Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Denis Carniato"'
Autor:
Fabien Schmidlin, Sophie Bozec, Franck F. Lepifre, Denis Carniato, Serge Christmann-Franck, Eric Valeur, Caroline Leriche, Didier Roche, Marc Lecomte, Liliane Doare, Christine Charon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:3682-3685
Spiro-carboxamides were identified as inhibitors of 11β-hydroxysteroid-dehydrogenase type 1 by high-throughput screening. Structure-based drug design was used to optimise the initial hit yielding a sub-nanomolar IC50 inhibitor (0.5 nM) on human 11β
Autor:
Eric Valeur, Marc Lecomte, Christine Charon, Caroline Leriche, Franck F. Lepifre, Liliane Doare, Fabien Schmidlin, Denis Carniato, Serge Christmann-Franck, Didier Roche, Ulrich Graedler, Sophie Bozec
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2674-2678
Benzylamides of pentanedioic acid were identified as inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) by high-throughput screening. Optimisation to 2-adamantyl amides yielded inhibitors with single digit nanomolar IC(50)s on the
Autor:
Catherine Guillou, Yves Collette, Stéphanie Miserey-Lenkei, Bruno Goud, Bernard Pau, Denis Carniato, Cécile Bougeret, Norbert Vey
Publikováno v:
Cancer Research. 77:4140-4140
Mitotic kinesins are essential regulators of cancer cell replication and migration. The mitotic kinesin MKLP2/KIF20A, a member of the kinesin-6 family, plays an essential role during cytokinesis and was identified as a potential new target for cancer
Autor:
Thomas R. Gadek, Denis Carniato, Martine Gaillard, Marielle Auberval, Jochen Knolle, Roland Baron, Jean-Marie Ruxer, Karl-Heinz Scheunemann, Jean-Francois Gourvest, Gerhard Breipohl, Hans Ulrich Stilz, Volkmar Wehner, Sarah C. Bodary, Bernard Doucet, David William Will, Anusch Peyman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2011-2015
A series of novel, highly potent αvβ3 antagonists based on a thiophene scaffold and containing an acylguanidine as an Arg-mimetic is described. A number of structural features, such as cyclic versus open guanidine and a variety of lipophilic side c
Autor:
Jochen Knolle, Denis Carniato, Hans Ulrich Stilz, Jean-Marie Ruxer, Karl-Heinz Scheunemann, Anusch Peyman, Gerhard Breipohl, Thomas R. Gadek, Volkmar Wehner, Jean-Francois Gourvest, Sarah C. Bodary
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:179-182
The synthesis of a series of RGD mimetic α V β 3 antagonists containing a hydantoin scaffold is shown. The results demonstrate some of the structural requirements for the design of selective α V β 3 antagonists (vs α IIb β 3 ) in terms of the A
Autor:
Denis Carniato, Paul A. Foster, Jean-François Briand, Gregoire Prevost, Mathieu Gutmann, Anne Chauchereau, Armand De Grammont, Maria Serova, Patrick Ladam, Marc-Henry Pitty, Marine Garrido, Annemilaï Tijeras-Raballand
Publikováno v:
Cancer Research. 76:3760-3760
Protein disulfide isomerase (PDI) is a chaperone protein that regulates oxidative protein folding as well as cell viability. Increased PDI levels have been documented in a variety of human cancers, including ovarian, prostate, and lung cancers. Inhib
Autor:
Per Hillertz, Eric Valeur, Christine Charon, Didier Roche, Serge Christmann-Franck, Djordje Musil, Denis Carniato, Liliane Doare, Sophie Bozec, Fabien Schmidlin, Melanie Schultz, Cravo Daniel, Franck F. Lepifre, Marc Lecomte
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(18)
Indole-pyrrolidines were identified as inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) by high-throughput screening. Optimisation of the initial hit through structure-based design led to 7-azaindole-derivatives, with the best analo
Autor:
Paul A. Foster, Jean-François Briand, Marc-Henry Pitty, Gregoire Prevost, Denis Carniato, Maria Serova, Anne Chauchereau, Nouri Neamati, Shili Xu, Armand De Grammont, Annemilaï Tijeras-Raballand, Christian Gespach, Eric Raymond, Marine Garrido, Mathieu Gutmann, Celine Lefebvre, Michèle Sabbah
Publikováno v:
Cancer Research. 75:4466-4466
Protein disulfide isomerase (PDI) is a chaperone protein that regulates oxidative protein folding as well as cell viability. Increased PDI levels have been documented in a variety of human cancers, including ovarian, prostate, and lung cancers. Inhib
Publikováno v:
Cancer Research. 73:987-987
Cancer drug pan-resistance is associated with patients having a disease progression despite receiving new treatments. Often resistance arises in two steps, initially, the tumor responds to the drug, but not all tumor cells are killed leading to a sel