Growth hormone secretagogue receptor antagonists
Expert Opinion on Therapeutic Patents, 2012The patent claims peptidic/nonpeptidic inhibitors of the ghrelin receptor, the growth hormone secretagogue receptor (GHSR) 1A. Among these compounds, it was disclosed that the addition in some compounds of a GlyMetAla tripeptide at the N-terminus of the ghrelin peptide agonists converts them into ghrelin receptor antagonists.
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On the use of cells or membranes for receptor binding: Growth hormone secretagogues
Analytical Biochemistry, 2010Receptor binding techniques have been widely used in different biochemical applications, with isolated membranes being the most used receptor preparation in this type of assays. In this study, intact cells were compared with isolated membranes as receptor support for radioligand receptor binding assay.
Zoran Nikolovski+4 more
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Analysis of polymorphism of growth hormone secretagogue receptor in goat
Indian Journal of Animal Research, 2018Two pairs of primers (GHSR-3, GHSR-4) were used to amplify GHSR gene of Boer goat, Yaoshan goat and black goat. Totally two mutation sites (SNP loci), G200A and T628C were detected in amplification fragments of GHSR-3 and GHSR-4 respectively. For locus G200A, allele frequencies of G and A in Yaoshan goat, Boer goat and black goat were 0.637/0.595/0.827
X. Wang+5 more
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Known and Unknown Growth Hormone Secretagogue Receptors and their Ligands
2004The discovery of ghrelin is a typical example of reverse pharmacology: first the synthetic analogues (i.e. peptidyl and non-peptidyl growth hormone secretagogues (GHS)); second the receptor; third the natural ligand for this orphan receptor, i.e. ghrelin. Ghrelin is providing new understanding about how the gastrointestinal tract and nutritional intake
MUCCIOLI, Giampiero+3 more
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Characterization of a Monoclonal Antibody Specific for the Growth Hormone Secretagogue Receptor
Monoclonal Antibodies in Immunodiagnosis and Immunotherapy, 2017Ghrelin is an orexigenic peptide hormone that primarily regulates growth hormone secretion, food intake, and energy homeostasis. It has been shown to also play a role in numerous higher brain functions, such as the regulation of inflammation and cell proliferation. Ghrelin is the endogenous ligand of the growth hormone secretagogue receptor (GHSR), a G-
K. Crotta+5 more
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Molecular characterization of chicken growth hormone secretagogue receptor gene
General and Comparative Endocrinology, 2003Synthetic growth hormone secretagogues stimulate growth hormone secretion by binding to a specific receptor, growth hormone secretagogue receptor (GHS-R). In this study, we investigated the cDNA and the genomic structure of chicken GHS-R. Chicken GHS-R gene is composed of two exons separated by an intron.
Yoshiyuki Ohta+7 more
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Discovery and Pharmacological Evaluation of Growth Hormone Secretagogue Receptor Antagonists
Journal of Medicinal Chemistry, 2006The discovery and pharmacological evaluation of potent, selective, and orally bioavailable growth hormone secretagogue receptor (GHS-R) antagonists are reported. Previously, 2,4-diaminopyrimidine-based GHS-R antagonists reported from our laboratories have been shown to be dihydrofolate reductase (DHFR) inhibitors.
Christi Kosogof+24 more
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Distribution and regulation of chicken growth hormone secretagogue receptor isoforms
General and Comparative Endocrinology, 2003Chicken ghrelin has recently been isolated as a hormone which stimulates growth hormone and corticosterone secretion in chicken. Ghrelin mediates these actions in mammals by binding to the growth hormone secretagogue receptor (GHS-R). In this study, we describe the partial cloning of two chicken GHS-R (cGHS-R) isoforms: cGHS-R1a and cGHS-R1c.
Veerle Darras+4 more
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Thyroid Hormones Regulate Pituitary Growth Hormone Secretagogue Receptor Gene Expression
Journal of Neuroendocrinology, 2001AbstractThyroid hormones regulate growth hormone (GH) secretion by actions both at the hypothalamus and at the pituitary gland. At the level of the pituitary, thyroid hormones increase GH and GH‐releasing hormone receptor (GHRH‐R) mRNA expression.
Jun Kamegai+4 more
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Glucocorticoids Regulate Pituitary Growth Hormone Secretagogue Receptor Gene Expression
Journal of Neuroendocrinology, 2000AbstractGlucocorticoids regulate growth hormone (GH) secretion by modulating both hypothalamic and pituitary function. At the level of the pituitary, glucocorticoids increase GH and GH‐releasing hormone receptor (GHRH‐R) gene expression. To test if glucocorticoids might also regulate the pituitary expression of the recently identified GH secretagogue ...
Ichiji Wakabayashi+5 more
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