Journal ArticleDOI
A Receptor in Pituitary and Hypothalamus That Functions in Growth Hormone Release
Andrew D. Howard,Scott D. Feighner,Doris F. Cully,Joseph P. Arena,Paul A. Liberator,Charles Rosenblum,Michel J. Hamelin,Donna L. Hreniuk,Oksana C. Palyha,Jennifer W. Anderson,Philip S. Paress,Carmen Diaz,Michael Chou,Ken K. Liu,Karen K. McKee,Sheng-Shung Pong,Lee-Yuh Chaung,Alex Elbrecht,Mike Dashkevicz,Robert P. Heavens,Michael Rigby,Dalip J. S. Sirinathsinghji,Dennis C. Dean,David G. Melillo,Arthur A. Patchett,Ravi P. Nargund,Patrick R. Griffin,Julie A. DeMartino,Sunil Gupta,James M. Schaeffer,Roy G. Smith,Lex H.T. Van der Ploeg +31 more
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TLDR
A heterotrimeric GTP-binding protein (G protein)-coupled receptor (GPC-R) of the pituitary and arcuate ventro-medial and infundibular hypothalamus of swine and humans was cloned and was shown to be the target of the GHSs.Abstract:
Small synthetic molecules termed growth hormone secretagogues (GHSs) act on the pituitary gland and the hypothalamus to stimulate and amplify pulsatile growth hormone (GH) release. A heterotrimeric GTP-binding protein (G protein)-coupled receptor (GPC-R) of the pituitary and arcuate ventro-medial and infundibular hypothalamus of swine and humans was cloned and was shown to be the target of the GHSs. On the basis of its pharmacological and molecular characterization, this GPC-R defines a neuroendocrine pathway for the control of pulsatile GH release and supports the notion that the GHSs mimic an undiscovered hormone.read more
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Peripheral ghrelin deepens torpor bouts in mice through the arcuate nucleus neuropeptide Y signaling pathway
TL;DR: Data suggest that ghrelin's actions on torpor are mediated via NPY neurons within the ARC, one of the major pathways that regulate food intake reside in the ARC.
Journal ArticleDOI
The truncated ghrelin receptor polypeptide (GHS-R1b) is localized in the endoplasmic reticulum where it forms heterodimers with ghrelin receptors (GHS-R1a) to attenuate their cell surface expression.
TL;DR: It is suggested that ghrelin receptors can be retained in the endoplasmic reticulum by heterodimerization with GHS-R1b, and constitutive activation of phospholipase C is attenuated due to decreased cell surface expression of gh Relin receptors.
Journal ArticleDOI
N-Terminal Liver-Expressed Antimicrobial Peptide 2 (LEAP2) Region Exhibits Inverse Agonist Activity toward the Ghrelin Receptor.
Céline M'Kadmi,Agustina Cabral,Franco Barrile,Julien Giribaldi,Sonia Cantel,Marjorie Damian,Sophie Mary,Séverine Denoyelle,Sébastien Dutertre,Sylvie Péraldi-Roux,Jérémie Neasta,Catherine Oiry,Jean-Louis Banères,Jacky Marie,Mario Perello,Jean-Alain Fehrentz +15 more
TL;DR: It is found that both LEAP2 and its N-terminal part behave as inverse agonists of GHSR and as competitive antagonists of ghrelin-induced inositol phosphate production and calcium mobilization.
Journal ArticleDOI
Hedonic Eating and the "Delicious Circle": From Lipid-Derived Mediators to Brain Dopamine and Back.
TL;DR: A pivotal role is suggested for endocannabinoids in food reward processing within the lateral hypothalamus, and for orexin neurons to integrate endocrine signals with food reinforcement and hedonic eating in order to avoid compulsive eating.
Journal ArticleDOI
Hormonal control of T-cell development in health and disease.
TL;DR: The accumulating data that shows the thymus gland is under complex and multifaceted hormonal control that affects the process of T-cell development in health and disease is discussed.
References
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Journal ArticleDOI
Effects of Human Growth Hormone in Men over 60 Years Old
Daniel Rudman,Axel G. Feller,Hoskote S. Nagraj,Gregory A. Gergans,Pardee Y. Lalitha,Allen Fred Goldberg,Robert A. Schlenker,Lester Cohn,Inge W. Rudman,Dale E. Mattson +9 more
TL;DR: Diminished secretion of growth hormone is responsible in part for the decrease of lean body mass, the expansion of adipose-tissue mass, and the thinning of the skin that occur in old age.
Journal ArticleDOI
On the in vitro and in vivo activity of a new synthetic hexapeptide that acts on the pituitary to specifically release growth hormone
TL;DR: [His1,Lys6] GHRP may be a valuable peptide for investigating the function of the pituitary somatotrophs and has the potential for increasing BW gain of a variety of normal animals by inducing GH release via a direct pituitsary site of action.
Journal ArticleDOI
A versatile in vivo and in vitro eukaryotic expression vector for protein engineering
TL;DR: The pSG5 vector as mentioned in this paper was constructed by combining the eukaryotic expression vector, pKCR2, and the high copy plasmid vector Bluescribe Ml3+ (Stratagene).
Journal ArticleDOI
Expression cloning of a human B1 bradykinin receptor.
John G. Menke,Joseph A. Borkowski,Kathleen K. Bierilo,Tanya MacNeil,Amanda W. Derrick,K.A. Schneck,Richard W. Ransom,Catherine D. Strader,David L. Linemeyer,J.F. Hess +9 more
TL;DR: The availability of both the cloned human B1 and B2 bradykinin receptors should allow the elucidation of the relative contributions of these two receptor subtypes in acute and chronic inflammatory processes.
Journal ArticleDOI
A nonpeptidyl growth hormone secretagogue
Roy G. Smith,Kang Cheng,William R. Schoen,Sheng-Shung Pong,Gerard J. Hickey,Tom Jacks,B. Butler,Wanda W.-S. Chan,L.-Y. Chaung,F Judith +9 more
TL;DR: The mechanism of action of L-692,429 and studies with peptidyl and nonpeptidyl antagonists suggest that this molecule is a mimic of the growth hormone-releasing hexapeptide His-D-Trp-Ala-Tr phe-Phe-Lys-NH2 (GHRP-6).