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Vol. 56, Issue 2, 308-315, August 1999
Laboratoire de Biophysique Moleculaire et Celluraire,
Département de Biologie Moléculaire et Structurale,
Commissariat à l'Energie Atomique, Grenoble, France
ATP-sensitive K+ (KATP) channels are a
complex of an ATP-binding cassette transporter, the sulfonylurea
receptor (SUR), and an inward rectifier K+ channel subunit,
Kir6.2. The diverse pharmacological responsiveness of KATP
channels from various tissues are thought to arise from distinct SUR
isoforms. Thus, when assembled with Kir6.2, the pancreatic 
cell
isoform SUR1 is activated by the hyperglycemic drug diazoxide but not
by hypotensive drugs like cromakalim, whereas the cardiac muscle
isoform SUR2A is activated by cromakalim and not by diazoxide. We
exploited these differences between SUR1 and SUR2A to pursue a chimeric
approach designed to identify the structural determinants of SUR
involved in the pharmacological activation of KATP
channels. Wild-type and chimeric SUR were coexpressed with Kir6.2 in
Xenopus oocytes, and we studied the resulting channels
with the patch-clamp technique in the excised inside-out configuration.
The third transmembrane domain of SUR is found to be an important
determinant of the response to cromakalim, which possibly harbors at
least part of its binding site. Contrary to expectations, diazoxide
sensitivity could not be linked specifically to the carboxyl-terminal
end (nucleotide-binding domain 2) of SUR but appeared to involve
complex allosteric interactions between transmembrane and
nucleotide-binding domains. In addition to providing direct evidence
for the structure-function relationship governing KATP
channel activation by potassium channel-opening drugs, a family of
drugs of the highest therapeutic interest, these findings delineate the
determinants of ligand specificity within the modular ATP-binding
cassette-transporter architecture of SUR.
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