KCa3.1—a microglial target ready for drug repurposing?

GLIA - Tập 64 Số 10 - Trang 1733-1741 - 2016
E Dale1, Roland G. W. Staal1, Claudia Eder2, Thomas Möller1
1Neuroinflammation Disease Biology Unit, Lundbeck Research USA, Paramus, New Jersey
2Institute for Infection and Immunity, St. George's, University of London, United Kingdom

Tóm tắt

Over the past decade, glial cells have attracted attention for harboring unexploited targets for drug discovery. Several glial targets have attracted de novo drug discovery programs, as highlighted in this GLIA Special Issue. Drug repurposing, which has the objective of utilizing existing drugs as well as abandoned, failed, or not yet pursued clinical development candidates for new indications, might provide a faster opportunity to bring drugs for glial targets to patients with unmet needs. Here, we review the potential of the intermediate‐conductance calcium‐activated potassium channels KCa3.1 as the target for such a repurposing effort. We discuss the data on KCa3.1 expression on microglia in vitro and in vivo and review the relevant literature on the two KCa3.1 inhibitors TRAM‐34 and Senicapoc. Finally, we provide an outlook of what it might take to harness the potential of KCa3.1 as a bona fide microglial drug target. GLIA 2016;64:1733–1741

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GLIA

Tập 64 Số 10

1733-1741

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