Methods and protocols of modern solid phase peptide synthesis
Essential protocols for the synthesis of fully deprotected peptides are presented including resin handling, coupling, capping, Fmoc-deprotection, final cleavage and disulfide bridge formation.
Toward potent ghrelin receptor ligands based on trisubstituted 1,2,4-triazole structure. 2. Synthesis and pharmacological in vitro and in vivo evaluations.
- A. Moulin, Luc Demange, Jean Martinez
- Biology, ChemistryJournal of Medicinal Chemistry
- 10 October 2007
It is shown that it is possible to modulate food intake without altering growth hormone secretion, using ghrelin receptor ligands based on the trisubstituted 1,2,4-triazole structure.
Rapid sensing of circulating ghrelin by hypothalamic appetite-modifying neurons
- M. Schaeffer, F. Langlet, P. Mollard
- BiologyProceedings of the National Academy of Sciences
- 7 January 2013
In vivo multiphoton microscopy is used to demonstrate that circulating ghrelin, a versatile regulator of energy expenditure and feeding behavior, rapidly binds neurons in the vicinity of fenestrated capillaries, and that the number of labeled cell bodies varies with feeding status.
N-Terminal Liver-Expressed Antimicrobial Peptide 2 (LEAP2) Region Exhibits Inverse Agonist Activity toward the Ghrelin Receptor.
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.
Ligands and signaling proteins govern the conformational landscape explored by a G protein-coupled receptor
- S. Mary, Marjorie Damian, J. Banères
- Biology, ChemistryProceedings of the National Academy of Sciences
- 9 May 2012
It is demonstrated that ligand efficacy and functional selectivity are directly related to different receptor conformations, and a modulation of a GPCR conformational landscape by pharmacologically distinct ligands and effectors provides insights into the structural bases that decisively affect ligand effectiveness and subsequent biological responses.
Ghrelin knockout mice show decreased voluntary alcohol consumption and reduced ethanol-induced conditioned place preference
High Constitutive Activity Is an Intrinsic Feature of Ghrelin Receptor Protein
This is the first direct evidence for the high constitutive activity of the ghrelin receptor being an intrinsic property of the protein rather than the result of influence of its cellular environment, as assessed through guanosine 5′-O-(thiotriphosphate) binding experiments.
Palatability Can Drive Feeding Independent of AgRP Neurons.
Detergent-free Isolation of Functional G Protein-Coupled Receptors into Nanometric Lipid Particles.
The potential of styrene-maleic stabilized lipid discs for analyzing the molecular bases of GPCR-mediated signaling in a well-controlled membrane-like environment is highlighted.
Melanin-concentrating hormone binding sites in human SVK14 keratinocytes.
- J. Burgaud, R. Poosti, J. Fehrentz, J. Martinez, J. Nahon
- Biology, ChemistryBiochemical and Biophysical Research…
- 29 December 1997
The widespread expression of MCH binding sites on mammalian cells, particularly on skin carcinoma cells is revealed, however, the low affinity of these sites for the native MCH and MCH-related peptides as well as competitivity with ANP and CNP indicates that further biochemical and functional characterizations are needed to validate them as genuine physiological MCH receptors.