Search Results - "Waelbroeck, Magali"
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Ghrelin Degradation by Serum and Tissue Homogenates: Identification of the Cleavage Sites
Published in Endocrinology (Philadelphia) (01-11-2004)“…The endogenous ligand for the GH secretagogue receptor is ghrelin, a peptide recently purified from the stomach. Ghrelin is n-octanoylated on the Ser3 residue,…”
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Propiverine and metabolites: differences in binding to muscarinic receptors and in functional models of detrusor contraction
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-11-2006)“…Propiverine is a commonly used antimuscarinic drug used as therapy for symptoms of an overactive bladder. Propiverine is extensively biotransformed into…”
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Two Basic Residues of the h-VPAC1 Receptor Second Transmembrane Helix Are Essential for Ligand Binding and Signal Transduction
Published in The Journal of biological chemistry (12-01-2001)“…We mutated the vasoactive intestinal peptide (VIP) Asp3 residue and two VPAC1receptor second transmembrane helix basic residues (Arg188and Lys195). VIP had a…”
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In vitro properties of a high affinity selective antagonist of the VIP1 receptor
Published in Peptides (New York, N.Y. : 1980) (1997)“…A selective high affinity VIP1 receptor antagonist [Acetyl-His1, D-Phe2, Lys15, Arg16, Leu17] VIP(3-7)/GRF(8-27) or PG 97-269 was synthesized, by analogy with…”
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Development of high affinity selective VIP1 receptor agonists
Published in Peptides (New York, N.Y. : 1980) (1997)“…The biological effects of VIP are mediated by at least two VIP receptors: the VIP1 and the VIP2 receptors that were cloned in rat, human and mice. As the mRNA…”
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Synthesis and affinity studies of himbacine derived muscarinic receptor antagonists
Published in Bioorganic & medicinal chemistry letters (05-08-2002)“…A series of himbacine ( 1)-related analogues has been prepared featuring three different isomeric configurations with respect to the B-ring ( a, b and natural…”
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Techniques: Promiscuous Gα proteins in basic research and drug discovery
Published in Trends in pharmacological sciences (Regular ed.) (01-11-2005)“…Assay technologies that measure the activation of heterotrimeric (αβγ) G proteins by G-protein-coupled receptors (GPCRs) are well established within the…”
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Characterization of a novel VPAC1 selective agonist and identification of the receptor domains implicated in the carboxyl‐terminal peptide recognition
Published in British journal of pharmacology (01-06-2000)“…Vasoactive Intestinal Polypeptide (VIP) interacts with a high affinity to two subclasses of G protein coupled receptors named VPAC1 and VPAC2, and has a 3–10…”
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DNA immunization combined with scFv phage display identifies antagonistic GCGR specific antibodies and reveals new epitopes on the small extracellular loops
Published in mAbs (17-08-2016)“…The identification of functional monoclonal antibodies directed against G-protein coupled receptors (GPCRs) is challenging because of the membrane-embedded…”
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Analysis of the glucagon receptor first extracellular loop by the substituted cysteine accessibility method
Published in Peptides (New York, N.Y. : 1980) (01-08-2011)“…[Display omitted] ► SCAM of the first glucagon receptor extracellular loop (197–224). ► TM2 continues to position 202, TM3 from 215 ► Most side chains…”
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Synthesis and binding affinity studies of muscarinic receptor antagonists related to dehydrohimbacine
Published in ARKIVOC (03-02-2003)Get full text
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Properties of the VIP-PACAP type II receptor stably expressed in CHO cells
Published in Regulatory peptides (15-12-1994)“…The VIP receptor cloned from rat lung (VIP1 receptor from the group of the PACAP-VIP type II receptors) was inserted into a mammalian expression vector and…”
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Pharmacological discrimination between enantiomeric germanes by muscarinic receptors: a study on germanium/silicon bioisosterism
Published in Journal of organometallic chemistry (23-08-1996)“…The (hydroxymethyl)diorgano(2-piperidinoethyl)germanes rac-Ph( c-Hex)Ge(CH 2OH)CH 2CH 2NR 2 ( rac- 1a), Ph 2Ge(CH 2OH)CH 2-CH 2NR 2 ( 3a) and ( c-Hex) 2Ge(CH…”
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An alternative presentation of metabolism
Published in Biochemistry and molecular biology education (01-07-2007)“…Why should we think of enzymes as sluice gates? We are used to talk about “metabolic flux”: I should like to suggest that we should indeed envision metabolism…”
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An alternative presentation of metabolism: Enzyme-catalyzed reactions can be viewed as atoms flowing through sluice gates
Published in Biochemistry and molecular biology education (01-07-2007)“…Why should we think of enzymes as sluice gates? We are used to talk about "metabolic flux": I should like to suggest that we should indeed envision metabolism…”
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Mutational and Cysteine Scanning Analysis of the Glucagon Receptor N-terminal Domain
Published in The Journal of biological chemistry (01-10-2010)“…The glucagon receptor belongs to the B family of G-protein coupled receptors. Little structural information is available about this receptor and its…”
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New functionally selective muscarinic agonists
Published in Life sciences (1973) (1993)“…The muscarinic pharmacology of two novel agonists related to McN-A-343, 4-F-PyMcN and 4-F-PyMcN+, has been studied by the use of pharmacological and…”
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Properties of a recombinant human secretin receptor : A comparison with the rat and rabbit receptors
Published in Pancreas (01-07-1999)“…A secretin receptor was cloned from a commercial human pancreatic complementary DNA (cDNA) bank. The amino acid sequence deduced from the nucleotide sequence…”
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