Dexras1 blocks receptor-mediated heterologous sensitization of adenylyl cyclase 1.
作者： Chau H. Nguyen , Val J. Watts
DOI: 10.1016/J.BBRC.2005.05.041
关键词:
摘要: Abstract Dexras1/AGS1/RasD1 is a member of the Ras superfamily monomeric G proteins and has been suggested to disrupt receptor-G protein signaling. We examined ability Dexras1 modulate dopamine D2L receptor regulation adenylyl cyclase (AC) type 1 in HEK293 cells. Acute receptor-mediated inhibition A23187-stimulated AC1 activity (IC50, 4.0 ± 1.4 nM; 50 ± 3% inhibition) was not altered presence 2.4 ± 1.3 nM, 50 ± 1% inhibition); however, blocked acute activation ERK 1/2 by approximately 50%. Heterologous sensitization induced persistent receptors completely under basal conditions. The block concentration-dependent observed with nucleotide binding-deficient Dexras1G31V mutant. Sensitization Gβγ-dependent as demonstrated using C-terminus β-adrenergic kinase (βARK-ct). These data suggest that selectively regulates Gβγ signaling pathways.
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