Selective Voltage Gated KV1.3 Potassium Channel Inhibitors

Abstract

Researchers at the University of California, Davis, have discovered a composition of 5-phenoxyalkoxypsoralens that inhibits potassium channels to treat autoimmune diseases and disorders that involve abnormal homeostasis, body weight and peripheral insulin sensitivity.

Full Description

T-lymphocytes are key players in autoimmune diseases. Current therapies for T cell-mediated autoimmune diseases typically involve the use of immunosuppressants. Immunosuppressants are non-specific and as a result have severe side effects including liver and renal damage. There is a need for new targeted therapies and treatments for autoimmune diseases with lower risk for side effects.

Researchers at the University of California, Davis, have developed a new class of small-molecule inhibitors that block low nanomolar Kv1.3 potassium channels. By targeting Kv1.3 channels, the predominate potassium channel in effector memory T cells, the molecules preferentially suppress T-cell proliferation. Kv1.3 channels have also been shown to regulate energy homeostasis, body weight, and peripheral insulin sensitivity, lending to their use in such disorders. By inhibiting specific channels, the small molecules provide specific therapeutic effects with minimal side effects.

Applications

• Autoimmune diseases
• Organ rejection and/or graft vs. host disease
• Diseases and disorders that involve abnormal homeostasis, body weight and peripheral insulin sensitivity

Features/Benefits

• Treats issues such as organ rejection and/or graft vs. host disease
• Treats autoimmune disorders (blood, endocrine, GI, musculoskeletal, ophthalmologic, skin nervous, vascular)
• Regulates energy homeostasis, body weight, and peripheral insulin sensitivity

Patent Status