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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Journal ArticleDOI
An aromatic region to induce a switch between agonism and inverse agonism at the ghrelin receptor.
Sylvia Els,Enrico Schild,Pia Steen Petersen,Tom-Marten Kilian,Tom-Marten Kilian,Jacek Mokrosinski,Thomas M. Frimurer,Constance Chollet,Thue W. Schwartz,Birgitte Holst,Annette G. Beck-Sickinger +10 more
TL;DR: In this article, small changes in the core binding motif -wFw- of the hexapeptide KwFwLL-NH(2) can swap the peptide behavior from inverse agonism to agonism, indicating the importance of this sequence.
Journal ArticleDOI
Heterodimerization with Its Splice Variant Blocks the Ghrelin Receptor 1a in a Non-signaling Conformation A STUDY WITH A PURIFIED HETERODIMER ASSEMBLED INTO LIPID DISCS
Sophie Mary,Jean-Alain Fehrentz,Marjorie Damian,Gérald Gaibelet,Hélène Orcel,Pascal Verdié,Bernard Mouillac,Jean Martinez,Jacky Marie,Jean-Louis Banères +9 more
TL;DR: This work provides direct evidence that allosteric conformational events within dimeric assemblies can be directly responsible for modulation of signaling mediated by G protein-coupled receptors.
Journal ArticleDOI
On the central mechanism underlying ghrelin's chronic pro-obesity effects in rats: new insights from studies exploiting a potent ghrelin receptor antagonist.
Nicolas Salomé,Caroline Hansson,Magdalena Taube,L Gustafsson-Ericson,Emil Egecioglu,Linda Karlsson-Lindahl,Jean-Alain Fehrentz,Jean Martinez,Daniel Perrissoud,Suzanne L. Dickson +9 more
TL;DR: The hypothesis emerging from these data, namely that GHS‐R1A mediates the chronic effects of ghrelin on fat accumulation, at least partly independent of food intake, is discussed in light of the accompanying data regarding the hypothalamic genes coding for peptides and receptors involved in energy balance regulation, which were found to have altered expression in these studies.
Journal ArticleDOI
Hypotensive effect of des-acyl ghrelin at nucleus tractus solitarii of rat.
TL;DR: The results suggest that des-acyl ghrelin contribute to the regulation of cardiovascular control and that a receptor other than GHSR-1a exists in NTS.
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).