Pharmacological Targeting of the Host-Pathogen Interaction: Alternatives to Classical Antibiotics to Combat Drug-Resistant Superbugs.

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：:14-3-3 Proteins enact a range of cellular functions through protein-protein interactions (PPIs) with client proteins. Kaplan and colleagues recently demonstrated that a semisynthetic compound was able to selectively stabilize or disrupt specific interactions, depending on the binding partner. This finding presents an ...

journal_title：Trends in pharmacological sciences

authors： Gannon M,Yacoubian TA

更新日期：2020-07-01 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：:All currently available general anesthetics produce potentially deadly side effects. Unfortunately, few approaches have been developed to design safer ones, despite important advances in anesthetic mechanisms research. Cayla and colleagues recently showed that computational methods can be used to identify anesthetic l...

journal_title：Trends in pharmacological sciences

authors： McGrath M,Pence A,Raines DE

更新日期：2019-11-01 00:00:00

abstract：:Traditional African medicine (TAM) is a shorthand reference to indigenous forms of healing that are practiced all over Africa. Although TAM is based on the accumulated experience of ancient Africans, its mode of transmission by word-of-mouth has hindered emergence of a generally accepted theory and hence of the system...

journal_title：Trends in pharmacological sciences

authors： Okpako DT

更新日期：1999-12-01 00:00:00

abstract：:Behavioural pharmacology is an interdisciplinary field at the intersection of several research areas that ultimately lead to the development of drugs for clinical use and build understanding of how brain functions enable cognition and behaviour. In this article, the development of behavioural pharmacology in the UK is...

journal_title：Trends in pharmacological sciences

authors： Robbins TW,Murphy ER

更新日期：2006-03-01 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：: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：:From the deep part of the main ligand-binding crevice, a minor, often shallower pocket extends between the extracellular ends of transmembrane domains (TM)-I, II, III and VII of 7TM receptors. This minor binding pocket is defined by a highly conserved kink in TM-II that is induced by a proline residue located in one o...

journal_title：Trends in pharmacological sciences

authors： Rosenkilde MM,Benned-Jensen T,Frimurer TM,Schwartz TW

更新日期：2010-12-01 00:00:00

abstract：:Current medicines for the clinical management of inflammatory diseases act by inhibiting specific enzymes or antagonising specific receptors or blocking their ligands. In the past decade, a new paradigm in our understanding of the inflammatory process has emerged with the appreciation of genetic, molecular, and cellul...

journal_title：Trends in pharmacological sciences

authors： Perretti M,Leroy X,Bland EJ,Montero-Melendez T

更新日期：2015-11-01 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：: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：:Recent studies have proposed a functional link between annexin 1 (ANXA1), an endogenous anti-inflammatory mediator, and receptors of the formyl-peptide family. In particular, exogenous and endogenous ANXA1 and its peptidomimetics interact with one member of this family, the formyl-peptide-receptor-like 1. Further anal...

journal_title：Trends in pharmacological sciences

authors： Perretti M

更新日期：2003-11-01 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：:Oxidative stress is a key pathologic factor in neurodegenerative diseases such as Alzheimer and Parkinson diseases (AD, PD). The failure of free-radical-scavenging antioxidants in clinical trials pinpoints an urgent need to identify and to block major sources of oxidative stress in neurodegenerative diseases. As a maj...

journal_title：Trends in pharmacological sciences

authors： Gao HM,Zhou H,Hong JS

更新日期：2012-06-01 00:00:00

abstract：:Within five years of discovering endothelin (ET-1) in 1988, the first report of an orally available ET receptor antagonist was published. Within twelve years, bosentan, the first ET receptor antagonist to gain marketing authorization, was made available for the treatment of pulmonary artery hypertension (PAH). Since t...

