Novel interactions between K+ channels and scorpion toxins.

Abstract:

:K(+) channels are macromolecules embedded in biological membranes, where they play a key role in cellular excitability and signal transduction pathways. Knowledge of their structure should help improve our understanding of their function and lead to the design of therapeutic compounds. Most pharmacological and structural characteristics of these channels have been elucidated by using high-affinity channel blockers isolated from scorpion venoms. Recent data on the three-dimensional structures of K(+) channels and novel scorpion toxins suggest a variety of novel interacting modes of these channels and toxins, which should help increase our understanding of the K(+) channel structure-function relationship.

journal_name

Trends Pharmacol Sci

authors

Rodríguez de la Vega RC,Merino E,Becerril B,Possani LD

doi

10.1016/S0165-6147(03)00080-4

subject

Has Abstract

pub_date

2003-05-01 00:00:00

pages

222-7

issue

5

eissn

0165-6147

issn

1873-3735

pii

S0165-6147(03)00080-4

journal_volume

24

pub_type

杂志文章,评审
  • Anxiety and alcohol abuse disorders: a common role for CREB and its target, the neuropeptide Y gene.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/S0165-6147(03)00226-8

    authors: Pandey SC

    更新日期:2003-09-01 00:00:00

  • Zn(2+): a novel ionic mediator of neural injury in brain disease.

    abstract::Zn(2+) is the second most prevalent trace element in the body and is present in particularly large concentrations in the mammalian brain. Although Zn(2+) is a cofactor for many enzymes in all tissues, a unique feature of brain Zn(2+) is its vesicular localization in presynaptic terminals, where its release is dependen...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/s0165-6147(00)01541-8

    authors: Weiss JH,Sensi SL,Koh JY

    更新日期:2000-10-01 00:00:00

  • Hormone and growth factor receptor-mediated regulation of phospholipase C activity.

    abstract::The broad importance of receptor-activated phosphoinositide hydrolysis in the physiological action of hormones, neurotransmitters and growth factors has sparked interest in the study of transmembrane signalling events responsible for activation of phospholipase C. As with receptors involved in regulation of adenylyl c...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/0165-6147(89)90008-4

    authors: Boyer JL,Hepler JR,Harden TK

    更新日期:1989-09-01 00:00:00

  • Targeting the melanocortin receptor system for anti-stroke therapy.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2010.11.010

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

    更新日期:2011-02-01 00:00:00

  • Exploring the potential of adjunct therapy in tuberculosis.

    abstract::A critical unmet need for treatment of drug-resistant tuberculosis (TB) is to find novel therapies that are efficacious, safe, and shorten the duration of treatment. Drug discovery approaches for TB primarily target essential genes of the pathogen Mycobacterium tuberculosis (Mtb) but novel strategies such as host-dire...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2015.05.005

    authors: Rayasam GV,Balganesh TS

    更新日期:2015-08-01 00:00:00

  • Exploring the pharmacological properties of insect nicotinic acetylcholine receptors.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2006.11.006

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

    更新日期:2007-01-01 00:00:00

  • Therapeutic Targeting of Siglecs using Antibody- and Glycan-Based Approaches.

    abstract::The sialic acid-binding immunoglobulin-like lectins (Siglecs) are a family of immunomodulatory receptors whose functions are regulated by their glycan ligands. Siglecs are attractive therapeutic targets because of their cell type-specific expression pattern, endocytic properties, high expression on certain lymphomas/l...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2015.06.008

    authors: Angata T,Nycholat CM,Macauley MS

    更新日期:2015-10-01 00:00:00

  • Tumour necrosis factor alpha and interleukin 1 signalling: do MAPKK kinases connect it all?

    abstract::The potent pro-inflammatory cytokines tumour necrosis factor alpha (TNF-alpha) and interleukin 1 (IL-1) are capable of triggering biologically similar effects through activation of the same set of transcription factors. Based on recent findings it is now becoming evident that certain members of the mitogen-activated p...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/s0165-6147(97)01097-3

    authors: Eder J

    更新日期:1997-09-01 00:00:00

  • Beyond Cannabis: Plants and the Endocannabinoid System.

