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Article: Zika M-A Potential Viroporin: Mutational Study and Drug Repurposing.

Tomar, Prabhat Pratap Singh / Krugliak, Miriam / Singh, Anamika / Arkin, Isaiah T

2022 Volume 10, Issue 3

Abstract: Genus Flavivirus contains several important human pathogens. Among these, the Zika virus is an emerging etiological agent that merits concern. One of its structural proteins, prM, plays an essential role in viral maturation and assembly, making it an ... ...

Abstract	Genus Flavivirus contains several important human pathogens. Among these, the Zika virus is an emerging etiological agent that merits concern. One of its structural proteins, prM, plays an essential role in viral maturation and assembly, making it an attractive drug and vaccine development target. Herein, we have characterized ZikV-M as a potential viroporin candidate using three different bacteria-based assays. These assays were subsequently employed to screen a library of repurposed drugs from which ten compounds were identified as ZikV-M blockers. Mutational analyses of conserved amino acids in the transmembrane domain of other flaviviruses, including West Nile and Dengue virus, were performed to study their role in ion channel activity. In conclusion, our data show that ZikV-M is a potential ion channel that can be used as a drug target for high throughput screening and drug repurposing.
Language	English
Publishing date	2022-03-10
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2720867-9
ISSN	2227-9059
ISSN	2227-9059
DOI	10.3390/biomedicines10030641
Database	MEDical Literature Analysis and Retrieval System OnLINE

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Article: Identification of SARS-CoV-2 E Channel Blockers from a Repurposed Drug Library.

Tomar, Prabhat Pratap Singh / Krugliak, Miriam / Arkin, Isaiah T

Pharmaceuticals (Basel, Switzerland)

2021 Volume 14, Issue 7

Abstract: SARS-CoV-2, the etiological agent of the COVID-19 pandemic, is a member of the Coronaviridae family. It is an enveloped virus with ion channels in its membrane, the most characterized of which is the E protein. Therefore, in an attempt to identify ... ...

Abstract	SARS-CoV-2, the etiological agent of the COVID-19 pandemic, is a member of the Coronaviridae family. It is an enveloped virus with ion channels in its membrane, the most characterized of which is the E protein. Therefore, in an attempt to identify blockers of the E channel, we screened a library of 2839 approved-for-human-use drugs. Our approach yielded eight compounds that exhibited appreciable activity in three bacteria-based channel assays. Considering the fact that the E channel is the most conserved of all SARS-CoV-2 proteins, any inhibitor of its activity may provide an option to curb the viral spread. In addition, inhibitors can also enhance our ability to understand the exact role played by the E protein during the infectivity cycle. Finally, detailed electrophysiological analyses, alongside in vitro and in vivo studies will be needed to establish the exact potential of each of the blockers identified in our study.
Language	English
Publishing date	2021-06-23
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2193542-7
ISSN	1424-8247
ISSN	1424-8247
DOI	10.3390/ph14070604
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Article ; Online: Blockers of the SARS-CoV-2 3a Channel Identified by Targeted Drug Repurposing.

Tomar, Prabhat Pratap Singh / Krugliak, Miriam / Arkin, Isaiah T

Viruses

2021 Volume 13, Issue 3

Abstract: The etiological agent of the COVID-19 pandemic is SARS-CoV-2. As a member of the Coronaviridae, the enveloped pathogen has several membrane proteins, of which two, E and 3a, were suggested to function as ion channels. In an effort to increase our ... ...

