[HTML][HTML] ShK-Dap22, a potent Kv1. 3-specific immunosuppressive polypeptide
K Kalman, MW Pennington, MD Lanigan… - Journal of Biological …, 1998 - ASBMB
The voltage-gated potassium channel in T lymphocytes, Kv1. 3, is an important molecular
target for immunosuppressive agents. A structurally defined polypeptide, ShK, from the sea
anemone Stichodactyla helianthusinhibited Kv1. 3 potently and also blocked Kv1. 1, Kv1. 4,
and Kv1. 6 at subnanomolar concentrations. Using mutant cycle analysis in conjunction with
complementary mutagenesis of ShK and Kv1. 3, and utilizing the structure of ShK, we
determined a likely docking configuration for this peptide in the channel. Based upon this …
target for immunosuppressive agents. A structurally defined polypeptide, ShK, from the sea
anemone Stichodactyla helianthusinhibited Kv1. 3 potently and also blocked Kv1. 1, Kv1. 4,
and Kv1. 6 at subnanomolar concentrations. Using mutant cycle analysis in conjunction with
complementary mutagenesis of ShK and Kv1. 3, and utilizing the structure of ShK, we
determined a likely docking configuration for this peptide in the channel. Based upon this …