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.
Original language | English |
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Pages (from-to) | 5746-5750 |
Number of pages | 5 |
Journal | FEBS Letters |
Volume | 579 |
Issue number | 25 |
DOIs | |
State | Published - 24 Oct 2005 |
Keywords
- Adenylyl cyclase
- Biosensors
- G-proteins
- Phage display
- Signal transduction
- Surface plasmon resonance