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Methods and protocols of modern solid phase peptide synthesis
TLDR
Essential protocols for the synthesis of fully deprotected peptides are presented including resin handling, coupling, capping, Fmoc-deprotection, final cleavage and disulfide bridge formation. Expand
Toward potent ghrelin receptor ligands based on trisubstituted 1,2,4-triazole structure. 2. Synthesis and pharmacological in vitro and in vivo evaluations.
TLDR
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. Expand
Rapid sensing of circulating ghrelin by hypothalamic appetite-modifying neurons
TLDR
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. Expand
Arginine 197 of the cholecystokinin‐A receptor binding site interacts with the sulfate of the peptide agonist cholecystokinin
TLDR
Data support an interaction between Arg 197 of the CCK‐AR binding site and the sulfate of CCK, suggesting that Arg 197‐sulfate interaction regulates conformational changes of the CCP‐AR that are required for its physiological activation. Expand
Arginine 336 and Asparagine 333 of the Human Cholecystokinin-A Receptor Binding Site Interact with the Penultimate Aspartic Acid and the C-terminal Amide of Cholecystokinin*
TLDR
The identified interactions are crucial for stabilizing the high affinity phospholipase C-coupled state of the CCK-AR·CCK complex, and Arg-336 and Asn-333 are directly involved in interactions with nonpeptide antagonists SR-27,897 and L-364,718. Expand
Ligands and signaling proteins govern the conformational landscape explored by a G protein-coupled receptor
TLDR
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. Expand
Ghrelin knockout mice show decreased voluntary alcohol consumption and reduced ethanol-induced conditioned place preference
TLDR
Results suggest that ghrelin neurotransmission is necessary for the stimulatory effect of ethanol to occur, whereas lack of gh Relin leads to changes that reduce the voluntary intake as well as conditioned reward by ethanol. Expand
Melanin-concentrating hormone binding sites in human SVK14 keratinocytes.
TLDR
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. Expand
Syntheses and biological activities of potent bombesin receptor antagonists.
TLDR
Several inhibitors were able to recognize the bombesin receptor on rat pancreatic acini and antagonized bombsin stimulated amylase secretion in the nanomolar range and to inhibit [3H] thymidine incorporation in 3T3 cells with the same potency. Expand
Heterodimerization with Its Splice Variant Blocks the Ghrelin Receptor 1a in a Non-signaling Conformation
TLDR
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. Expand
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