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zetekitoxin ab

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Description

zetekitoxin AB: a sodium channel blocker; isolated from the frog Atelopus zeteki; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID21589240
CHEMBL ID3617050
MeSH IDM0469215

Synonyms (10)

Synonym
zetekitoxin ab
62996-38-7
c7a2uz79fj ,
CHEMBL3617050 ,
bdbm50118519
DTXSID401336333
PD189253
[(3r,5s,6s,11r,12s,16s)-14,17-diamino-19,19-dihydroxy-6-(hydroxymethyl)-10-oxo-3-sulfooxy-8-oxa-1,9,13,15,18-pentazapentacyclo[9.5.2.13,16.05,9.012,16]nonadeca-14,17-dien-13-yl]methyl n-hydroxycarbamate
((3as,4r,6r,7as,8s,13r,13as)-2,15-diamino-5,6,7,7a,8,9,13,13a-octahydro-16,16-dihydroxy-8-(hydroxymethyl)-12-oxo-6-(sulfooxy)-3a,6-methano-13,4-(nitrilometheno)imidazo(4,5-g)isoxazolo(2,3-a)(1,6)diazecin-1(12h)-yl)methyl n-hydroxycarbamate
carbamic acid, hydroxy-, ((3as,4r,6r,7as,8s,13r,13as)-2,15-diamino-5,6,7,7a,8,9,13,13a-octahydro-16,16-dihydroxy-8-(hydroxymethyl)-12-oxo-6-(sulfooxy)-3a,6-methano-13,4-(nitrilometheno)imidazo(4,5-g)isoxazolo(2,3-a)(1,6)diazecin-1(12h)-yl)methyl ester

Research Excerpts

Overview

Zetekitoxin AB is an extremely potent blocker of voltage-dependent sodium channels expressed in Xenopus oocytes.

ExcerptReferenceRelevance
"Zetekitoxin AB proved to be an extremely potent blocker of voltage-dependent sodium channels expressed in Xenopus oocytes."( The structure of zetekitoxin AB, a saxitoxin analog from the Panamanian golden frog Atelopus zeteki: a potent sodium-channel blocker.
Choudhary, G; Daly, JW; Dudley, SC; Kim, YH; Oshima, Y; Pfahnl, A; Yotsu-Yamashita, M, 2004
)
1.38
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Sodium channel protein type 4 subunit alphaHomo sapiens (human)IC50 (µMol)0.00010.00013.507510.0000AID1246043
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC50 (µMol)0.00030.00033.64849.2000AID1246044
Sodium channel protein type 2 subunit alphaHomo sapiens (human)IC50 (µMol)0.00000.00003.740110.0000AID1246042
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (49)

Processvia Protein(s)Taxonomy
sodium ion transportSodium channel protein type 4 subunit alphaHomo sapiens (human)
muscle contractionSodium channel protein type 4 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 4 subunit alphaHomo sapiens (human)
regulation of skeletal muscle contraction by action potentialSodium channel protein type 4 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 4 subunit alphaHomo sapiens (human)
regulation of heart rateSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac conduction system developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac ventricle developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
brainstem developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
response to denervation involved in regulation of muscle adaptationSodium channel protein type 5 subunit alphaHomo sapiens (human)
telencephalon developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cerebellum developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
odontogenesis of dentin-containing toothSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of epithelial cell proliferationSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cellular response to calcium ionSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of cardiac muscle cell contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
ventricular cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during Purkinje myocyte cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell to bundle of His cell communicationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of heart rate by cardiac conductionSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 2 subunit alphaHomo sapiens (human)
nervous system developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
intrinsic apoptotic signaling pathway in response to osmotic stressSodium channel protein type 2 subunit alphaHomo sapiens (human)
neuron apoptotic processSodium channel protein type 2 subunit alphaHomo sapiens (human)
memorySodium channel protein type 2 subunit alphaHomo sapiens (human)
determination of adult lifespanSodium channel protein type 2 subunit alphaHomo sapiens (human)
neuronal action potentialSodium channel protein type 2 subunit alphaHomo sapiens (human)
dentate gyrus developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
nerve developmentSodium channel protein type 2 subunit alphaHomo sapiens (human)
myelinationSodium channel protein type 2 subunit alphaHomo sapiens (human)
cellular response to hypoxiaSodium channel protein type 2 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 2 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 2 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (17)

Processvia Protein(s)Taxonomy
voltage-gated sodium channel activitySodium channel protein type 4 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 4 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 5 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
fibroblast growth factor bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
enzyme bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein kinase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein domain specific bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ankyrin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ubiquitin protein ligase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
nitric-oxide synthase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in Purkinje myocyte action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
scaffold protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 2 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 2 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 2 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (19)

Processvia Protein(s)Taxonomy
plasma membraneSodium channel protein type 4 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 4 subunit alphaHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleolusSodium channel protein type 5 subunit alphaHomo sapiens (human)
endoplasmic reticulumSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
cell surfaceSodium channel protein type 5 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 5 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
lateral plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 5 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 5 subunit alphaHomo sapiens (human)
sarcolemmaSodium channel protein type 5 subunit alphaHomo sapiens (human)
perinuclear region of cytoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 2 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 2 subunit alphaHomo sapiens (human)
axonSodium channel protein type 2 subunit alphaHomo sapiens (human)
node of RanvierSodium channel protein type 2 subunit alphaHomo sapiens (human)
paranode region of axonSodium channel protein type 2 subunit alphaHomo sapiens (human)
presynaptic membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
glutamatergic synapseSodium channel protein type 2 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 2 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 2 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (3)

Assay IDTitleYearJournalArticle
AID1246042Inhibition of NaV1.2 channel (unknown origin) expressed in Xenopus laevis oocytes by two-electrode oocyte voltage-clamp method2015Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18
Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications.
AID1246043Inhibition of NaV1.4 channel (unknown origin) expressed in Xenopus laevis oocytes by two-electrode oocyte voltage-clamp method2015Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18
Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications.
AID1246044Inhibition of NaV1.5 channel (unknown origin) expressed in Xenopus laevis oocytes by two-electrode oocyte voltage-clamp method2015Journal of medicinal chemistry, Sep-24, Volume: 58, Issue:18
Voltage-Gated Sodium Channels: Structure, Function, Pharmacology, and Clinical Indications.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's2 (40.00)29.6817
2010's3 (60.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews3 (60.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other2 (40.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]