The family of G‐protein‐coupled receptors

Strader, Catherine D.; Fong, Tung M.; Graziano, Michael P.; Tota, Michael R.

doi:10.1096/fasebj.9.9.7601339

Cited by 339 publications

(267 citation statements)

References 51 publications

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“…Serotonin (5-hydroxytryptamine or 5-HT) receptors are members of a superfamily of seven transmembrane domain receptors (Strader et al, 1995) that couple to GTP-binding regulatory proteins (G-proteins). Serotonergic signaling appears to play a key role in the generation and modulation of various cognitive and behavioral functions including sleep, mood, pain, addiction, locomotion, sexual activity, depression, anxiety, alcohol abuse, aggression, and learning (Artigas et al, 1996;Ramboz et al, 1998).…”

Section: Introductionmentioning

confidence: 99%

Solubilization of Serotonin_1AReceptors Heterologously Expressed in Chinese Hamster Ovary Cells

2004

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SUMMARY1. The serotonin 1A (5-HT 1A ) receptors are members of a superfamily of seven transmembrane domain receptors that couple to G-proteins. They appear to be involved in various behavioral and cognitive functions.2. We report here, for the first time, the solubilization of 5-HT 1A receptors stably expressed in Chinese Hamster Ovary (CHO) cells using the zwitterionic detergent CHAPS in presence of NaCl followed by polyethylene glycol (PEG) precipitation. We show by ligand-binding assay that the 5-HT 1A receptor solubilized this way is functionally active. We have optimized the efficiency of solubilization with respect to total protein and NaCl concentration.3. Our results show that careful control of salt and protein concentration is crucial in optimal solubilization of membrane receptors heterologously expressed in cells in culture. The effective solubilization of important neurotransmitter receptors such as 5-HT 1A receptors which are present in very low amounts in the native tissue may represent an important step in characterizing membrane receptors expressed in mammalian cells in culture.

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Section: Introductionmentioning

confidence: 99%

Solubilization of Serotonin_1AReceptors Heterologously Expressed in Chinese Hamster Ovary Cells

2004

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“…These ion channels belong to the superfamily of four transmembrane domain receptors (Ortells and Lunt, 1995). However, the role of the other important class of membrane receptors, the seven transmembrane domain G-protein-coupled receptors (GPCRs) which includes several neurotransmitter receptors (Bikker et al, 1998;Pierce et al, 2002;Strader et al, 1995), in the action of anesthetics is an emerging area of research. Inhibition of G-protein signaling pathways is thought to be an important component of the action of both general (Pentyala et al, 1999) and local (Xiong et al, 1999;Zhou et al, 2001) anesthetics.…”

Section: Introductionmentioning

confidence: 99%

“…Serotonin receptors are members of a superfamily of seven transmembrane domain receptors (Pierce et al, 2002;Strader et al, 1995) that couple to GTP-binding regulatory proteins (G-proteins). Serotonergic signaling appears to play a key role in the generation and modulation of various cognitive and behavioral functions (Heath and Hen, 1995).…”

Section: Introductionmentioning

confidence: 99%

Interaction of Serotonin_1AReceptors from Bovine Hippocampus with Tertiary Amine Local Anesthetics

Kalipatnapu

Chattopadhyay

2004

Cell Mol Neurobiol

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SUMMARY1. We have examined the interaction of tertiary amine local anesthetics with the bovine hippocampal serotonin 1A (5-HT 1A ) receptor, an important member of the G-proteincoupled receptor superfamily.2. The local anesthetics inhibit specific agonist and antagonist binding to the 5-HT 1A receptor at a clinically relevant concentration range of the anesthetics. This is accompanied by a concomitant reduction in the binding affinity of the 5-HT 1A receptor to the agonist. Interestingly, the extent of G-protein coupling of the receptor is reduced in the presence of the local anesthetics.3. Fluorescence polarization measurements using depth-dependent fluorescent probes show that procaine and lidocaine do not show any significant change in membrane fluidity. On the other hand, tetracaine and dibucaine were found to alter fluidity of the membrane as indicated by a fluorescent probe which monitors the headgroup region of the membrane.4. The local anesthetics showed inhibition of agonist binding to the 5-HT 1A receptor in membranes depleted of cholesterol more or less to the same extent as that of control membranes in all cases. This suggests that the inhibition in ligand binding to the 5-HT 1A receptor brought about by local anesthetics is independent of the membrane cholesterol content.5. Our results on the effects of the local anesthetics on the ligand binding and G-protein coupling of the 5-HT 1A receptor support the possibility that G-protein-coupled receptors could be involved in the action of local anesthetics.

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“…G protein-coupled receptors mediate cellular responses elicited by a variety of extracellular stimuli ranging from photons, odorants and ions to neurotransmitters, regulatory peptides and bioactive lipids [1,2]. Molecular cloning of these seventransmembrane-domain receptors has revealed a large gene family with many common structural features [3][4][5].…”

Section: Introductionmentioning

confidence: 99%

Cloning, sequencing and tissue distribution of two related G protein‐coupled receptor candidates expressed prominently in human lung tissue

Tsai

Goetzl

1995

FEBS Letters

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A novel G protein-coupled receptor, named GPR12A, was cloned by a PCR strategy using degenerate primers designed from sequences conserved among receptors for inflammatory mediators. Screening of a human lung cDNA library with GPR12A as a probe also identified a closely-related cDNA (GPR6C.1) that has been previously reported as GPR4 [13]. GPR12A and GPR6C.1 are 46.1% identical in amino acid sequence, but are less than 33% identical to any other known receptors. Northern analysis revealed that they are expressed prominently in the lung. Although the ligands for GPR12A and GPR6C.1 are unknown, their similarity suggests that they are receptors for ligands of similar or identical chemical nature.

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The family of G‐protein‐coupled receptors

Cited by 339 publications

References 51 publications

Solubilization of Serotonin_1AReceptors Heterologously Expressed in Chinese Hamster Ovary Cells

Solubilization of Serotonin_1AReceptors Heterologously Expressed in Chinese Hamster Ovary Cells

Interaction of Serotonin_1AReceptors from Bovine Hippocampus with Tertiary Amine Local Anesthetics

Cloning, sequencing and tissue distribution of two related G protein‐coupled receptor candidates expressed prominently in human lung tissue

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The family of G‐protein‐coupled receptors

Cited by 339 publications

References 51 publications

Solubilization of Serotonin1AReceptors Heterologously Expressed in Chinese Hamster Ovary Cells

Solubilization of Serotonin1AReceptors Heterologously Expressed in Chinese Hamster Ovary Cells

Interaction of Serotonin1AReceptors from Bovine Hippocampus with Tertiary Amine Local Anesthetics

Cloning, sequencing and tissue distribution of two related G protein‐coupled receptor candidates expressed prominently in human lung tissue

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Solubilization of Serotonin_1AReceptors Heterologously Expressed in Chinese Hamster Ovary Cells

Solubilization of Serotonin_1AReceptors Heterologously Expressed in Chinese Hamster Ovary Cells

Interaction of Serotonin_1AReceptors from Bovine Hippocampus with Tertiary Amine Local Anesthetics