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Discovery and Pharmacological Evaluation of Growth Hormone Secretagogue Receptor Antagonists

Journal of Medicinal Chemistry, 2006
The 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
openaire   +3 more sources

Distribution and regulation of chicken growth hormone secretagogue receptor isoforms

General and Comparative Endocrinology, 2003
Chicken 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
openaire   +3 more sources

Structure-function studies on the new growth hormone-releasing peptide, ghrelin: minimal sequence of ghrelin necessary for activation of growth hormone secretagogue receptor 1a.

Journal of Medicinal Chemistry, 2000
The recently discovered growth hormone secretagogue, ghrelin, is a potent agonist at the human growth hormone secretagogue receptor 1a (hGHSR1a). To elucidate structural features of this peptide necessary for efficient binding to and activation of the ...
Maria A. Bednarek   +9 more
semanticscholar   +1 more source

Thyroid Hormones Regulate Pituitary Growth Hormone Secretagogue Receptor Gene Expression

Journal of Neuroendocrinology, 2001
AbstractThyroid 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
openaire   +3 more sources

Glucocorticoids Regulate Pituitary Growth Hormone Secretagogue Receptor Gene Expression

Journal of Neuroendocrinology, 2000
AbstractGlucocorticoids 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
openaire   +3 more sources

Ghrelin- and growth hormone secretagogue receptor-immunoreactive cells in Xenopus pancreas

Regulatory Peptides, 2011
Ghrelin and its receptor, growth hormone secretagogue receptor (GHS-R), are produced by various cell types and affect feeding behavior, metabolic regulation, and energy balance. In the mammalian pancreas, the types of endocrine cells immunoreactive for ghrelin vary. Further, no study has clarified the type of endocrine cells producing ghrelin and GHS-R
Hirohumi Suzuki, Toshiharu Yamamoto
openaire   +3 more sources

Glucocorticoid regulation of growth hormone (GH) secretagogue-induced growth responses and GH secretagogue receptor expression in the rat

Growth Hormone & IGF Research, 2000
Synthetic GH-releasing peptides such as GHRP-6 are potent GH secretagogues (GHSs) in several species, but attempts to stimulate growth by continuous GHS exposure have had limited success. GHSs also release ACTH and adrenal steroids. Since glucocorticoid excess is associated with poor linear growth, stimulation of the hypothalamo-pituitary-adrenal (HPA)
G. B. Thomas   +3 more
openaire   +3 more sources

Circulating ghrelin crosses the blood-cerebrospinal fluid barrier via growth hormone secretagogue receptor dependent and independent mechanisms

Molecular and Cellular Endocrinology, 2021
Maia Uriarte   +11 more
semanticscholar   +1 more source

The prospects of antagonizing the growth hormone secretagogue receptor to treat obesity

Expert Opinion on Therapeutic Patents, 2008
Background: Ghrelin is an endogenous ligand of the growth hormone secretagogue receptor (GHS-R) that functions as a short-term meal initiator and a long-term energy balance regulator. Antagonizing GHS-R could be a method to treat obesity. Objective: To review the published in vivo characterization of GHS-R antagonists between 2005 and 2008 and evaluate
Bo Liu, Hongyu Zhao, Michael D. Serby
openaire   +2 more sources

Role of the Growth Hormone Secretagogue Receptor in the Central Nervous System

2002
Aging is accompanied by a decline in the amplitude of the release of hormones, neurotransmitters and neuropeptides. These changes are associated with alterations in metabolism resulting in increases in deposition of visceral fat at the expense of muscle.
L. Betancourt, R. G. Smith, Yuxiang Sun
openaire   +2 more sources

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