Showing papers by "Michel Bouvier published in 1997"
TL;DR: A patient with Cushing's syndrome and corticotropin-independent bilateral adrenal hyperplasia is described in whom endogenous catecholamines, acting through an ectopic adrenal β-adrenergic receptor, stimulated cortisol secretion; the hyperadrenocorticism was inhibited by β-blockade.
Abstract: Most patients with corticotropin-independent Cushing's syndrome have an adrenal adenoma or carcinoma,1 but a few have bilateral adrenal hyperplasia. Three patients with Cushing's syndrome and corticotropin-independent bilateral adrenal hyperplasia2–4 and two patients with adrenal adenomas5,6 in whom food stimulated cortisol secretion have been described; the abnormal adrenal tissues in these patients aberrantly overexpressed receptors for gastric inhibitory polypeptide.6,7 We describe a patient with Cushing's syndrome and corticotropin-independent bilateral adrenal hyperplasia in whom endogenous catecholamines, acting through an ectopic adrenal β-adrenergic receptor, stimulated cortisol secretion; the hyperadrenocorticism was inhibited by β-blockade. Case Report A 56-year-old man presented with . . .
200 citations
TL;DR: It is shown that vire particles released from Sf9 cells infected with a recombinant baculovirus coding for the human β2-adrenergic receptor (β2AR) cDNA contain glycosylated and biologically active β2AR.
Abstract: Expression in baculovirus-infected insect cells allows sufficient production of G-protein coupled receptor for structural studies. An important drawback of this expression system comes from the presence of unprocessed and biologically inactive receptors that have to be eliminated during receptor purification steps. We show that viral particles released from Sf9 cells infected with a recombinant baculovirus coding for the human beta 2-adrenergic receptor (beta 2AR) cDNA contain glycosylated and biologically active beta 2AR. In addition, post-translational modifications known to modulate receptor activity were found to occur in these particles.
95 citations
TL;DR: Chronic β-blockade increases skeletal muscle β-adrenergic-receptor density and enhances contractile force strength in mice by up to 50% and reduces the chance of injury.
Abstract: Murphy, Rene J. L., Phillip F. Gardiner, Guy Rousseau, Michel Bouvier, and Louise Beliveau. Chronic β-blockade increases skeletal muscle β-adrenergic-receptor density and enhances contractile force...
17 citations
TL;DR: Data suggest that the early development of hereditary cardiomyopathy in hamsters is accompanied by a specific overexpression of the α 1A - and α 1B -ARs, which could contribute to eliciting coronary microspasms and participating in the development of focal necrotic lesions that are characteristic of the hamsterCardiomyopathic model.
12 citations
TL;DR: Although different molecular events are involved in the desensitization evoked by different levels of stimulation, its phenotypic expression can be qualitatively identical in cells expressing a relatively small number of receptors.
10 citations
Patent•
01 Jul 1997
TL;DR: In this article, short peptides of a preferred length of up to about 15-20 amino acid residues are modeled on transmembrane domains of G-protein-coupled receptors, whose activities are affected by the formation of oligomers.
Abstract: This invention relates to peptides and peptidomimetic compounds that modulate the function of G-protein-coupled receptors by affecting the ratio of receptor monomer to homo-oligomeric forms. Novel short peptides of a preferred length of up to about 15-20 amino acid residues are modeled on transmembrane domains of G-protein-coupled receptors, whose activities are affected by the formation of oligomers. These novel peptides and peptidomimetic compounds can be used to selectively affect the activity of G-protein-coupling receptors, thereby functioning as potential therapeutic drugs, etc.. A preferred peptide is GIIMGTFTLCWLPFFIVNIV.
10 citations
TL;DR: Because β ARs represent important pharmacological targets in the treatment of hypertension, angina pectoris, arrhythmias, heart failure, and obesity, analysis of the mechanisms leading to alterations of β AR responsiveness is essential, because it may lead to the identification of new means to normalize the receptor function.
Abstract: Publisher Summary One of the most fascinating features of β -adrenergic receptors ( β ARs) signaling systems is their high degree of plasticity. This permits the cell to adapt to its environment and may play a major role in the sorting and integration of the information detected at the receptor levels. β ARs, which belong to the family of G-protein-coupled receptors, are the target of various regulatory processes. In particular, negative regulation and desensitization in response to sustained activation have been well researched. Changes in the responsiveness of β ARs are believed to contribute to the phenomenon of habituation and withdrawal syndrome associated with the use of β -adrenergic agonists and antagonists, respectively. Because β ARs represent important pharmacological targets in the treatment of hypertension, angina pectoris, arrhythmias, heart failure, and obesity, analysis of the mechanisms leading to alterations of β AR responsiveness is essential, because it may lead to the identification of new means to normalize the receptor function. Recent evidence suggests subtype-specific signaling between β 1 AR and β 2 AR. Indeed, although convincing data show that, as β 1 AR, β 2 AR can promote positive chronotropic and inotropic responses in human ventricle, discrepancies between the efficacy of β 2 AR to stimulate adenylyl cyclase and to modulate contractile function have raised questions regarding the precise relation between cyclic adenosine monophosphate (cAMP) production and cardiac regulation.
7 citations
Patent•
30 Jun 1997
TL;DR: In this paper, the authors proposed a new method of assaying compounds that modulate the activity of G protein-coupled receptors based on measurement of changes in the relative proportions of monomeric to multimeric receptor polypeptides.
Abstract: This invention is a new method of assaying compounds that modulate the activity of G protein-coupled receptors based on measurement of changes in the relative proportions of monomeric to multimeric receptor polypeptides. More specifically, techniques are described herein which permit the prediction of the pharmacological efficacy of drug candidates based solely on the ability of the candidate compounds to alter the ratio of receptor monomer to homo-oligomeric forms of the receptor. This method provides a novel means of assaying compounds as potential therapeutic drugs at G protein-coupled receptors which is greatly simplified and more generally applicable than existing methods.
6 citations
1 citations
Patent•
01 Jul 1997
TL;DR: Les peptides et composes peptidomimetiques de l'invention peuvent s'utiliser pour affecter de facon selective l'activite des recepteurs couples a la proteine G, ce qui fait qu'ils sont capables d'agir, notamment, comme d'eventuels medicaments.
Abstract: La presente invention concerne des peptides et de composes peptidomimetiques qui modulent la fonction des recepteurs couples a la proteine G en affectant le rapport entre les formes monomeres et homo-oligomeres du recepteur. Les peptides courts de l'invention, qui ont une longueur atteignant de preference environ 15 a 20 radicaux d'acides amines sont modeles sur les domaines transmembranaires des recepteurs couples a la proteine G, recepteurs dont les activites sont affectees par la formation des oligomeres. Les peptides et composes peptidomimetiques de l'invention peuvent s'utiliser pour affecter de facon selective l'activite des recepteurs couples a la proteine G, ce qui fait qu'ils sont capables d'agir, notamment, comme d'eventuels medicaments. Un peptide prefere est GIIMGTFTLCWLPFFIVNIV.