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Stockinger, F.

Publications and source records attributed to Stockinger, F..

2 recordsLinked to original sources

Molecular assembly of the KCNQ1-KCNE1-BACE1 complex

We previously showed that the {beta}-secretase BACE1 directly modulates KCNQ1 channels through a non-proteolytic mechanism. Here, we dissect the molecular interplay among KCNQ1, its canonical auxiliary subunit KCNE1, and BACE1 using bimolecular fluorescence complementation (BiFC), electrophysiology, single-molecule pull-down (SiMPull), and a Forster resonance energy transfer (FRET)-based interaction assay. BiFC validated KCNQ1 homotetramerization and confirmed specific interactions of KCNQ1 with KCNE1 and with BACE1 at the plasma membrane. To map interaction determinants, we generated six KCNE1/BACE1 chimeras. BiFC and electrophysiological recordings revealed domain-specific contributions: BACE1s large extracellular domain primarily mediates its modulatory effects on KCNQ1 gating, while--consistent with previous reports--the KCNE1 transmembrane segment is necessary and sufficient to confer an IKs-like phenotype, and the KCNE1 intracellular domain tunes the voltage dependence of activation. Notably, a chimera combining the BACE1 extracellular region with KCNE1 transmembrane and intracellular regions produced an IKs-like current with additional BACE1-like slowing of activation, indicating functional additivity. Stoichiometry measurements by SiMPull and bleaching-step analysis demonstrated that KCNQ1 channel complexes predominantly recruit two BACE1 molecules. Although BACE1 oligomerizes at the plasma membrane, BiFC and FRET showed that KCNQ1 co-expression reduces BACE1 homomeric assembly, and this effect is unchanged by KCNE1 co-expression. Together, our data support a model in which BACE1 binds directly to KCNQ1, occupies a site distinct from KCNE1, and modulates KCNQ1 gating via its extracellular domain while remaining compatible with KCNE1 co-assembly.

biophysics↗

BACE1 regulates sleep-wake cycle through both enzymatic and non-enzymatic actions.

The {beta}-secretase BACE1 has become a prime target in Alzheimers disease (AD) therapy, because it drives the production of pathogenic amyloid {beta} peptides. However, clinical trials with BACE1-targeting drugs were halted due to adverse effects on cognitive performance. We propose here that cognitive impairment by BACE1 inhibitors may be a corollary of a higher function of BACE1 related to proper sleep regulation. To address non-enzymatic effects of BACE1 on ion channels likely involved in the sleep-wake cycle, we analyzed sleep patterns in both BACE1-KO mice and a newly generated transgenic line expressing a proteolysis-deficient BACE1 variant (BACE1-KI). We found that BACE1-KI and BACE1-KO mice displayed common and distinct sleep-wake disturbances. Compared to their respective wild-type littermates, both mutant lines slept less during the light phase (when they preferentially rest). Furthermore, transition rates between wake and sleep states were altered, as were sleep spindles and EEG power spectra mainly in the gamma range. Thus, a better understanding of how BACE1 interferes with sleep-modulated behaviors is needed if clinical trials with BACE1-targeted inhibitors are to resume.

animal behavior and cognition↗