Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Christophe Thurieau"'
Autor:
Christophe Thurieau, S. J. Stanway, Atul Purohit, Michael J. Reed, Barry V. L. Potter, L. W. Lawrence Woo, Patrick Delavault
Publikováno v:
The Oncologist. 12:370-374
Inhibitors of steroid sulfatase are being developed as a novel therapy for hormone-dependent breast cancer in postmenopausal women. Data suggest that steroid sulfatase (STS) activity is much higher than aromatase activity in breast tumors and high le
Autor:
Pierre Roubert, Christophe Thurieau, Dennis Bigg, Lydie Poitout, Christophe Moinet, Jacques Pommier, Pascale Plas, Marie-Odile Contour-Galcera, Lannoy Jacques
Publikováno v:
Journal of Medicinal Chemistry. 44:2990-3000
Using a solution-phase parallel synthesis strategy, a series of non-peptide somatostatin analogues were prepared, and their binding affinities to the five human somatostatin receptor subtypes (sst(1-5)) were determined. Imidazolyl derivatives 2 were
Autor:
Lydie Poitout, Marie-Odile Contour-Galcera, Barry A. Morgan, Christophe Moinet, Pierre Roubert, Thomas D. Gordon, Christophe Thurieau
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:991-995
A series of imidazole derivatives has been prepared using high throughput parallel synthesis. Several compounds showed high affinity (Ki in 10(-6)-10(-8) M range) and selectivity at recombinant human somatostatin receptor subtype 3 (hsst3).
Autor:
Christophe Thurieau, Barry A. Morgan, Pierre Roubert, Christophe Moinet, Lydie Poitout, Thomas D. Gordon, Marie-Odile Contour-Galcera
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:741-745
A new preparation of trisubstituted imidazopyrazines and dihydroimidazopyrazines via parallel synthesis using aminoacids and bromoketones resulted in the discovery of non-peptidic sst5 selective agonists.
Publikováno v:
Thrombosis and Haemostasis. 80:310-315
The interaction between GPIb and thrombin promotes platelet activation elicited via the hydrolysis of the thrombin receptor and involves structures located on the segment 238-290 within the N-terminal domain of GPIbalpha and the positively charged ex
Autor:
Michel Félétou, Isabelle Jamonneau, Martine Germain, Christophe Thurieau, Jean-Luc Fauchere, Pietro Ghezzi, Emmanuel Canet, Pia Villa
Publikováno v:
Journal of Cardiovascular Pharmacology. 27:500-507
The purpose of our work was to evaluate the role of bradykinin B2 receptors in the early phase (first 3 h) of bacterial lipopolysaccharide (LPS)-induced shock in anesthetized and mechanically ventilated rabbits and to determine if HOE 140, a specific
Autor:
Michel Félétou, Christophe Thurieau, Eric Raimbaud, Philippe Hennig, Emmanuel Canet, Jean-Luc Fauchère
Publikováno v:
Journal of Medicinal Chemistry. 39:2095-2101
We report here on the synthesis and pharmacological properties of a new series of small linear and cyclic peptides derived from the five C-terminal amino acid residues of second-generation bradykinin receptor antagonists. Variations of the two first
Autor:
Mathieu Molimard, Christophe Thurieau, Emmanuel Canet, Martine Germain, Michel Félétou, Emmanuel Naline, Jean-Luc Fauchere, Charles Advenier, Corinne A.E. Martin
Publikováno v:
European Journal of Pharmacology. 274:57-64
Bradykinin is a potent inflammatory mediator which may be involved in various airway diseases. A selective and potent antagonist of the bradykinin B2 receptor has recently been discovered (HOE 140: D-Arg-[Hyp3,Thi5,D-Tic7,Oic8]bradykinin). The purpos
Autor:
S. Krantic, Jean-Paul Vilaine, Jean-Luc Fauchere, Philip Janiak, C. Guyard, N. Kucharczyk, Christophe Thurieau, A Pillon
Publikováno v:
European Journal of Medicinal Chemistry. 30:115-122
Summary We report on the synthesis and pharmacological properties of a new series of somatostatin analogs. Two lower homologs of lysine, 2,3-diaminopropanoic acid and 2,4-diaminobutyric acid, were prepared and used for cyclization via amide formation
Publikováno v:
British Journal of Pharmacology. 112:683-689
1. Hoe 140, a recently described bradykinin B2 antagonist, and NPC 567 from an earlier generation of bradykinin B2 antagonists, were tested in rabbit and sheep isolated blood vessels. 2. In rabbit jugular vein, a bradykinin B2 preparation, NPC 567 wa