Showing papers by "ACADIA Pharmaceuticals Inc. published in 1998"
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TL;DR: It is proposed that the constitutively activating face normally constrains the receptor in the “off-state,” while the other face couples G-proteins in the“on-state” and the i2 loop functions as the switch enabling G-protein activation.
133 citations
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TL;DR: Results suggest that TM6 is a switch that defines the activation state of the receptor, and that ligand interactions with TM6 stabilize the receptor in either an active or an inactive conformation.
88 citations
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TL;DR: It is proposed that the third intracellular loop of the m5 muscarinic receptor forms a G-protein coupling pocket comprised of a positively charged "lip" and a hydrophobic core and that A441 contributes to receptor affinity for G-proteins.
Abstract: Using random saturation mutagenesis, we have previously identified the amino acids K439, A440, and A441 in the C-terminus of the third intracellular loop (Ci3) of the m5 muscarinic receptor as bein...
40 citations
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TL;DR: Results demonstrate that rac mediates the proliferative effects of G-protein coupled receptors through a pathway that is distinct from the proliferatives signaling pathway utilized by tyrosine kinase linked and JAK-linked receptors.
Abstract: The ras-related GTPase rac1 regulates a proliferative pathway selectively utilized by G-protein coupled receptors
28 citations