MgADP Antagonism to Mg2+-independent ATP Binding of the Sulfonylurea Receptor SUR1

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Population

In vitro model of the sulfonylurea receptor SUR1 (pancreatic beta-cell KATP channel subunit)

Design

Preclinical

Authors

Discussion

Refines SUR1 nucleotide-binding mechanisms in vitro; leaves open translation to KATP-targeted therapies in patients.

Population

In vitro model of the sulfonylurea receptor SUR1 (pancreatic beta-cell KATP channel subunit)

Intervention

Point mutations into the core consensus sequence of the Walker A or B motif of each nucleotide-binding fold (NBF) of SUR1

Outcome

ATP binding and ADP or MgADP antagonism

SUR1 strongly binds ATP at NBF1 even in the absence of Mg2+, and MgADP antagonizes this binding through NBF2.

Ueda et al. (1997) studied this question.

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