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Literature DB >> 9029481

Constitutively active G protein-coupled receptors: potential mechanisms of receptor activation.

Abstract

Mutations of G protein-coupled receptors can increase their constitutive (agonist-independent) activity. Some of these mutations have been artificially introduced by site-directed mutagenesis, others occur spontaneously in human diseases. The analysis of the constitutively active G protein-coupled receptors has provided important informations about the molecular mechanisms underlying receptor activation and drug action.

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Year: 1997 PMID： 9029481 DOI： 10.3109/10799899709036594

Source DB: PubMed Journal: J Recept Signal Transduct Res ISSN： 1079-9893 Impact factor: 2.092

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Cited

15 in total

1. How activated receptors couple to G proteins.

Authors: H E Hamm
Journal: Proc Natl Acad Sci U S A Date: 2001-04-24 Impact factor: 11.205

2. Systematic identification of mutations that constitutively activate the angiotensin II type 1A receptor by screening a randomly mutated cDNA library with an original pharmacological bioassay.

Authors: C Parnot; S Bardin; S Miserey-Lenkei; D Guedin; P Corvol; E Clauser
Journal: Proc Natl Acad Sci U S A Date: 2000-06-20 Impact factor: 11.205

3. Detection of receptor ligands by monitoring selective stabilization of a Renilla luciferase-tagged, constitutively active mutant, G-protein-coupled receptor.

Authors: D Ramsay; N Bevan; S Rees; G Milligan
Journal: Br J Pharmacol Date: 2001-05 Impact factor: 8.739

4. Common structural requirements for heptahelical domain function in class A and class C G protein-coupled receptors.

Authors: Virginie Binet; Béatrice Duthey; Jennifer Lecaillon; Claire Vol; Julie Quoyer; Gilles Labesse; Jean-Philippe Pin; Laurent Prézeau
Journal: J Biol Chem Date: 2007-02-19 Impact factor: 5.157

5. The effect of site-directed mutagenesis of two transmembrane serine residues on agonist-specific coupling of a cloned human alpha2A-adrenoceptor to adenylyl cyclase.

Authors: J E Rudling; K Kennedy; P D Evans
Journal: Br J Pharmacol Date: 1999-06 Impact factor: 8.739

Constitutively active G protein-coupled receptors: potential mechanisms of receptor activation.

1. How activated receptors couple to G proteins.

2. Systematic identification of mutations that constitutively activate the angiotensin II type 1A receptor by screening a randomly mutated cDNA library with an original pharmacological bioassay.

3. Detection of receptor ligands by monitoring selective stabilization of a Renilla luciferase-tagged, constitutively active mutant, G-protein-coupled receptor.

4. Common structural requirements for heptahelical domain function in class A and class C G protein-coupled receptors.

5. The effect of site-directed mutagenesis of two transmembrane serine residues on agonist-specific coupling of a cloned human alpha2A-adrenoceptor to adenylyl cyclase.

6. Constitutive activation of the neurotensin receptor 1 by mutation of Phe(358) in Helix seven.

7. A constitutively active G-protein-coupled receptor causes mating self-compatibility in the mushroom Coprinus.

8. Dynamics of heme complexed with human serum albumin: a theoretical approach.

9. Molecular modeling of the human vasopressin V2 receptor/agonist complex.

10. Regulated and constitutive activation of specific signalling pathways by the human S1P5 receptor.