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Article ; Online: Transcriptomic profiling reveals a pronociceptive role for angiotensin II in inflammatory bowel disease.

Higham, James P / Bhebhe, Charity N / Gupta, Rohit A / Tranter, Michael M / Barakat, Farah M / Dogra, Harween / Bab, Natalie / Wozniak, Eva / Barker, Katie H / Wilson, Catherine H / Mein, Charles A / Raine, Tim / Cox, James J / Wood, John N / Croft, Nicholas M / Wright, Paul D / Bulmer, David C

Pain

2024

Abstract: Abstract: Visceral pain is a leading cause of morbidity in inflammatory bowel disease (IBD), contributing significantly to reduced quality of life. Currently available analgesics often lack efficacy or have intolerable side effects, driving the need for ...

Abstract	Abstract: Visceral pain is a leading cause of morbidity in inflammatory bowel disease (IBD), contributing significantly to reduced quality of life. Currently available analgesics often lack efficacy or have intolerable side effects, driving the need for a more complete understanding of the mechanisms causing pain. Whole transcriptome gene expression analysis was performed by bulk RNA sequencing of colonic biopsies from patients with ulcerative colitis (UC) and Crohn's disease (CD) reporting abdominal pain and compared with noninflamed control biopsies. Potential pronociceptive mediators were identified based on gene upregulation in IBD biopsy tissue and cognate receptor expression in murine colonic sensory neurons. Pronociceptive activity of identified mediators was assessed in assays of sensory neuron and colonic afferent activity. RNA sequencing analysis highlighted a 7.6-fold increase in the expression of angiotensinogen transcripts, Agt , which encode the precursor to angiotensin II (Ang II), in samples from UC patients ( P = 3.2 × 10 -8 ). Consistent with the marked expression of the angiotensin AT 1 receptor in colonic sensory neurons, Ang II elicited an increase in intracellular Ca 2+ in capsaicin-sensitive, voltage-gated sodium channel subtype Na V 1.8-positive sensory neurons. Ang II also evoked action potential discharge in high-threshold colonic nociceptors. These effects were inhibited by the AT 1 receptor antagonist valsartan. Findings from our study identify AT 1 receptor-mediated colonic nociceptor activation as a novel pathway of visceral nociception in patients with UC. This work highlights the potential utility of angiotensin receptor blockers, such as valsartan, as treatments for pain in IBD.
Language	English
Publishing date	2024-01-29
Publishing country	United States
Document type	Journal Article
ZDB-ID	193153-2
ISSN	1872-6623 ; 0304-3959
ISSN (online)	1872-6623
ISSN	0304-3959
DOI	10.1097/j.pain.0000000000003159
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Article ; Online: Two-Pore Domain Potassium Channels as Drug Targets: Anesthesia and Beyond.

Mathie, Alistair / Veale, Emma L / Cunningham, Kevin P / Holden, Robyn G / Wright, Paul D

Annual review of pharmacology and toxicology

2020 Volume 61, Page(s) 401–420

Abstract: Two-pore domain potassium (K2P) channels stabilize the resting membrane potential of both excitable and nonexcitable cells and, as such, are important regulators of cell activity. There are many conditions where pharmacological regulation of K2P channel ... ...

Abstract	Two-pore domain potassium (K2P) channels stabilize the resting membrane potential of both excitable and nonexcitable cells and, as such, are important regulators of cell activity. There are many conditions where pharmacological regulation of K2P channel activity would be of therapeutic benefit, including, but not limited to, atrial fibrillation, respiratory depression, pulmonary hypertension, neuropathic pain, migraine, depression, and some forms of cancer. Up until now, few if any selective pharmacological regulators of K2P channels have been available. However, recent publications of solved structures with small-molecule activators and inhibitors bound to TREK-1, TREK-2, and TASK-1 K2P channels have given insight into the pharmacophore requirements for compound binding to these sites. Together with the increasing availability of a number of novel, active, small-molecule compounds from K2P channel screening programs, these advances have opened up the possibility of rational activator and inhibitor design to selectively target K2P channels.
MeSH term(s)	Anesthesia ; Humans ; Pharmaceutical Preparations ; Potassium Channels, Tandem Pore Domain
Chemical Substances	Pharmaceutical Preparations ; Potassium Channels, Tandem Pore Domain
Language	English
Publishing date	2020-07-17
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	196587-6
ISSN	1545-4304 ; 0362-1642
ISSN (online)	1545-4304
ISSN	0362-1642
DOI	10.1146/annurev-pharmtox-030920-111536
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Article ; Online: A "Target Class" Screen to Identify Activators of Two-Pore Domain Potassium (K2P) Channels.

