Vm24, a natural immunosuppressive peptide, potently and selectively blocks Kv1.3 potassium channels of human T cells.
Mol Pharmacol
; 82(3): 372-82, 2012 Sep.
Article
em En
| MEDLINE
| ID: mdl-22622363
ABSTRACT
Blockade of Kv1.3 K(+) channels in T cells is a promising therapeutic approach for the treatment of autoimmune diseases such as multiple sclerosis and type 1 diabetes mellitus. Vm24 (α-KTx 23.1) is a novel 36-residue Kv1.3-specific peptide isolated from the venom of the scorpion Vaejovis mexicanus smithi. Vm24 inhibits Kv1.3 channels of human lymphocytes with high affinity (K(d) = 2.9 pM) and exhibits >1500-fold selectivity over other ion channels assayed. It inhibits the proliferation and Ca(2+) signaling of human T cells in vitro and reduces delayed-type hypersensitivity reactions in rats in vivo. Our results indicate that Vm24 has exceptional pharmacological properties that make it an excellent candidate for treatment of certain autoimmune diseases.
Texto completo:
1
Coleções:
01-internacional
Temas:
Geral
Base de dados:
MEDLINE
Assunto principal:
Linfócitos T
/
Bloqueadores dos Canais de Potássio
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Canal de Potássio Kv1.3
/
Imunossupressores
Limite:
Animals
/
Female
/
Humans
Idioma:
En
Revista:
Mol Pharmacol
Ano de publicação:
2012
Tipo de documento:
Article
País de afiliação:
Hungria