journal_title：Trends in pharmacological sciences

authors： Dhaun N,Pollock DM,Goddard J,Webb DJ

更新日期：2007-11-01 00:00:00

abstract：:Degradation of heme requires its conversion to biliverdin (BV) by heme oxygenase, followed by reduction of BV to the free-radical quencher bilirubin (BR) by biliverdin reductase (BVR). It is now recognized that human BVR (hBVR) is a dual-specificity kinase (Ser/Thr and Tyr) upstream activator of the insulin/insulin gr...

journal_title：Trends in pharmacological sciences

authors： Kapitulnik J,Maines MD

更新日期：2009-03-01 00:00:00

abstract：:B7x (B7 homolog x, also known as B7-H4, B7S1, and VTCN1) was discovered by ourselves and others in 2003 as the seventh member of the B7 family. It is an inhibitory immune checkpoint of great significance to human disease. Tissue-expressed B7x minimizes autoimmune and inflammatory responses. It is overexpressed in a br...

journal_title：Trends in pharmacological sciences

authors： John P,Wei Y,Liu W,Du M,Guan F,Zang X

更新日期：2019-11-01 00:00:00

abstract：:Humans are exposed to mixtures of chemicals, rather than to individual chemicals. From a public health point of view, it is most relevant to answer the question of whether or not the components in a mixture interact in a way that results in an increase in their overall effect compared with the sum of the effects of th...

journal_title：Trends in pharmacological sciences

authors： Groten JP,Feron VJ,Sühnel J

更新日期：2001-06-01 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：:The alpha-adrenoceptor was subdivided into three subtypes: alpha 2A-, alpha 2B- and alpha 2C-adrenoceptors almost ten years ago. Since then, the search has been on to discover and develop subtype-selective agonists and antagonists, but as yet no major breakthrough has been made. In the past year, several strains of ge...

journal_title：Trends in pharmacological sciences

authors： MacDonald E,Kobilka BK,Scheinin M

更新日期：1997-06-01 00:00:00

abstract：:The tachykinin family has recently been extended by the discovery of a third tachykinin gene encoding previously unknown mammalian tachykinins (hemokinin 1, endokinin A and endokinin B) that have a widespread peripheral distribution and a tachykinin NK(1) receptor selectivity. This and the identification of other tach...

journal_title：Trends in pharmacological sciences

authors： Patacchini R,Lecci A,Holzer P,Maggi CA

更新日期：2004-01-01 00:00:00

abstract：:Methylphenidate (Ritalin), a psychostimulant used in the treatment of Attention-Deficit Hyperactivity Disorder, has pharmacological effects similar to cocaine and amphetamine. Clinical use of methylphenidate, as well as diversion and abuse, have significantly increased during the past 10-15 years, heightening concerns...

journal_title：Trends in pharmacological sciences

authors： Yano M,Steiner H

更新日期：2007-11-01 00:00:00

abstract：:HIV-1 integrase (IN) executes the insertion of proviral DNA into the host cell genome, an essential step in the retroviral life cycle. This is a multi-step process that starts in the cytosol and culminates in the nucleus of the infected cell. It is becoming increasingly clear that IN interacts with a wide range of dif...

journal_title：Trends in pharmacological sciences

authors： Al-Mawsawi LQ,Neamati N

更新日期：2007-10-01 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：: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：: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：:Cytochrome P450 3A (CYP3A) enzymes metabolize a wide variety of xenobiotics including many drugs. Because CYP3A is localized in both the liver and intestine, it can make a major contribution to the presystemic elimination of substrate drugs after oral administration ('first-pass metabolism'). However, assessments of t...

journal_title：Trends in pharmacological sciences

authors： van Herwaarden AE,van Waterschoot RA,Schinkel AH

更新日期：2009-05-01 00:00:00

abstract：:Clinical experience with muscarinic agonists in the symptomatic treatment of Alzheimer's disease includes studies of the effects of pilocarpine, arecoline, bethanechol, oxotremorine and RS 86. Although the results are somewhat conflicting, there is evidence that a subgroup of patients may respond with an improvement o...

journal_title：Trends in pharmacological sciences

authors： Gray JA,Enz A,Spiegel R

更新日期：1989-12-01 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