McCoull, David / Ococks, Emma / Large, Jonathan M / Tickle, David C / Mathie, Alistair / Jerman, Jeffrey / Wright, Paul D

SLAS discovery : advancing life sciences R & D

2020 Volume 26, Issue 3, Page(s) 428–438

Abstract: Two-pore domain potassium (K2P) channels carry background (or leak) potassium current and play a key role in regulating resting membrane potential and cellular excitability. Accumulating evidence points to a role for K2Ps in human pathophysiologies, most ...

Abstract	Two-pore domain potassium (K2P) channels carry background (or leak) potassium current and play a key role in regulating resting membrane potential and cellular excitability. Accumulating evidence points to a role for K2Ps in human pathophysiologies, most notably in pain and migraine, making them attractive targets for therapeutic intervention. However, there remains a lack of selective pharmacological tools. The aim of this work was to apply a "target class" approach to investigate the K2P superfamily and identify novel activators across all the described subclasses of K2P channels. Target class drug discovery allows for the leveraging of accumulated knowledge and maximizing synergies across a family of targets and serves as an additional approach to standard target-based screening. A common assay platform using baculovirus (BacMam) to transiently express K2P channels in mammalian cells and a thallium flux assay to determine channel activity was developed, allowing the simultaneous screening of multiple targets. Importantly, this system, by allowing precise titration of channel function, allows optimization to facilitate the identification of activators. A representative set of channels (THIK-1, TWIK-1, TREK-2, TASK-3, and TASK-2) were screened against a library of Food and Drug Administration (FDA)-approved compounds and the LifeArc Index Set. Activators were then analyzed in concentration-response format across all channels to assess selectivity. Using the target class approach to investigate the K2P channels has enabled us to determine which of the K2Ps are amenable to small-molecule activation, de-risk multiple channels from a technical point of view, and identify a diverse range of previously undescribed pharmacology.
MeSH term(s)	Baculoviridae/genetics ; Baculoviridae/metabolism ; Cell Line, Tumor ; Cloning, Molecular ; Drug Discovery/methods ; Epithelial Cells/cytology ; Epithelial Cells/drug effects ; Epithelial Cells/metabolism ; Gene Expression ; Genetic Vectors/chemistry ; Genetic Vectors/metabolism ; High-Throughput Screening Assays ; Humans ; Ion Transport ; Potassium/metabolism ; Potassium Channels, Tandem Pore Domain/agonists ; Potassium Channels, Tandem Pore Domain/genetics ; Potassium Channels, Tandem Pore Domain/metabolism ; Recombinant Proteins/genetics ; Recombinant Proteins/metabolism ; Small Molecule Libraries/pharmacology ; Thallium/metabolism
Chemical Substances	KCNK1 protein, human ; KCNK10 protein, human ; KCNK13 protein, human ; KCNK5 protein, human ; KCNK9 protein, human ; Potassium Channels, Tandem Pore Domain ; Recombinant Proteins ; Small Molecule Libraries ; Thallium (AD84R52XLF) ; Potassium (RWP5GA015D)
Language	English
Publishing date	2020-12-29
Publishing country	United States
Document type	Journal Article
ZDB-ID	2885123-7
ISSN	2472-5560 ; 2472-5552
ISSN (online)	2472-5560
ISSN	2472-5552
DOI	10.1177/2472555220976126
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Article: Pranlukast is a novel small molecule activator of the two-pore domain potassium channel TREK2

