- Beeton, Christine;
- Wulff, Heike;
- Standifer, Nathan E;
- Azam, Philippe;
- Mullen, Katherine M;
- Pennington, Michael W;
- Kolski-Andreaco, Aaron;
- Wei, Eric;
- Grino, Alexandra;
- Counts, Debra R;
- Wang, Ping H;
- LeeHealey, Christine J;
- Andrews, Brian S;
- Sankaranarayanan, Ananthakrishnan;
- Homerick, Daniel;
- Roeck, Werner W;
- Tehranzadeh, Jamshid;
- Stanhope, Kimber L;
- Zimin, Pavel;
- Havel, Peter J;
- Griffey, Stephen;
- Knaus, Hans-Guenther;
- Nepom, Gerald T;
- Gutman, George A;
- Calabresi, Peter A;
- Chandy, K George
Autoreactive memory T lymphocytes are implicated in the pathogenesis of autoimmune diseases. Here we demonstrate that disease-associated autoreactive T cells from patients with type-1 diabetes mellitus or rheumatoid arthritis (RA) are mainly CD4+ CCR7- CD45RA- effector memory T cells (T(EM) cells) with elevated Kv1.3 potassium channel expression. In contrast, T cells with other antigen specificities from these patients, or autoreactive T cells from healthy individuals and disease controls, express low levels of Kv1.3 and are predominantly naïve or central-memory (T(CM)) cells. In T(EM) cells, Kv1.3 traffics to the immunological synapse during antigen presentation where it colocalizes with Kvbeta2, SAP97, ZIP, p56(lck), and CD4. Although Kv1.3 inhibitors [ShK(L5)-amide (SL5) and PAP1] do not prevent immunological synapse formation, they suppress Ca2+-signaling, cytokine production, and proliferation of autoantigen-specific T(EM) cells at pharmacologically relevant concentrations while sparing other classes of T cells. Kv1.3 inhibitors ameliorate pristane-induced arthritis in rats and reduce the incidence of experimental autoimmune diabetes in diabetes-prone (DP-BB/W) rats. Repeated dosing with Kv1.3 inhibitors in rats has not revealed systemic toxicity. Further development of Kv1.3 blockers for autoimmune disease therapy is warranted.