T3DB: Kaliotoxin-3

Identification Taxonomy Biological Properties Physical Properties Toxicity Profile Spectra Concentrations Links References Gene Regulation Targets (6)XML

Targets (6)

Record Information

Version

2.0

Creation Date

2009-07-03 22:19:08 UTC

Update Date

2014-12-24 20:25:39 UTC

Accession Number

T3D2518

Identification

Common Name

Kaliotoxin-3

Class

Protein

Description

Kaliotoxin-3 is a peptide toxin produced by the Common European scorpion (Buthus occitanus tunetanus). It is a neurotoxin that binds to voltage-gated and calcium-activated potassium channels. (4)

Compound Type

Amide
Amine
Animal Toxin
Natural Compound
Organic Compound
Protein
Scorpion Toxin

Protein Structure

Synonyms

Synonym
KTX-3
KTX3
Potassium channel toxin alpha-KTx 3.9

Chemical Formula

Not Available

Average Molecular Mass

4027.840 g/mol

CAS Registry Number

223246-26-2

Sequence

Not Available

Chemical Taxonomy

Description

Not Available

Kingdom

Organic Compounds

Super Class

Organic Acids

Class

Carboxylic Acids and Derivatives

Sub Class

Amino Acids, Peptides, and Analogues

Direct Parent

Peptides

Alternative Parents

Not Available

Substituents

Not Available

Molecular Framework

Not Available

External Descriptors

Not Available

Biological Properties

Status

Detected and Not Quantified

Origin

Exogenous

Cellular Locations

Not Available

Biofluid Locations

Not Available

Tissue Locations

Not Available

Pathways

Not Available

Applications

Not Available

Biological Roles

Not Available

Chemical Roles

Not Available

Physical Properties

State

Liquid

Appearance

Clear solution.

Experimental Properties

Property	Value
Melting Point	Not Available
Boiling Point	Not Available
Solubility	>10 mg/mL
LogP	Not Available

Predicted Properties

Not Available

Spectra

Spectrum Type	Description	Splash Key	Deposition Date	View

Toxicity Profile

Route of Exposure

Injection (sting/bite) (5)

Mechanism of Toxicity

Kaliotoxin is a neurotoxin that binds to voltage-gated and calcium-activated potassium channels. It binds to the extracellular surface and blocks the channel, affecting the regulation of processes such as neurotransmitter release, heart rate, insulin secretion, smooth muscle contraction. (4)

Metabolism

Free toxin may be removed by opsonization via the reticuloendothelial system (primarily the liver and kidneys) or it may be degraded through cellular internalization via the lysosomes. Lysosomes are membrane-enclosed organelles that contain an array of digestive enzymes, including several proteases.

Toxicity Values

LD50: 0.90 mg/kg (Subcutaneous, Mouse) (2)

Lethal Dose

Not Available

Carcinogenicity (IARC Classification)

No indication of carcinogenicity to humans (not listed by IARC).

Uses/Sources

Kaliotoxin-3 is a peptide toxin produced by the Common European scorpion (Buthus occitanus tunetanus). (4)

Minimum Risk Level

Not Available

Health Effects

Kaliotoxin is neurotoxic. (4)

Symptoms

Scorpion stings cause tingling or burning at the site of the sting. In more severe cases, symptoms may include spasm in the throat, feeling of thick tongue, restlessness, muscular fibrillation, abdominal cramps, convulsions, incontinence, hypertension, hypotension, oliguria, cardiac arrhythmias, pulmonary edema, and respiratory failure. (1)

Treatment

An antivenom exists for Buthus stings. (3)

Normal Concentrations

Not Available

Abnormal Concentrations

Not Available

External Links

DrugBank ID

Not Available

HMDB ID

Not Available

PubChem Compound ID

Not Available

ChEMBL ID

Not Available

ChemSpider ID

Not Available

KEGG ID

Not Available

UniProt ID

P59290

OMIM ID

ChEBI ID

Not Available

BioCyc ID

Not Available

CTD ID

Not Available

Stitch ID

Not Available

PDB ID

Not Available

ACToR ID

Not Available

Wikipedia Link

Not Available

References

Synthesis Reference

Not Available

MSDS

Not Available

General References

Dreisbach, RH (1983). Handbook of Poisoning. Los Altos, California: Lange Medical Publications.
Watt DD, Simard JM. Neurotoxic proteins in scorpion venom. J. Toxicol. Toxin Rev. 1984;3:181-221.
Wikipedia. Antivenom. Last Updated 1 July 2009. [Link]
Wikipedia. Kaliotoxin. Last Updated 24 June 2009. [Link]
Wikipedia. Scorpion toxin. Last Updated 12 July 2009. [Link]