Wright, Paul D / McCoull, David / Walsh, Yvonne / Large, Jonathan M / Hadrys, Barbara W / Gaurilcikaite, Egle / Byrom, Lewis / Veale, Emma L / Jerman, Jeff / Mathie, Alistair

Biochemical and biophysical research communications. 2019 Nov. 26, v. 520, no. 1

2019

Abstract: TREK2 (KCNK10, K2P10.1) is a two-pore domain potassium (K2P) channel and a potential target for the treatment of pain. Like the majority of the K2P superfamily, there is currently a lack of useful pharmacological tools to study TREK2. Here we present a ... ...

Abstract	TREK2 (KCNK10, K2P10.1) is a two-pore domain potassium (K2P) channel and a potential target for the treatment of pain. Like the majority of the K2P superfamily, there is currently a lack of useful pharmacological tools to study TREK2. Here we present a strategy for identifying novel TREK2 activators. A cell-based thallium flux assay was developed and used to screen a library of drug-like molecules, from which we identified the CysLT1 antagonist Pranlukast as a novel activator of TREK2. This compound was selective for TREK2 versus TREK1 and showed no activity at TRAAK. Pranlukast was also screened against other members of the K2P superfamily. Several close analogues of Pranlukast and other CysLT1 antagonists were also tested for their ability to activate K2P channels. Consistent with previous work, structure activity relationships showed that subtle structural changes to these analogues completely attenuated the activation of TREK2, whereas for TREK1, analogues moved from activators to inhibitors. Pranlukast’s activity was also confirmed using whole-cell patch clamp electrophysiology. Studies using mutant forms of TREK2 suggest Pranlukast does not bind in the K2P modulator pocket or the BL-1249 binding site. Pranlukast therefore represents a novel tool by which to study the mechanism of TREK2 activation.
Keywords	antagonists ; electrophysiology ; mutants ; pain ; potassium ; potassium channels ; research ; thallium
Language	English
Dates of publication	2019-1126
Size	p. 35-40.
Publishing place	Elsevier Inc.
Document type	Article
Note	NAL-AP-2-clean
ZDB-ID	205723-2
ISSN	0006-291X ; 0006-291X
ISSN (online)	0006-291X
ISSN	0006-291X
DOI	10.1016/j.bbrc.2019.09.093
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Article ; Online: Pranlukast is a novel small molecule activator of the two-pore domain potassium channel TREK2.

Wright, Paul D / McCoull, David / Walsh, Yvonne / Large, Jonathan M / Hadrys, Barbara W / Gaurilcikaite, Egle / Byrom, Lewis / Veale, Emma L / Jerman, Jeff / Mathie, Alistair

Biochemical and biophysical research communications

2019 Volume 520, Issue 1, Page(s) 35–40

Abstract: TREK2 (KCNK10, ... ...

Abstract	TREK2 (KCNK10, K
MeSH term(s)	Binding Sites ; Cell Line, Tumor ; Chromones/chemistry ; Chromones/pharmacology ; Crystallography, X-Ray ; Humans ; Pain Management ; Pain Measurement ; Patch-Clamp Techniques ; Potassium Channels, Tandem Pore Domain/chemistry ; Protein Binding ; Structure-Activity Relationship ; Tetrahydronaphthalenes/chemistry ; Tetrazoles/chemistry ; Thallium/chemistry
Chemical Substances	(5,6,7,8-tetrahydronaphthalen-1-yl)-(2-(1H-tetrazol-5-yl)phenyl)amine ; Chromones ; KCNK10 protein, human ; Potassium Channels, Tandem Pore Domain ; Tetrahydronaphthalenes ; Tetrazoles ; potassium channel protein TREK-1 ; Thallium (AD84R52XLF) ; pranlukast (TB8Z891092)
Language	English
Publishing date	2019-09-26
Publishing country	United States
Document type	Journal Article
ZDB-ID	205723-2
ISSN	1090-2104 ; 0006-291X ; 0006-291X
ISSN (online)	1090-2104 ; 0006-291X
ISSN	0006-291X
DOI	10.1016/j.bbrc.2019.09.093
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Zs.A 116: Show issues

