Discovery of KV 1.3 ion channel inhibitors: Medicinal chemistry approaches and challenges.
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ABSTRACT: The KV 1.3 voltage-gated potassium ion channel is involved in many physiological processes both at the plasma membrane and in the mitochondria, chiefly in the immune and nervous systems. Therapeutic targeting KV 1.3 with specific peptides and small molecule inhibitors shows great potential for treating cancers and autoimmune diseases, such as multiple sclerosis, type I diabetes mellitus, psoriasis, contact dermatitis, rheumatoid arthritis, and myasthenia gravis. However, no KV 1.3-targeted compounds have been approved for therapeutic use to date. This review focuses on the presentation of approaches for discovering new KV 1.3 peptide and small-molecule inhibitors, and strategies to improve the selectivity of active compounds toward KV
SUBMITTER: Gubic S
PROVIDER: S-EPMC8252768 | biostudies-literature | 2021 Jul
REPOSITORIES: biostudies-literature
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