Gene Regulation

Up-Regulated Genes

Not Available

Down-Regulated Genes

Not Available

Targets

Target Details

1. Calcium-activated potassium channel subunit alpha-1

General Function:: Voltage-gated potassium channel activity
Specific Function:: Potassium channel activated by both membrane depolarization or increase in cytosolic Ca(2+) that mediates export of K(+). It is also activated by the concentration of cytosolic Mg(2+). Its activation dampens the excitatory events that elevate the cytosolic Ca(2+) concentration and/or depolarize the cell membrane. It therefore contributes to repolarization of the membrane potential. Plays a key role in controlling excitability in a number of systems, such as regulation of the contraction of smooth muscle, the tuning of hair cells in the cochlea, regulation of transmitter release, and innate immunity. In smooth muscles, its activation by high level of Ca(2+), caused by ryanodine receptors in the sarcoplasmic reticulum, regulates the membrane potential. In cochlea cells, its number and kinetic properties partly determine the characteristic frequency of each hair cell and thereby helps to establish a tonotopic map. Kinetics of KCNMA1 channels are determined by alternative splicing, phosphorylation status and its combination with modulating beta subunits. Highly sensitive to both iberiotoxin (IbTx) and charybdotoxin (CTX).
Gene Name:: KCNMA1
Uniprot ID:: Q12791
Molecular Weight:: 137558.115 Da

References

Wikipedia. Kaliotoxin. Last Updated 24 June 2009. [Link]

Target Details

2. Calcium-activated potassium channel subunit beta-1

General Function:: Potassium channel regulator activity
Specific Function:: Regulatory subunit of the calcium activated potassium KCNMA1 (maxiK) channel. Modulates the calcium sensitivity and gating kinetics of KCNMA1, thereby contributing to KCNMA1 channel diversity. Increases the apparent Ca(2+)/voltage sensitivity of the KCNMA1 channel. It also modifies KCNMA1 channel kinetics and alters its pharmacological properties. It slows down the activation and the deactivation kinetics of the channel. Acts as a negative regulator of smooth muscle contraction by enhancing the calcium sensitivity to KCNMA1. Its presence is also a requirement for internal binding of the KCNMA1 channel opener dehydrosoyasaponin I (DHS-1) triterpene glycoside and for external binding of the agonist hormone 17-beta-estradiol (E2). Increases the binding activity of charybdotoxin (CTX) toxin to KCNMA1 peptide blocker by increasing the CTX association rate and decreasing the dissociation rate.
Gene Name:: KCNMB1
Uniprot ID:: Q16558
Molecular Weight:: 21797.27 Da

References

Wikipedia. Kaliotoxin. Last Updated 24 June 2009. [Link]

Target Details

3. Calcium-activated potassium channel subunit beta-2

General Function:: Potassium channel regulator activity
Specific Function:: Regulatory subunit of the calcium activated potassium KCNMA1 (maxiK) channel. Modulates the calcium sensitivity and gating kinetics of KCNMA1, thereby contributing to KCNMA1 channel diversity. Acts as a negative regulator that confers rapid and complete inactivation of KCNMA1 channel complex. May participate in KCNMA1 inactivation in chromaffin cells of the adrenal gland or in hippocampal CA1 neurons.
Gene Name:: KCNMB2
Uniprot ID:: Q9Y691
Molecular Weight:: 27129.37 Da

References

Wikipedia. Kaliotoxin. Last Updated 24 June 2009. [Link]

Target Details

4. Calcium-activated potassium channel subunit beta-3

General Function:: Potassium channel regulator activity
Specific Function:: Regulatory subunit of the calcium activated potassium KCNMA1 (maxiK) channel. Modulates the calcium sensitivity and gating kinetics of KCNMA1, thereby contributing to KCNMA1 channel diversity. Alters the functional properties of the current expressed by the KCNMA1 channel. Isoform 2, isoform 3 and isoform 4 partially inactivate the current of KCNBMA. Isoform 4 induces a fast and incomplete inactivation of KCNMA1 channel that is detectable only at large depolarizations. In contrast, isoform 1 does not induce detectable inactivation of KCNMA1. Two or more subunits of KCNMB3 are required to block the KCNMA1 tetramer.
Gene Name:: KCNMB3
Uniprot ID:: Q9NPA1
Molecular Weight:: 31603.26 Da

References

Wikipedia. Kaliotoxin. Last Updated 24 June 2009. [Link]

Target Details

5. Calcium-activated potassium channel subunit beta-4

General Function:: Potassium channel regulator activity
Specific Function:: Regulatory subunit of the calcium activated potassium KCNMA1 (maxiK) channel. Modulates the calcium sensitivity and gating kinetics of KCNMA1, thereby contributing to KCNMA1 channel diversity. Decreases the gating kinetics and calcium sensitivity of the KCNMA1 channel, but with fast deactivation kinetics. May decrease KCNMA1 channel openings at low calcium concentrations but increases channel openings at high calcium concentrations. Makes KCNMA1 channel resistant to 100 nM charybdotoxin (CTX) toxin concentrations.
Gene Name:: KCNMB4
Uniprot ID:: Q86W47
Molecular Weight:: 23948.465 Da

References

Wikipedia. Kaliotoxin. Last Updated 24 June 2009. [Link]

Target Details

6. Potassium voltage-gated channel subfamily A member 3

General Function:: Voltage-gated ion channel activity
Specific Function:: Mediates the voltage-dependent potassium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a potassium-selective channel through which potassium ions may pass in accordance with their electrochemical gradient.
Gene Name:: KCNA3
Uniprot ID:: P22001
Molecular Weight:: 63841.09 Da

References

Wikipedia. Kaliotoxin. Last Updated 24 June 2009. [Link]

Kaliotoxin-3 (T3D2518)

Targets

References

References

References

References

References

References