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Article: Terbinafine is a novel and selective activator of the two-pore domain potassium channel TASK3

Wright, Paul D / Alistair Mathie / Catherine Kettleborough / David C. Tickle / David McCoull / Emma L. Veale / Emma Ococks / Gemma Gothard / Jeffrey Jerman / Jonathan M. Large

Biochemical and biophysical research communications. 2017,

2017

Abstract: Two-pore domain potassium channels (K2Ps) are characterized by their four transmembrane domain and two-pore topology. They carry background (or leak) potassium current in a variety of cell types. Despite a number of important roles there is currently a ... ...

Abstract	Two-pore domain potassium channels (K2Ps) are characterized by their four transmembrane domain and two-pore topology. They carry background (or leak) potassium current in a variety of cell types. Despite a number of important roles there is currently a lack of pharmacological tools with which to further probe K2P function. We have developed a cell-based thallium flux assay, using baculovirus delivered TASK3 (TWIK-related acid-sensitive K+ channel 3, KCNK9, K2P9.1) with the aim of identifying novel, selective TASK3 activators. After screening a library of 1000 compounds, including drug-like and FDA approved molecules, we identified Terbinafine as an activator of TASK3. In a thallium flux assay a pEC50 of 6.2 (±0.12) was observed. When Terbinafine was screened against TASK2, TREK2, THIK1, TWIK1 and TRESK no activation was observed in thallium flux assays. Several analogues of Terbinafine were also purchased and structure activity relationships examined. To confirm Terbinafine's activation of TASK3 whole cell patch clamp electrophysiology was carried out and clear potentiation observed in both the wild type channel and the pathophysiological, Birk-Barel syndrome associated, G236R TASK3 mutant. No activity at TASK1 was observed in electrophysiology studies. In conclusion, we have identified the first selective activator of the two-pore domain potassium channel TASK3.
Keywords	Baculoviridae ; electrophysiology ; mutants ; potassium ; potassium channels ; screening ; structure-activity relationships ; thallium ; topology
Language	English
Size	p. .
Publishing place	Elsevier Inc.
Document type	Article
Note	Pre-press version
ZDB-ID	205723-2
ISSN	0006-291X ; 0006-291X
ISSN (online)	0006-291X
ISSN	0006-291X
DOI	10.1016/j.bbrc.2017.09.002
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Article ; Online: Quantitative GPCR and ion channel transcriptomics in primary alveolar macrophages and macrophage surrogates

Groot-Kormelink Paul J / Fawcett Lindsay / Wright Paul D / Gosling Martin / Kent Toby C

BMC Immunology, Vol 13, Iss 1, p

2012 Volume 57

Abstract: Abstract Background Alveolar macrophages are one of the first lines of defence against invading pathogens and play a central role in modulating both the innate and acquired immune systems. By responding to endogenous stimuli within the lung, alveolar ... ...

