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K Ca 3.1—a microglial target ready for drug repurposing?
Author(s) -
Dale Elena,
Staal Roland G. W.,
Eder Claudia,
Möller Thomas
Publication year - 2016
Publication title -
glia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.954
H-Index - 164
eISSN - 1098-1136
pISSN - 0894-1491
DOI - 10.1002/glia.22992
Subject(s) - repurposing , drug repositioning , microglia , drug discovery , drug , biology , drug development , in vivo , neuroscience , pharmacology , neuroglia , bioinformatics , immunology , central nervous system , inflammation , microbiology and biotechnology , ecology
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 K Ca 3.1 as the target for such a repurposing effort. We discuss the data on K Ca 3.1 expression on microglia in vitro and in vivo and review the relevant literature on the two K Ca 3.1 inhibitors TRAM‐34 and Senicapoc. Finally, we provide an outlook of what it might take to harness the potential of K Ca 3.1 as a bona fide microglial drug target. GLIA 2016;64:1733–1741

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