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Margatoxin

 

 
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Margatoxin
 
 
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Margatoxin (MgTx) is a Kv1.3 voltage-dependent potassium channel
Potassium channel

In the field of cell biology, potassium channels are the most widely distributed type of ion channel and are found in virtually all living organisms....
-blocking toxic peptide
Peptide

Peptides are short polymers formed from the linking, in a defined order, of a-amino acids. The link between one amino acid residue and the next is known as an amide chemical bond or a peptide bond....
 found in the venom of the South American scorpion
Scorpion

Scorpions are any arachnid of the order Scorpionida. They are members of the order Scorpiones within the class Arachnida. There are about 2,000 species of scorpions, found widely distributed south of about Latitude, except New Zealand and Antarctica....
 Centruroides margaritatus.

entruroides margaritatus is also known as the Central American bark scorpion. It is native to Central and South America. Typical examples are 5-8 cm long, including the tail.

amino acid
Amino acid

In chemistry, an amino acid is a molecule containing both amine and carboxyl functional groups. These molecules are particularly important in biochemistry, where this term refers to alpha-amino acids with the general formula H2NCHRCOOH, where R is an organic substituent....
 sequence is:

H-Thr-Ile-Ile-Asn-Val-Lys-Cys-Thr-Ser-Pro-Lys-Gln-Cys-Leu-Pro-Pro-Cys-Lys-Ala-Gln-Phe-Gly-Gln-Ser-Ala-Gly-Ala-Lys-Cys-Met-Asn-Gly-Lys-Cys-Lys-Cys-Tyr-Pro-His-OH (Disulfide bonds between Cys7-Cys29, Cys13-Cys34 and Cys17-Cys36).

The molecular formula is C178H286N52O50S7 and the molecular weight is 4179.0.

atoxin is a specific blocker for Kv1.3 potassium channels
Potassium channel

In the field of cell biology, potassium channels are the most widely distributed type of ion channel and are found in virtually all living organisms....
.

atoxin blocks Kv1.3 channels specifically with high chemical affinity
Chemical affinity

In chemical physics and physical chemistry, chemical affinity can be defined as electronic properties by which dissimilar chemical species are capable of forming chemical compounds....
 (picomolar concentrations) as a peptidyl inhibitor.






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Margatoxin (MgTx) is a Kv1.3 voltage-dependent potassium channel
Potassium channel

In the field of cell biology, potassium channels are the most widely distributed type of ion channel and are found in virtually all living organisms....
-blocking toxic peptide
Peptide

Peptides are short polymers formed from the linking, in a defined order, of a-amino acids. The link between one amino acid residue and the next is known as an amide chemical bond or a peptide bond....
 found in the venom of the South American scorpion
Scorpion

Scorpions are any arachnid of the order Scorpionida. They are members of the order Scorpiones within the class Arachnida. There are about 2,000 species of scorpions, found widely distributed south of about Latitude, except New Zealand and Antarctica....
 Centruroides margaritatus.

Source

Centruroides margaritatus is also known as the Central American bark scorpion. It is native to Central and South America. Typical examples are 5-8 cm long, including the tail.

Chemistry

The amino acid
Amino acid

In chemistry, an amino acid is a molecule containing both amine and carboxyl functional groups. These molecules are particularly important in biochemistry, where this term refers to alpha-amino acids with the general formula H2NCHRCOOH, where R is an organic substituent....
 sequence is:

H-Thr-Ile-Ile-Asn-Val-Lys-Cys-Thr-Ser-Pro-Lys-Gln-Cys-Leu-Pro-Pro-Cys-Lys-Ala-Gln-Phe-Gly-Gln-Ser-Ala-Gly-Ala-Lys-Cys-Met-Asn-Gly-Lys-Cys-Lys-Cys-Tyr-Pro-His-OH (Disulfide bonds between Cys7-Cys29, Cys13-Cys34 and Cys17-Cys36).

The molecular formula is C178H286N52O50S7 and the molecular weight is 4179.0.

Target

Margatoxin is a specific blocker for Kv1.3 potassium channels
Potassium channel

In the field of cell biology, potassium channels are the most widely distributed type of ion channel and are found in virtually all living organisms....
.

Mode of action

Margatoxin blocks Kv1.3 channels specifically with high chemical affinity
Chemical affinity

In chemical physics and physical chemistry, chemical affinity can be defined as electronic properties by which dissimilar chemical species are capable of forming chemical compounds....
 (picomolar concentrations) as a peptidyl inhibitor. These channels play a key role in neurotransmitter
Neurotransmitter

Neurotransmitters are chemistry which relay, amplify and modulate signals between a neuron and another cell . Neurotransmitters are packaged into vesicles that cluster beneath the membrane on the presynaptic side of a synapse, and are released into the synaptic cleft, where they bind to receptors in the membrane on the postsynaptic side of...
 release. Blocking these channels results in a loss of outward current
Current

Current may refer to:* Current affairs* Electric current* Current ** Ocean current* Current , geometrical current in differential topology...
.

Toxicity

The median lethal dose (LD50) of margatoxin is 59.9 mg/kg, so Centruroides margaritatus stings are not dangerous to humans except as a result of possible anaphylactic
Anaphylaxis

Anaphylaxis is an acute Circulatory system and very severe Type I hypersensitivity allergy reaction in humans and other mammals. The term comes from the Greek words a?a ana and f??a??? phylaxis ....
 responses. They do cause pain, local swelling and tingling for 3-4 hours, but no intervention beyond symptomatic relief should be necessary.