Abstract	The etiological agent of the COVID-19 pandemic is SARS-CoV-2. As a member of the Coronaviridae, the enveloped pathogen has several membrane proteins, of which two, E and 3a, were suggested to function as ion channels. In an effort to increase our treatment options, alongside providing new research tools, we have sought to inhibit the 3a channel by targeted drug repurposing. To that end, using three bacteria-based assays, we screened a library of 2839 approved-for-human-use drugs and identified the following potential channel-blockers: Capreomycin, Pentamidine, Spectinomycin, Kasugamycin, Plerixafor, Flumatinib, Litronesib, Darapladib, Floxuridine and Fludarabine. The stage is now set for examining the activity of these compounds in detailed electrophysiological studies and their impact on the whole virus with appropriate biosafety measures.
MeSH term(s)	Antiviral Agents/pharmacology ; COVID-19/drug therapy ; COVID-19/virology ; Drug Evaluation, Preclinical ; Drug Repositioning ; Humans ; SARS-CoV-2/drug effects ; SARS-CoV-2/genetics ; SARS-CoV-2/metabolism ; Viral Envelope Proteins/antagonists & inhibitors ; Viral Envelope Proteins/genetics ; Viral Envelope Proteins/metabolism ; Viroporin Proteins/antagonists & inhibitors ; Viroporin Proteins/genetics ; Viroporin Proteins/metabolism
Chemical Substances	3a protein, SARS-CoV ; Antiviral Agents ; Viral Envelope Proteins ; Viroporin Proteins
Language	English
Publishing date	2021-03-23
Publishing country	Switzerland
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2516098-9
ISSN	1999-4915 ; 1999-4915
ISSN (online)	1999-4915
ISSN	1999-4915
DOI	10.3390/v13030532
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Article ; Online: Zika M—A Potential Viroporin

Prabhat Pratap Singh Tomar / Miriam Krugliak / Anamika Singh / Isaiah T. Arkin

Biomedicines, Vol 10, Iss 641, p

Mutational Study and Drug Repurposing

2022 Volume 641

Abstract	Genus Flavivirus contains several important human pathogens. Among these, the Zika virus is an emerging etiological agent that merits concern. One of its structural proteins, prM, plays an essential role in viral maturation and assembly, making it an attractive drug and vaccine development target. Herein, we have characterized ZikV-M as a potential viroporin candidate using three different bacteria-based assays. These assays were subsequently employed to screen a library of repurposed drugs from which ten compounds were identified as ZikV-M blockers. Mutational analyses of conserved amino acids in the transmembrane domain of other flaviviruses, including West Nile and Dengue virus, were performed to study their role in ion channel activity. In conclusion, our data show that ZikV-M is a potential ion channel that can be used as a drug target for high throughput screening and drug repurposing.
Keywords	flavivirus ; Zika virus ; West Nile virus ; Dengue virus ; membrane glycoprotein ; ion channel proteins ; Biology (General) ; QH301-705.5
Language	English
Publishing date	2022-03-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Urinary metabolite signatures reflect the altered host metabolism in severe obstructive sleep apnea.

Mohit / Tomar, Manendra Singh / Araniti, Fabrizio / Sahai, Prabhat Kumar / Singh, Bhanu Pratap / Shrivastava, Ashutosh / Chand, Pooran

Journal of chromatography. B, Analytical technologies in the biomedical and life sciences

2023 Volume 1231, Page(s) 123938

Abstract: Obstructive sleep apnea (OSA) is a common sleep-related breathing disorder. The onset and progression of OSA are often linked with severe cardiovascular and metabolic comorbidities. At the same time, given the increasing prevalence of OSA, novel methods ... ...

Abstract	Obstructive sleep apnea (OSA) is a common sleep-related breathing disorder. The onset and progression of OSA are often linked with severe cardiovascular and metabolic comorbidities. At the same time, given the increasing prevalence of OSA, novel methods to screen OSA and its follow-up are needed. Untargeted metabolic profiling of OSA patients and healthy controls was planned to capture a snapshot of urinary metabolites and potential biomarkers using the gas chromatography-mass spectrometry (GC-MS) method.Polysomnography (PSG) confirmed severe OSA patients with AHI index ≥ 30 were considered for urine sample collection. The sample size was constituted of OSA (n = 36) and healthy controls (n = 36). Metabolite extraction and derivatization were performed and metabolomic analysis was performed by using GC-MS.The obtained data set was statistically analyzed using univariate and multivariate analysis. The Orthogonal partial least-squares discriminant analysis (OPLS-DA) was performed to screen differential metabolites between OSA patients and healthy controls.The metabolomic analysis revealed a total of 142 significantly altered metabolites of interest.Biomarker analysis allows for the creation of a list of putative urinary biomarkers including GABA, malic acid, glutamic acid, epichoric acid etc., with an accuracy of 99.8 % to 100 % for OSA screening. Subsequently, pathway analysis revealed that related biochemical pathways like the tricarboxylic acid cycle (TCA), glutamate/glutamine, amino acid and fatty acid metabolism, that are significantly interlinked with these metabolic biomarkers can play a crucial role in the pathogenesis of OSA. This study paves the way to undertake mass screening in a larger population to identify specific and reliable biomarkers.
MeSH term(s)	Humans ; Biomarkers/urine ; Sleep Apnea, Obstructive/diagnosis ; Sleep Apnea, Obstructive/epidemiology ; Metabolomics/methods ; Gas Chromatography-Mass Spectrometry/methods ; Comorbidity
Chemical Substances	Biomarkers
Language	English
Publishing date	2023-11-18
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	1180823-8
ISSN	1873-376X ; 0378-4347 ; 1570-0232 ; 1387-2273
ISSN (online)	1873-376X
ISSN	0378-4347 ; 1570-0232 ; 1387-2273
DOI	10.1016/j.jchromb.2023.123938
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Article ; Online: SARS-CoV-2 E protein is a potential ion channel that can be inhibited by Gliclazide and Memantine.

