Molecular overlap in the regulation of SK channels by small molecules and phosphoinositides | Zendy

Miao Zhang | Zendy; Xuan-Yu Meng | Zendy; Jifang Zhang | Zendy; Meng Cui | Zendy; Diomedes E. Logothetis | Zendy

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Molecular overlap in the regulation of SK channels by small molecules and phosphoinositides

Author(s) -

Miao Zhang,

Xuan-Yu Meng,

Jifang Zhang,

Meng Cui,

Diomedes E. Logothetis

Publication year - 2015

Publication title -

science advances

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 5.928

H-Index - 146

ISSN - 2375-2548

DOI - 10.1126/sciadv.1500008

Subject(s) - calmodulin , small molecule , biophysics , phosphatidylinositol , channel (broadcasting) , conductance , chemistry , microbiology and biotechnology , biology , biochemistry , signal transduction , physics , computer science , enzyme , telecommunications , condensed matter physics

Phosphatidylinositol 4,5-bisphosphate (PIP2) directly interacts with the small-conductance Ca2+-activated K+ 2-a (SK2-a) channel/calmodulin complex, serving as a critical element in the regulation of channel activity. We report that changes of protein conformation in close proximity to the PIP2 binding site induced by a small-molecule SK channel modulator, NS309, can effectively enhance the interaction between the protein and PIP2 to potentiate channel activity. This novel modulation of PIP2 sensitivity by small-molecule drugs is likely not to be limited in its application to SK channels, representing an intriguing strategy to develop drugs controlling the activity of the large number of PIP2-dependent proteins.

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