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- Title
A bifunctional Gα<sub>i</sub>/Gα<sub>s</sub> modulatory peptide that attenuates adenylyl cyclase activity
- Authors
Johnston, Christopher A.; Ramer, J. Kevin; Blaesius, Rainer; Fredericks, Zoey; Watts, Val J.; Siderovski, David P.
- Abstract
Abstract: Signaling via G-protein coupled receptors is initiated by receptor-catalyzed nucleotide exchange on Gα subunits normally bound to GDP and Gβγ. Activated Gα·GTP then regulates effectors such as adenylyl cyclase. Except for Gβγ, no known regulators bind the adenylyl cyclase-stimulatory subunit Gαs in its GDP-bound state. We recently described a peptide, KB-752, that binds and enhances the nucleotide exchange rate of the adenylyl cyclase-inhibitory subunit Gαi. Herein, we report that KB-752 binds Gαs ·GDP yet slows its rate of nucleotide exchange. KB-752 inhibits GTPγS-stimulated adenylyl cyclase activity in cell membranes, reflecting its opposing effects on nucleotide exchange by Gαi and Gαs.
- Subjects
ADENYLATE cyclase; BIOSENSORS; MICROBIAL genetics; CYCLIC adenylic acid
- Publication
FEBS Letters, 2005, Vol 579, Issue 25, p5746
- ISSN
0014-5793
- Publication type
Article
- DOI
10.1016/j.febslet.2005.09.059