Abstract	Abstract Background Alveolar macrophages are one of the first lines of defence against invading pathogens and play a central role in modulating both the innate and acquired immune systems. By responding to endogenous stimuli within the lung, alveolar macrophages contribute towards the regulation of the local inflammatory microenvironment, the initiation of wound healing and the pathogenesis of viral and bacterial infections. Despite the availability of protocols for isolating primary alveolar macrophages from the lung these cells remain recalcitrant to expansion in-vitro and therefore surrogate cell types, such as monocyte derived macrophages and phorbol ester-differentiated cell lines (e.g. U937, THP-1, HL60) are frequently used to model macrophage function. Methods The availability of high throughput gene expression technologies for accurate quantification of transcript levels enables the re-evaluation of these surrogate cell types for use as cellular models of the alveolar macrophage. Utilising high-throughput TaqMan arrays and focussing on dynamically regulated families of integral membrane proteins, we explore the similarities and differences in G-protein coupled receptor (GPCR) and ion channel expression in alveolar macrophages and their widely used surrogates. Results The complete non-sensory GPCR and ion channel transcriptome is described for primary alveolar macrophages and macrophage surrogates. The expression of numerous GPCRs and ion channels whose expression were hitherto not described in human alveolar macrophages are compared across primary macrophages and commonly used macrophage cell models. Several membrane proteins known to have critical roles in regulating macrophage function, including CXCR6, CCR8 and TRPV4, were found to be highly expressed in macrophages but not expressed in PMA-differentiated surrogates. Conclusions The data described in this report provides insight into the appropriate choice of cell models for investigating macrophage biology and highlights the importance of confirming experimental data in primary alveolar macrophages.
Keywords	COPD ; Microfluidics ; TaqMan ; Arrays ; High-throughput ; Immunologic diseases. Allergy ; RC581-607 ; Specialties of internal medicine ; RC581-951 ; Internal medicine ; RC31-1245 ; Medicine ; R ; DOAJ:Allergy and Immunology ; DOAJ:Medicine (General) ; DOAJ:Health Sciences
Subject code	610
Language	English
Publishing date	2012-10-01T00:00:00Z
Publisher	BioMed Central
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Quantitative GPCR and ion channel transcriptomics in primary alveolar macrophages and macrophage surrogates.

Groot-Kormelink, Paul J / Fawcett, Lindsay / Wright, Paul D / Gosling, Martin / Kent, Toby C

BMC immunology

2012 Volume 13, Page(s) 57

Abstract: Background: Alveolar macrophages are one of the first lines of defence against invading pathogens and play a central role in modulating both the innate and acquired immune systems. By responding to endogenous stimuli within the lung, alveolar ... ...

Abstract	Background: Alveolar macrophages are one of the first lines of defence against invading pathogens and play a central role in modulating both the innate and acquired immune systems. By responding to endogenous stimuli within the lung, alveolar macrophages contribute towards the regulation of the local inflammatory microenvironment, the initiation of wound healing and the pathogenesis of viral and bacterial infections. Despite the availability of protocols for isolating primary alveolar macrophages from the lung these cells remain recalcitrant to expansion in-vitro and therefore surrogate cell types, such as monocyte derived macrophages and phorbol ester-differentiated cell lines (e.g. U937, THP-1, HL60) are frequently used to model macrophage function. Methods: The availability of high throughput gene expression technologies for accurate quantification of transcript levels enables the re-evaluation of these surrogate cell types for use as cellular models of the alveolar macrophage. Utilising high-throughput TaqMan arrays and focussing on dynamically regulated families of integral membrane proteins, we explore the similarities and differences in G-protein coupled receptor (GPCR) and ion channel expression in alveolar macrophages and their widely used surrogates. Results: The complete non-sensory GPCR and ion channel transcriptome is described for primary alveolar macrophages and macrophage surrogates. The expression of numerous GPCRs and ion channels whose expression were hitherto not described in human alveolar macrophages are compared across primary macrophages and commonly used macrophage cell models. Several membrane proteins known to have critical roles in regulating macrophage function, including CXCR6, CCR8 and TRPV4, were found to be highly expressed in macrophages but not expressed in PMA-differentiated surrogates. Conclusions: The data described in this report provides insight into the appropriate choice of cell models for investigating macrophage biology and highlights the importance of confirming experimental data in primary alveolar macrophages.
MeSH term(s)	Cells, Cultured ; Cluster Analysis ; Gene Expression Profiling ; Gene Expression Regulation ; Humans ; Ion Channels/genetics ; Ion Channels/metabolism ; Macrophages, Alveolar/metabolism ; Oligonucleotide Array Sequence Analysis ; Receptors, G-Protein-Coupled/genetics ; Receptors, G-Protein-Coupled/metabolism ; Reproducibility of Results ; Tetradecanoylphorbol Acetate/pharmacology
Chemical Substances	Ion Channels ; Receptors, G-Protein-Coupled ; Tetradecanoylphorbol Acetate (NI40JAQ945)
Language	English
Publishing date	2012-10-26
Publishing country	England
Document type	Journal Article
ZDB-ID	2041500-X
ISSN	1471-2172 ; 1471-2172
ISSN (online)	1471-2172
ISSN	1471-2172
DOI	10.1186/1471-2172-13-57
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: Cloxyquin (5-chloroquinolin-8-ol) is an activator of the two-pore domain potassium channel TRESK

