab I,Bíró T,Cabral GA,Dey SK,Di Marzo V,Konje JC,Kunos G,Mechoulam R,Pacher P,Sharkey KA,Zimmer A

更新日期：2015-05-01 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：: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