Role of NKCC1 Activity in Glioma K⁺ Homeostasis and Cell Growth: New Insights With the Bumetanide-Derivative STS66.

ABSTRACT: Introduction: Na⁺-K⁺-2Cl^- cotransporter isoform 1 (NKCC1) is important in regulating intracellular K⁺ and Cl^- homeostasis and cell volume. In this study, we investigated a role of NKCC1 in regulating glioma K⁺ influx and proliferation in response to apoptosis inducing chemotherapeutic drug temozolomide (TMZ). The efficacy of a new bumetanide (BMT)-derivative NKCC1 inhibitor STS66 [3-(butylamino)-2-phenoxy-5-[(2, 2, 2-trifluoroethylamino) methyl] benzenesulfonamide] in blocking NKCC1 activity was compared with well-established NKCC1 inhibitor BMT. Methods: NKCC1 activity in cultured mouse GL26 and SB28-GFP glioma cells was measured by Rb⁺ (K⁺) influx. The WNK1-SPAK/OSR1-NKCC1 signaling and

SUBMITTER: Luo L 

PROVIDER: S-EPMC7413028 | biostudies-literature | 2020

REPOSITORIES: biostudies-literature