Wright, Paul D / Weir, Gregory / Cartland, Jamie / Tickle, David / Kettleborough, Catherine / Cader, M. Zameel / Jerman, Jeff

Biochemical and biophysical research communications. 2013 Nov. 15, v. 441, no. 2

2013

Abstract: TRESK is a two-pore domain potassium channel. Loss of function mutations have been linked to typical migraine with aura and due to TRESK’s expression pattern and role in neuronal excitability it represents a promising therapeutic target. We developed a ... ...

Abstract	TRESK is a two-pore domain potassium channel. Loss of function mutations have been linked to typical migraine with aura and due to TRESK’s expression pattern and role in neuronal excitability it represents a promising therapeutic target. We developed a cell based assay using baculovirus transduced U20S cells to screen for activators of TRESK. Using a thallium flux system to measure TRESK channel activity we identified Cloxyquin as a novel activator. Cloxyquin was shown to have an EC50 of 3.8μM in the thallium assay and displayed good selectivity against other potassium channels tested. Activity was confirmed using whole cell patch electrophysiology, with Cloxyquin causing a near two fold increase in outward current. The strategy presented here will be used to screen larger compound libraries with the aim of identifying novel chemical series which may be developed into new migraine prophylactics.
Keywords	electrophysiology ; migraine ; mutation ; potassium channels ; thallium
Language	English
Dates of publication	2013-1115
Size	p. 463-468.
Publishing place	Elsevier Inc.
Document type	Article
ZDB-ID	205723-2
ISSN	0006-291X ; 0006-291X
ISSN (online)	0006-291X
ISSN	0006-291X
DOI	10.1016/j.bbrc.2013.10.090
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Article ; Online: Terbinafine is a novel and selective activator of the two-pore domain potassium channel TASK3.

Wright, Paul D / Veale, Emma L / McCoull, David / Tickle, David C / Large, Jonathan M / Ococks, Emma / Gothard, Gemma / Kettleborough, Catherine / Mathie, Alistair / Jerman, Jeffrey

Biochemical and biophysical research communications

2017 Volume 493, Issue 1, Page(s) 444–450

Abstract	Two-pore domain potassium channels (K2Ps) are characterized by their four transmembrane domain and two-pore topology. They carry background (or leak) potassium current in a variety of cell types. Despite a number of important roles there is currently a lack of pharmacological tools with which to further probe K2P function. We have developed a cell-based thallium flux assay, using baculovirus delivered TASK3 (TWIK-related acid-sensitive K
MeSH term(s)	Drug Evaluation, Preclinical/methods ; Ion Channel Gating/drug effects ; Ion Channel Gating/physiology ; Naphthalenes/administration & dosage ; Naphthalenes/chemistry ; Porosity ; Potassium/chemistry ; Potassium/metabolism ; Potassium Channels, Tandem Pore Domain/agonists ; Potassium Channels, Tandem Pore Domain/metabolism ; Protein Domains ; Structure-Activity Relationship
Chemical Substances	KCNK9 protein, human ; Naphthalenes ; Potassium Channels, Tandem Pore Domain ; terbinafine (G7RIW8S0XP) ; Potassium (RWP5GA015D)
Language	English
Publishing date	2017-11-04
Publishing country	United States
Document type	Journal Article
ZDB-ID	205723-2
ISSN	1090-2104 ; 0006-291X ; 0006-291X
ISSN (online)	1090-2104 ; 0006-291X
ISSN	0006-291X
DOI	10.1016/j.bbrc.2017.09.002
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