期刊
MOLECULAR PHARMACOLOGY
卷 82, 期 3, 页码 372-382出版社
AMER SOC PHARMACOLOGY EXPERIMENTAL THERAPEUTICS
DOI: 10.1124/mol.112.078006
关键词
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资金
- National Institutes of Health National Institute of Neurological Disorders and Stroke [NS073712]
- Hungarian Scientific Research Fund [K 60740, NK 61412]
- Hungarian Social Renewal Operational Program [TAMOP-4.2.2-08/1/2008-0019, TAMOP-4.2.1/B-09/1/KONV-2010-007, TAMOP-4.2.2-A-11/1/KONV-20120025]
- General Management of Academic Personnel Matters
- National Autonomous University of Mexico [IN204110]
- National Council for Science and Technology of Mexico
- Hungarian Science and Technology Foundation [MX-10/207]
- European Union [246556]
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 (alpha-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 Ca2+ 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.
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