Overview
- Romi-Lebrun, R. et al. (1997) Biochemistry 36, 13473.
- Han, S. et al. (2008) J. Biol. Chem. 283, 19058.
- Li, Z. et al. (2012) J. Biol. Chem. 287, 29479.
Alomone Labs ADWX-1 inhibits KV1.3 currents heterologously expressed in Xenopus oocytes.A. Time course of ADWX-1 (#STW-100) blocking action on KV1.3 currents. Membrane potential was held at -80 mV and cells were stimulated by a 100 ms voltage ramp to +40 mV. 1 nM ADWX-1 was perfused as indicated by the bar (green) at +35 mV. B. Superimposed examples of KV1.3 channel current in the absence (control) and presence (green) of 1 nM ADWX-1 (taken from the experiment in A).
KV1.3 channel is an attractive pharmacological target for immunomodulation of T cell-mediated autoimmune diseases. ADWX-1 peptide is a potent and selective KV1.3 channel blocker. ADWX-1 peptide is a synthetic analog of the scorpion peptide BmKTx. This peptide is based on the natural BmKTX in which three important residues were mutated in a structure-modification strategy to enhance the KV1.3 channel selectivity1. ADWX-1 inhibits KV1.3 channels heterologously expressed in HEK-293 cells. ADWX-1 blocks KV1.3 currents with an IC50 of 0.0019 nM and displays specificity for KV1.3 over KV1.1 and KV1.2 (IC50 values are 0.65 nM).
ADWX-1 inhibits CD4+ CCR7- T-cell proliferation.
ADWX-1 is an interesting therapeutic candidate to treat auto-immune disorders such as multiple sclerosis, type-1 diabetes, rheumatoid arthritis and psoriasis. This peptide is a valuable tool for studying the structure-function of KV1.3 channel and auto-immunity pathways2.
