Phospholipase D activation by endogenous 5-hydroxytryptamine 2C receptors is mediated by Galpha13 and pertussis toxin-insensitive Gbetagamma subunits.
Phospholipase D activation was measured in primary cultures of rat choroid plexus epithelial cells, which endogenously express the 5-hydroxytryptamine (5-HT) 2C receptor, as well as a heterologous cell line expressing the cloned receptor. In both systems, serotonin stimulation of the 5-HT(2C) receptor activates phospholipase D in addition to phospholipase C, the traditional effector. Specific inhibitors and membrane permeable blocking peptides were used to determine which heterotrimeric G-proteins were involved. Results suggest that both alpha and free betagamma subunits from G(13) heterotrimers are responsible for phospholipase D activation.
McGrew
L
L
Department of Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232-6600, USA.
Chang
M S S
MS
Sanders-Bush
E
E
D016475:3T3 Cells; D000818:Animals; D004268:DNA-Binding Proteins / Q000378:metabolism*; D004789:Enzyme Activation; D044365:GTP-Binding Protein alpha Subunits, G12-G13; D051379:Mice; D037342:Pertussis Toxin / Q000494:pharmacology; D010739:Phospholipase D / Q000378:metabolism*; D021122:Protein Subunits / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley; D044405:Receptor, Serotonin, 5-HT2C; D011985:Receptors, Serotonin / Q000378:metabolism*; D012701:Serotonin / Q000737:chemistry / Q000378:metabolism; D015398:Signal Transduction / Q000502:physiology*; D010738:Type C Phospholipases; D020741:rho GTP-Binding Proteins / Q000378:metabolism
D004268:DNA-Binding Proteins; D021122:Protein Subunits; D044405:Receptor, Serotonin, 5-HT2C; D011985:Receptors, Serotonin; D012701:Serotonin; D037342:Pertussis Toxin; D010738:Type C Phospholipases; D010739:Phospholipase D; D044365:GTP-Binding Protein alpha Subunits, G12-G13; D020741:rho GTP-Binding Proteins