    abstract::Plants have been the predominant source of medicines throughout the vast majority of human history, and remain so today outside of industrialized societies. One of the most versatile in terms of its phytochemistry is cannabis, whose investigation has led directly to the discovery of a unique and widespread homeostatic...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2016.04.005

    authors: Russo EB

    更新日期:2016-07-01 00:00:00

  • GPR119 as a fat sensor.

    abstract::The GPR119 receptor is expressed predominantly in pancreatic β cells and in enteroendocrine cells. It is a major target for the development of anti-diabetic drugs that through GPR119 activation may stimulate both insulin and GLP-1 release. GPR119 can be activated by oleoylethanolamide and several other endogenous lipi...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2012.03.014

    authors: Hansen HS,Rosenkilde MM,Holst JJ,Schwartz TW

    更新日期:2012-07-01 00:00:00

  • Resolution of airway disease: removal of inflammatory cells through apoptosis, egression or both?

    abstract::Pathogenic granulocytes (eosinophils and neutrophils) infiltrate airway tissues in asthma and chronic obstructive pulmonary disease. Granulocytes release tissue-toxic and inflammatory mediators, making their removal an important pharmacological goal. Removal is thought to be accomplished through apoptosis followed by ...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.tips.2006.07.006

    authors: Uller L,Persson CG,Erjefält JS

    更新日期:2006-09-01 00:00:00

  • Intracellular 5-HT 2C-receptor dephosphorylation: a new target for treating drug addiction.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2006.07.003

    authors: Müller CP,Carey RJ

    更新日期:2006-09-01 00:00:00

  • Novel Therapeutic Targets for Managing Dyslipidemia.

    abstract::Atherosclerotic cardiovascular disease (ASCVD) remains the leading cause of morbidity and mortality in developed nations. Therapeutic modulation of dyslipidemia by inhibiting 3'-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase is standard practice throughout the world. However, based on findings from Mendelian ...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2018.06.001

    authors: Sathiyakumar V,Kapoor K,Jones SR,Banach M,Martin SS,Toth PP

    更新日期:2018-08-01 00:00:00

  • Excitatory actions of adenosine on ventricular automaticity.

    abstract::Due to its negative chronotropic and inotropic effects, adenosine has to date been considered as a cardiodepressant agent. However, adenosine increases ventricular automaticity. This review by Jesus Hernández and Alexandre Ribeiro discusses the experimental and clinical evidence for the excitatory effects of adenosine...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/0165-6147(96)81589-6

    authors: Hernández J,Ribeiro JA

    更新日期:1996-04-01 00:00:00

  • Neuroprotective strategies for Parkinson's disease: conceptual limits of animal models and clinical trials.

    abstract::Parkinson's disease (PD) is a progressive neurodegenerative disorder. Although therapies that treat the symptoms of the disease have proven efficacy, strategies that slow or stop the neurodegenerative process are currently not available. Recently, the National Institute of Neurological Disorders and Stroke (NINDS) con...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2004.03.003

    authors: Meissner W,Hill MP,Tison F,Gross CE,Bezard E

    更新日期:2004-05-01 00:00:00

  • Off-target effects associated with long dsRNAs in Drosophila RNAi screens.

    abstract::Evidence of off-target effects (OTEs) associated with small interfering (si)RNAs (19-29bp) in mammalian cells has existed for several years. Two recent articles demonstrate that short sequences within long double-stranded (ds)RNAs frequently cause undesirable OTEs in cultured Drosophila cells. These results reveal the...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.tips.2007.02.009

    authors: Moffat J,Reiling JH,Sabatini DM

    更新日期:2007-04-01 00:00:00

  • A three-state receptor model of agonist action.

    abstract::The concept that receptors can exist in multiple conformational states is becoming a physical reality. A fundamental question is how many active states need to be proposed in order to account for pharmacological observations, in particular, the finding that the same receptor type can exhibit a different agonist pharma...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/s0165-6147(97)01105-x

    authors: Leff P,Scaramellini C,Law C,McKechnie K

    更新日期:1997-10-01 00:00:00

  • Are formyl peptide receptors novel targets for therapeutic intervention in ischaemia-reperfusion injury?

    abstract::Ischaemia-reperfusion (I/R) injury is a common feature of several diseases associated with high morbidity and mortality, such as stroke and myocardial infarction. The damaged tissue displays cardinal signs of inflammation and microvascular injury that, unless resolved, lead to long-term tissue damage with associated d...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2010.04.001

    authors: Gavins FN

    更新日期:2010-06-01 00:00:00

  • The minor binding pocket: a major player in 7TM receptor activation.

