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A bifunctional Galphai/Galphas modulatory peptide that attenuates adenylyl cyclase activity.
- Source :
-
FEBS letters [FEBS Lett] 2005 Oct 24; Vol. 579 (25), pp. 5746-50. - Publication Year :
- 2005
-
Abstract
- Signaling via G-protein coupled receptors is initiated by receptor-catalyzed nucleotide exchange on Galpha subunits normally bound to GDP and Gbetagamma. Activated Galpha . GTP then regulates effectors such as adenylyl cyclase. Except for Gbetagamma, no known regulators bind the adenylyl cyclase-stimulatory subunit Galphas 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 Galpha(i). Herein, we report that KB-752 binds Galpha(s) . GDP yet slows its rate of nucleotide exchange. KB-752 inhibits GTPgammaS-stimulated adenylyl cyclase activity in cell membranes, reflecting its opposing effects on nucleotide exchange by Galpha(i) and Galpha(s).
Details
- Language :
- English
- ISSN :
- 0014-5793
- Volume :
- 579
- Issue :
- 25
- Database :
- MEDLINE
- Journal :
- FEBS letters
- Publication Type :
- Academic Journal
- Accession number :
- 16225870
- Full Text :
- https://doi.org/10.1016/j.febslet.2005.09.059