Singh Tomar, Prabhat Pratap / Arkin, Isaiah T

Biochemical and biophysical research communications

2020 Volume 530, Issue 1, Page(s) 10–14

Abstract: COVID-19 is one of the most impactful pandemics in recorded history. As such, the identification of inhibitory drugs against its etiological agent, SARS-CoV-2, is of utmost importance, and in particular, repurposing may provide the fastest route to curb ... ...

Abstract	COVID-19 is one of the most impactful pandemics in recorded history. As such, the identification of inhibitory drugs against its etiological agent, SARS-CoV-2, is of utmost importance, and in particular, repurposing may provide the fastest route to curb the disease. As the first step in this route, we sought to identify an attractive and viable target in the virus for pharmaceutical inhibition. Using three bacteria-based assays that were tested on known viroporins, we demonstrate that one of its essential components, the E protein, is a potential ion channel and, therefore, is an excellent drug target. Channel activity was demonstrated for E proteins in other coronaviruses, providing further emphasis on the importance of this functionally to the virus' pathogenicity. The results of a screening effort involving a repurposing drug library of ion channel blockers yielded two compounds that inhibit the E protein: Gliclazide and Memantine. In conclusion, as a route to curb viral virulence and abate COVID-19, we point to the E protein of SARS-CoV-2 as an attractive drug target and identify off-label compounds that inhibit it.
MeSH term(s)	Antiviral Agents/pharmacology ; Betacoronavirus/drug effects ; Betacoronavirus/metabolism ; COVID-19 ; Coronavirus Envelope Proteins ; Coronavirus Infections/drug therapy ; Coronavirus Infections/virology ; Drug Discovery ; Drug Repositioning ; Gliclazide/pharmacology ; Humans ; Ion Channels/antagonists & inhibitors ; Ion Channels/metabolism ; Memantine/pharmacology ; Pandemics ; Pneumonia, Viral/drug therapy ; Pneumonia, Viral/virology ; SARS-CoV-2 ; Viral Envelope Proteins/antagonists & inhibitors ; Viral Envelope Proteins/metabolism
Chemical Substances	Antiviral Agents ; Coronavirus Envelope Proteins ; Ion Channels ; Viral Envelope Proteins ; envelope protein, SARS-CoV-2 ; Gliclazide (G4PX8C4HKV) ; Memantine (W8O17SJF3T)
Keywords	covid19
Language	English
Publishing date	2020-06-20
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.2020.05.206
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Zs.A 116: Show issues

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Article ; Online: Identification of SARS-CoV-2 E Channel Blockers from a Repurposed Drug Library

Prabhat Pratap Singh Tomar / Miriam Krugliak / Isaiah T. Arkin

Pharmaceuticals, Vol 14, Iss 604, p

2021 Volume 604

Abstract	SARS-CoV-2, the etiological agent of the COVID-19 pandemic, is a member of the Coronaviridae family. It is an enveloped virus with ion channels in its membrane, the most characterized of which is the E protein. Therefore, in an attempt to identify blockers of the E channel, we screened a library of 2839 approved-for-human-use drugs. Our approach yielded eight compounds that exhibited appreciable activity in three bacteria-based channel assays. Considering the fact that the E channel is the most conserved of all SARS-CoV-2 proteins, any inhibitor of its activity may provide an option to curb the viral spread. In addition, inhibitors can also enhance our ability to understand the exact role played by the E protein during the infectivity cycle. Finally, detailed electrophysiological analyses, alongside in vitro and in vivo studies will be needed to establish the exact potential of each of the blockers identified in our study.
Keywords	COVID-19 ; viral channels ; bacterial assays ; channel blockers ; antiviral drugs ; Medicine ; R ; Pharmacy and materia medica ; RS1-441
Subject code	572
Language	English
Publishing date	2021-06-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article: SARS-CoV-2 E protein is a potential ion channel that can be inhibited by Gliclazide and Memantine

