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Chemical control of metabolically-engineered voltage-gated K+ channels.

Abstract：

:Metabolic oligosaccharide engineering is a powerful approach for installing unnatural glycans with unique functional groups into the glycocalyx of living cells and animals. Using this approach, we showed that K(+) channel complexes decorated with thiol-containing sialic acids were irreversibly inhibited with scorpion toxins bearing a pendant maleimide group. Irreversible inhibition required a glycosylated K(+) channel subunit and was completely reversible with mild reductant when the tether connecting the toxin to the maleimide contained a disulfide bond. Cleavage of the disulfide bond not only restored function, but delivered a biotin moiety to the modified K(+) channel subunit, providing a novel approach for preferentially labeling wild type K(+) channel complexes functioning in cells.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Hua Z,Lvov A,Morin TJ,Kobertz WR

doi

10.1016/j.bmcl.2011.04.099

subject

Has Abstract

pub_date

2011-09-01 00:00:00

pages

5021-4

issue

17

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)00569-5

journal_volume

21

pub_type

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