產(chǎn)品詳情

  • 產(chǎn)品名稱：(Dap22)-ShK

  • 產(chǎn)品型號：
  • 產(chǎn)品廠商：Smartox-Biotech
  • 產(chǎn)品文檔：
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簡單介紹：
(Dap22)-ShK
詳情介紹：
Sequence AA sequence: Arg-Ser-Cys3-Ile-Asp-Thr-Ile-Pro-Lys- Ser-Arg-Cys12-Thr-Ala-Phe-Gln-Cys17-Lys-His-Ser -Met-Dap-Tyr-Arg-Leu-Ser-Phe-Cys28-Arg-Lys -Thr-Cys32-Gly-Thr-Cys35-OH Disulfide bonds: Cys3-Cys35, Cys12-Cys28 and Cys17-Cys32
Characteristics Selective blocker of Kv1.3
Background (Dap22)-ShK (ShK Dap22) peptide is a synthetic derivative of the well-known ShK toxin (Stichodactyla helianthus neurotoxin) isolated from the venom of the Carribean sea anemone Stoichactis helianthus. Wild-type ShK blocks voltage-gated Kv1.1, Kv1.3, Kv1.4 and Kv1.6 channels at equal subnanomolar concentrations. In (Dap22)-ShK, lysine22 has been replaced by a diaminopropionic acid (Dap) residue that greatly improves the selectivity of the peptide for the voltage-gated potassium channel Kv1.3 (IC50 around 23 pM) against Kv1.1 (1.8 nM), Kv1.4 (37 nM) and Kv1.6 (10 nM) channels. The high selectivity of (Dap22)-Shk is achieved thanks to the strong binding between the Dap and His404 / Asp386 residues of Kv1.3 channel. (Dap22)-ShK inhibits T cell proliferation induced by anti-CD3 at subnanomolar concentrations.
Molecular Weight 4012.8 kDa
CAS-No 220384-25-8
Restrictions For Research Use only
Storage -20 °C
Background publications Robbins, Lee, Filipovich, Szigligeti, Neumeier, Petrovic, Conforti: "Hypoxia modulates early events in T cell receptor-mediated activation in human T lymphocytes via Kv1.3 channels." in: The Journal of physiology, Vol. 564, Issue Pt 1, pp. 131-43, 2005 (PubMed).

Norton, Pennington, Wulff: "Potassium channel blockade by the sea anemone toxin ShK for the treatment of multiple sclerosis and other autoimmune diseases." in: Current medicinal chemistry, Vol. 11, Issue 23, pp. 3041-52, 2004 (PubMed).

Middleton, Sanchez, Linde, Bugianesi, Dai, Felix, Koprak, Staruch, Bruguera, Cox, Ghosh, Hwang, Jones, Kohler, Slaughter, McManus, Kaczorowski, Garcia: "Substitution of a single residue in Stichodactyla helianthus peptide, ShK-Dap22, reveals a novel pharmacological profile." in: Biochemistry, Vol. 42, Issue 46, pp. 13698-707, 2003 (PubMed).

Lanigan, Kalman, Lefievre, Pennington, Chandy, Norton: "Mutating a critical lysine in ShK toxin alters its binding configuration in the pore-vestibule region of the voltage-gated potassium channel, Kv1.3." in: Biochemistry, Vol. 41, Issue 40, pp. 11963-71, 2002 (PubMed).

Beeton, Wulff, Barbaria, Clot-Faybesse, Pennington, Bernard, Cahalan, Chandy, Béraud: "Selective blockade of T lymphocyte K(+) channels ameliorates experimental autoimmune encephalomyelitis, a model for multiple sclerosis." in: Proceedings of the National Academy of Sciences of the United States of America, Vol. 98, Issue 24, pp. 13942-7, 2001 (PubMed).