    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

    pub_type: 杂志文章

    doi:10.1016/j.tips.2010.08.006

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

    更新日期:2010-12-01 00:00:00

  • Lithium therapy and signal transduction.

    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

    pub_type: 杂志文章

    doi:10.1016/s0165-6147(99)01428-5

    authors: Williams RS,Harwood AJ

    更新日期:2000-02-01 00:00:00

  • Drug Repurposing for the Development of Novel Analgesics.

    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

    pub_type: 杂志文章

    doi:10.1016/j.tips.2015.11.006

    authors: Sisignano M,Parnham MJ,Geisslinger G

    更新日期:2016-03-01 00:00:00

  • Targeting tumor-associated carbonic anhydrase IX in cancer therapy.

    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

    pub_type: 杂志文章

    doi:10.1016/j.tips.2006.09.002

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

    更新日期:2006-11-01 00:00:00

  • Thiol-Based Drugs in Pulmonary Medicine: Much More than Mucolytics.

    abstract::Thiol-based drugs are considered as mucolytics because they decrease the viscosity and mostly decrease the elasticity of bronchial secretions by reducing disulfide bonds in proteins. However, they can also act as antioxidant drugs directly through free sulfhydryl groups that serve as a source of reducing equivalents, ...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章

    doi:10.1016/j.tips.2019.04.015

    authors: Cazzola M,Calzetta L,Page C,Rogliani P,Matera MG

    更新日期:2019-07-01 00:00:00

  • Comparing nuclear receptors in worms, flies and humans.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/s0165-6147(00)01859-9

    authors: Enmark E,Gustafsson JA

    更新日期:2001-12-01 00:00:00

  • Frizzleds as GPCRs - More Conventional Than We Thought!

    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

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2018.07.001

    authors: Schulte G,Wright SC

    更新日期:2018-09-01 00:00:00

  • Updating Neuroimmune Targets in Central Nervous System Dysfunction.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2019.04.013

    authors: Valente LA,Begg LR,Filiano AJ

    更新日期:2019-07-01 00:00:00

  • Techniques: Visualizing apoptosis using nuclear magnetic resonance.

    abstract::Apoptosis plays a key role in tumour biology, and the induction of apoptosis forms a cornerstone of most anticancer therapies. New developments in nuclear magnetic resonance spectroscopy (MRS) and magnetic resonance imaging (MRI) have taken these techniques far beyond their original roles as the workhorses of structur...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/S0165-6147(03)00032-4

    authors: Hakumäki JM,Brindle KM

    更新日期:2003-03-01 00:00:00

  • Regulation of free calmodulin levels by neuromodulin: neuron growth and regeneration.

    abstract::Neuromodulin is a neurospecific calmodulin binding protein that is implicated in neurite extension, axonal elongation and long-term potentiation. Yuechueng Liu and Daniel Storm propose that neuromodulin binds and concentrates calmodulin on growth cone membranes and that stimulation of protein kinase C releases high lo...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/0165-6147(90)90195-e

    authors: Liu YC,Storm DR

    更新日期:1990-03-01 00:00:00

  • Functional, molecular and pharmacological advances in 5-HT7 receptor research.

    abstract::The 5-HT7 receptor was among a group of 5-HT receptors that were discovered using targeted cloning strategies 12 years ago. This receptor is a seven-transmembrane-domain G-protein-coupled receptor that is positively linked to adenylyl cyclase. The distributions of 5-HT7 receptor mRNA, immunolabeling and radioligand bi...

    journal_title:Trends in pharmacological sciences

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2004.07.002

    authors: Hedlund PB,Sutcliffe JG

    更新日期:2004-09-01 00:00:00

  • Ca2+ channel beta-subunits: structural insights AID our understanding.

    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

    pub_type: 杂志文章,评审

    doi:10.1016/j.tips.2004.10.008

    authors: Richards MW,Butcher AJ,Dolphin AC

    更新日期:2004-12-01 00:00:00