Zobrazeno 1 - 10
of 22
pro vyhledávání: '"Klaus Hinterding"'
Autor:
Barbara Nuesslein-Hildesheim, Nigel Graham Cooke, E Wallström, M Saltzman, Anne Gardin, Shifeng Pan, N Wang, A Vitaliti, Martin Traebert, Mara Rosenberg, W J Crumb, Andrea Groenewegen, Nathanael S. Gray, Danilo Guerini, Tobias Sing, Pál Gergely, Volker Brinkmann, J Yang, Klaus Hinterding, O Luttringer, Christian Bruns
Publikováno v:
British Journal of Pharmacology
BACKGROUND AND PURPOSE BAF312 is a next-generation sphingosine 1-phosphate (S1P) receptor modulator, selective for S1P1 and S1P5 receptors. S1P1 receptors are essential for lymphocyte egress from lymph nodes and a drug target in immune-mediated disea
Autor:
Eric Francotte, Danilo Guerini, Markus Streiff, Markus Zollinger, Karl Welzenbach, Rainer Albert, Klaus Hinterding, Trixie Wagner, Helmut Knecht, Nigel Graham Cooke, Frédéric Zecri, Corinne Simeon, Constanze Müller-Hartwieg, Volker Brinkmann
Publikováno v:
Journal of Medicinal Chemistry. 48:5373-5377
In vivo phosphorylation of FTY720 (1) in rats and humans resulted exclusively in the biologically active (S)-configured enantiomer, which was proven by an ex vivo o-phthaldialdehyde derivatization protocol especially elaborated for phosphates of 1. S
Autor:
Klemens Hoegenauer, Sylvain Cottens, Peter Nussbaumer, Frédéric Zecri, Peter Buehlmayer, Nathanael S. Gray, Shifeng Pan, Rainer Albert, Klaus Hinterding, Carsten Spanka, Peter Ettmayer, Volker Brinkmann
Publikováno v:
Synthesis. 2003:1667-1670
Efficient and versatile protocols for the synthesis of chiral analogues of the novel immunomodulator FTY720 and its phosphate are described. These synthetic procedures allow for broad structural variation and deliver essential tools to further elucid
Publikováno v:
Chemistry - A European Journal. 5:227-236
A modularly built bisubstrate inhibitor of farnesyltransferase, pepticinnamin E (depicted), has been synthesized and its inhibitory activity studied. The latter is decisively influenced by the central tripeptide unit and the absolute configuration of
Publikováno v:
Angewandte Chemie International Edition. 37:1236-1239
A modularly built bisubstrate inhibitor, the natural product pepticinnamin E (shown on the right) was sythesized for the first time. In the case of in vitro assays it inhibits the enzyme farnesyltransferase with respect to both the peptide substrate
Publikováno v:
Angewandte Chemie. 110:1298-1301
Ein modular aufgebauter Bisubstratinhibitor ist die naturlich vorkommende Titelverbindung (rechts gezeigt), die nun erstmals synthetisiert wurde. Bei In-vitro-Assays hemmte sie das Enzym Farnesyltransferase sowohl bezuglich eines Peptidsubtrats als a
Publikováno v:
Angewandte Chemie International Edition. 37:688-749
The understanding of cellular communication pathways in molecular detail is an important goal of bioorganic research. The synthesis of analogues of active substances (e.g. 1) to study the regulation of muscle contraction or the specific lipid modific
Autor:
Anne Gardin, Nathanael S. Gray, Barbara Nuesslein-Hildesheim, Klaus Hinterding, Jianwei Che, Yi Fan, Xing Wang, Yuan Mi, Tove Tuntland, Wenqi Gao, Shifeng Pan, Yu Chen, Peter End, Christian Bruns, Nigel Graham Cooke, Peter Heining, Alan Chu, Sophie Lefebvre
Publikováno v:
ACS medicinal chemistry letters. 4(3)
A novel series of alkoxyimino derivatives as S1P1 agonists were discovered through de novo design using FTY720 as the chemical starting point. Extensive structure–activity relationship studies led to the discovery of (E)-1-(4-(1-(((4-cyclohexyl-3-(
Publikováno v:
Tetrahedron Letters. 43:8095-8097
FTY720 is an immunosuppressant with a novel mode of action and is highly effective in animal models of transplantation and autoimmunity. Herein we describe the first asymmetric synthesis of chiral FTY720 analogues using the Schollkopf-protocol. We al
Publikováno v:
Tetrahedron Letters. 42:8463-8465
Intramolecular Claisen-type cleavage of the Evans-oxazolidinone with an acetate enolate followed by reduction of the resulting ketone using a borane–amine complex yielded β-hydroxy-δ-lactones as fully functionalized polyketide precursors stereose