Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Erwin Fraiponts"'
Autor:
Lutgarde Serneels, Rajeshwar Narlawar, Laura Perez Benito, Marti Municoy, Victor Guallar, Dries T’Syen, Maarten Dewilde, François Bischoff, Erwin Fraiponts, Gary Tresadern, Peter W.M. Roevens, Harrie J.M. Gijsen, Bart De Strooper
Clinical development of γ-secretases, a family of intramembrane cleaving proteases, as therapeutic targets for a variety of disorders including cancer and Alzheimer's disease was aborted because of serious mechanism-based side effects in the phase I
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::34173e9b72a677f8f8c9ec51792ad684
https://lirias.kuleuven.be/handle/20.500.12942/719766
https://lirias.kuleuven.be/handle/20.500.12942/719766
Autor:
Donald William Ludovici, Gilles Bignan, Carsten Schubert, Erwin Fraiponts, Karine Smans, Norbert Esser, Danielle Peeters, Michael H. Parker, Maxwell D. Cummings, Peter Vermeulen, Lieven Meerpoel, Sabine De Breucker, Tianbao Lu, Luc Van Nuffel, Richard Alexander, Bruce L. Grasberger, James R. Bischoff, Christian Rocaboy, Ron Gilissen, Christophe Meyer, Boudewijn Janssens, Peter J. Connolly
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:2159-2164
We designed and synthesized a new series of fatty acid synthase (FASN) inhibitors with potential utility for the treatment of cancer. Extensive SAR studies led to highly active FASN inhibitors with good cellular activity and oral bioavailability, exe
Autor:
Michel A.J. De Cleyn, Harrie J.M. Gijsen, Marjoleen J.M.A Nijsen, Erwin Fraiponts, Michel Surkyn, Bie M.P. Verbist, Jeroen Aerssens
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:2574-2579
A novel series of benzimidazole CB2-receptor agonists was synthesized and the structure-activity relationship explored. The results showed agonistic activities with an EC(50) up to 0.5 nM and excellent selectivity (>4000-fold) over the CB1 receptor.
Autor:
Danielle Peeters, Michael H. Parker, Donald William Ludovici, Christophe Meyer, Richard Alexander, Bruce L. Grasberger, S. de Breucker, Christian Rocaboy, Norbert Esser, Lieven Meerpoel, Tianbao Lu, Ronaldus Arnodus Hendrika Joseph Gilissen, Maxwell D. Cummings, Peter J. Connolly, James R. Bischoff, Gilles Bignan, Erwin Fraiponts, Boudewijn Janssens, Karine Smans, Carsten Schubert
Publikováno v:
European Journal of Cancer. 50:141-142
Autor:
Lieven Meerpoel, Gilles Bignan, Luc Van Nuffel, Peter Vermeulen, Ron Gilissen, Tianbao Lu, Max Cummings, Christophe Meyer, Bruce L. Grasberger, Peter J. Connolly, Michael H. Parker, Erwin Fraiponts, Richard Alexander, Karine Smans, Boudewijn Janssens, Danielle Peeters, Norbert Esser, Donald William Ludovici, Carsten Schubert, James R. Bischoff, Sabine De Breucker
Publikováno v:
Cancer Research. 74:4747-4747
Fatty Acid Synthase (FASN) is a multi-domain protein that carries out de novo fatty acid (palmitate) synthesis from acetate and malonate in mammalian cells. FASN is up-regulated in cancer cells, providing fatty acid building blocks for rapid cell gro
Autor:
Lieven Meerpoel, James R. Bischoff, Carsten Schubert, Boudewijn Janssen, Geert Van Hecke, Erwin Fraiponts, Karine Smans, Luc Van Nuffel, Sabine De Breucker, Tianbao Lu, Michael H. Parker, Danielle Peeters, Yolanda T. Chong, Bruce L. Grasberger, Peter Vermeulen, Christophe Meyer, Ralph Graeser, Gilles Bignan, Suzana Vidic, Norbert Esser, Donald William Ludovici, Ron Gilissen, Peter J. Connolly
Publikováno v:
Cancer Research. 74:801-801
Fatty Acid Synthase (FASN) catalyzes the final step in palmitate (PA) synthesis, using acetyl-CoA, malonyl-CoA and NADPH. Most normal tissues express low levels of FASN and rely on uptake of fatty acids (FA) from the diet. It has been proposed that F
Autor:
Carsten Schubert, Ron Gilissen, Bruce L. Grasberger, Christophe Meyer, Peter J. Connolly, Sabine De Breucker, Luc Van Nuffel, Norbert Esser, James R. Bischoff, Michael H. Parker, Donald William Ludovici, Erwin Fraiponts, Boudewijn Janssens, Danielle Peeters, Karine Smans, Tianbao Lu, Peter Vermeulen, Lieven Meerpoel, Gilles Bignan
Publikováno v:
Cancer Research. 74:2535-2535
De novo synthesis of fatty acids in mammalian cells is catalyzed by Fatty Acid Synthase (FASN), a complex dimeric protein with seven catalytic domains that processes acetyl-CoA and malonyl-CoA into palmitic acid. Palmitate and other fatty acids are e
Autor:
Mariette Bekkers, Menelas N. Pangalos, Liesbet van der Helm, David Ashton, Jean-Marc Neefs, Erwin Fraiponts, Marijke Somers, Robert Gordon, Peter Verhasselt
Publikováno v:
The Journal of biological chemistry. 274(13)
Hydrolysis of the neuropeptideN-acetyl-l-aspartyl-l-glutamate (NAAG) by N-acetylated α-linked acidic dipeptidase (NAALADase) to release glutamate may be important in a number of neurodegenerative disorders in which excitotoxic mechanisms are implica