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Modulators of small- and intermediate-conductance calcium-activated potassium channels and their therapeutic indications.
TLDR
The physiological properties, the structure activity relationships of the existing peptide and small molecule modulators and the therapeutic importance of the three small-conductance channels KCa2.1-K Ca2.3-KCa3.1 are reviewed to constitute attractive new targets for several diseases that currently have no effective therapies. Expand
Selective positive modulator of calcium-activated potassium channels exerts beneficial effects in a mouse model of spinocerebellar ataxia type 2.
TLDR
It is shown here that the type 2 small conductance calcium-activated potassium channel (SK2) play a key role in control of normal PC activity and that SK2 channels constitute a therapeutic target for SCA2 treatment and that the developed selective SK2/3 modulator NS13001 holds promise as a potential therapeutic agent for treatment ofSCA2 and possibly other cerebellar ataxias. Expand
K+ channel types targeted by synthetic OSK1, a toxin from Orthochirus scrobiculosus scorpion venom.
TLDR
Data suggest that OSK1 or [K16,D20]-OSK1 could serve as leads for the design and production of new immunosuppressive drugs. Expand
Evidence for neurotoxic activity of tat from human immunodeficiency virus type 1.
TLDR
Experiments in vivo showed that synthetic tat is a potent and lethal neurotoxic agent in mice and the use of tat peptide derivatives showed that basic region from 49 to 57 is necessary and sufficient for binding to cell membranes and toxicity. Expand
Design and Characterization of a Highly Selective Peptide Inhibitor of the Small Conductance Calcium-activated K+Channel, SkCa2*
TLDR
Lei-Dab7, a structure-based design of a selective inhibitor of SKCa2 that interacts with residues in the external vestibule of the channel, is generated and will be a useful tool to investigate the functional role ofSKCa2 in mammalian tissues. Expand
Diversity of folds in animal toxins acting on ion channels.
TLDR
An up-to-date overview of the various types of fold from animal toxins that act on ion channels selective for K+, Na+, Ca2+ or Cl- ions, with special emphasis on disulphide bridge frameworks and structural motifs associated with these peptide folds. Expand
Selective Blocking of Voltage-Gated K+ Channels Improves Experimental Autoimmune Encephalomyelitis and Inhibits T Cell Activation1
TLDR
KTX is a potent immunosuppressive agent with beneficial effects on the neurological symptoms of EAE, using experimental autoimmune encephalomyelitis (EAE), an animal model for multiple sclerosis. Expand
Animal toxins acting on voltage-gated potassium channels.
TLDR
It appears that the ability of structurally divergent toxins to interact with a particular Kv channel relies onto a similar spatial distribution of amino acid residues that are key to the toxin-channel interaction (rather than the type of toxin fold). Expand
Maurotoxin: a potent inhibitor of intermediate conductance Ca2+-activated potassium channels.
TLDR
The results from this study show that maurotoxin is a potent inhibitor of the IK1 subclass of K(Ca) potassium channels and may serve as a useful tool for further defining the physiological role of this channel subtype. Expand
Chemical synthesis and characterization of maurotoxin, a short scorpion toxin with four disulfide bridges that acts on K+ channels.
TLDR
The physicochemical and pharmacological properties of synthetic maurotoxin were indistinguishable from those of natural mau Rotoxin, which suggests that natural mAUrotoxin adopts the same half-cystine pairing pattern. Expand
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