Singh Tomar, Prabhat Pratap / Arkin, Isaiah T

Biochemical and biophysical research communications. 2020 Sept. 10, v. 530, no. 1

2020

Abstract	COVID-19 is one of the most impactful pandemics in recorded history. As such, the identification of inhibitory drugs against its etiological agent, SARS-CoV-2, is of utmost importance, and in particular, repurposing may provide the fastest route to curb the disease. As the first step in this route, we sought to identify an attractive and viable target in the virus for pharmaceutical inhibition. Using three bacteria-based assays that were tested on known viroporins, we demonstrate that one of its essential components, the E protein, is a potential ion channel and, therefore, is an excellent drug target. Channel activity was demonstrated for E proteins in other coronaviruses, providing further emphasis on the importance of this functionally to the virus’ pathogenicity. The results of a screening effort involving a repurposing drug library of ion channel blockers yielded two compounds that inhibit the E protein: Gliclazide and Memantine. In conclusion, as a route to curb viral virulence and abate COVID-19, we point to the E protein of SARS-CoV-2 as an attractive drug target and identify off-label compounds that inhibit it.
Keywords	COVID-19 infection ; Severe acute respiratory syndrome coronavirus 2 ; drugs ; etiological agents ; ion channels ; research ; virulence ; viruses
Language	English
Dates of publication	2020-0910
Size	p. 10-14.
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.2020.05.206
Database	NAL-Catalogue (AGRICOLA)

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Article ; Online: SARS-CoV-2 E protein is a potential ion channel that can be inhibited by Gliclazide and Memantine

Singh Tomar, Prabhat Pratap / Arkin, Isaiah T.

Biochemical and Biophysical Research Communications

2020 Volume 530, Issue 1, Page(s) 10–14

Keywords	Biophysics ; Cell Biology ; Biochemistry ; Molecular Biology ; covid19
Language	English
Publisher	Elsevier BV
Publishing country	us
Document type	Article ; Online
ZDB-ID	205723-2
ISSN	0006-291X ; 0006-291X
ISSN (online)	0006-291X
ISSN	0006-291X
DOI	10.1016/j.bbrc.2020.05.206
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Zs.A 116: Show issues

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Article ; Online: Targeted Drug Repurposing Against the SARS-CoV-2 E Channel Identifies Blockers With in vitro Antiviral Activity

Tomar, Prabhat Pratap Singh / Krugliak, Miriam / Arkin, Isaiah T

bioRxiv

Abstract: It is difficult to overstate the impact that COVID-19 had on humankind. The pandemic9s etiological agent, SARS-CoV-2, is a member of the Coronaviridae, and as such, is an enveloped virus with ion channels in its membrane. Therefore, in an attempt to ... ...

Abstract	It is difficult to overstate the impact that COVID-19 had on humankind. The pandemic9s etiological agent, SARS-CoV-2, is a member of the Coronaviridae, and as such, is an enveloped virus with ion channels in its membrane. Therefore, in an attempt to provide an option to curb the viral spread, we searched for blockers of its E protein viroporin. Using three bacteria-based assays, we identified eight compounds that exhibited activity after screening a library of ca. 3000 approved-for-human-use drugs. Reassuringly, analysis of viral replication in tissue culture indicated that most of the compounds could reduce infectivity to varying extents. In conclusion, targeting a particular channel in the virus for drug repurposing may increase our arsenal of treatment options to combat COVID-19 virulence.
Keywords	covid19
Language	English
Publishing date	2021-02-24
Publisher	Cold Spring Harbor Laboratory
Document type	Article ; Online
DOI	10.1101/2021.02.24.432490
Database	COVID19

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