Zobrazeno 1 - 10
of 16
pro vyhledávání: '"Olivier Defert"'
Autor:
Nele Kindt, Geert Reyns, Olivier Defert, Patrick Schöffski, Massimiliano Mazzone, Agnieszka Wozniak, Carla Riera-Domingo, Marjan Diricx, Marijke Pellens, Tom Janssens, Marzia De Petrini, Natalie De Geest, Peter Pokreisz, Britt Van Renterghem, Lawrence Van Helleputte, Andrea Casazza
Clinical use of doxorubicin (Dox) is limited by cumulative myelo- and cardiotoxicity. This research focuses on the detailed characterization of PhAc-ALGP-Dox, a targeted tetrapeptide prodrug with a unique dual-step activation mechanism, designed to c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8914754f35dc5e01e0cb964ae25c0fda
https://doi.org/10.1158/1535-7163.c.6543549
https://doi.org/10.1158/1535-7163.c.6543549
Autor:
Andrea Casazza, Lawrence Van Helleputte, Britt Van Renterghem, Peter Pokreisz, Natalie De Geest, Marzia De Petrini, Tom Janssens, Marijke Pellens, Marjan Diricx, Carla Riera-Domingo, Agnieszka Wozniak, Massimiliano Mazzone, Patrick Schöffski, Olivier Defert, Geert Reyns, Nele Kindt
Publikováno v:
Molecular cancer therapeutics. 21(4)
Clinical use of doxorubicin (Dox) is limited by cumulative myelo- and cardiotoxicity. This research focuses on the detailed characterization of PhAc-ALGP-Dox, a targeted tetrapeptide prodrug with a unique dual-step activation mechanism, designed to c
Autor:
Melissa Dullaers, Yves-Paul Vandewynckel, Dirk Leysen, Lien Van den Bossche, Karolien Castermans, Roosmarijn E. Vandenbroucke, Sarah Devriese, Lindsey Devisscher, Riet De Rycke, Karel Geboes, Olivier Defert, Sandro Boland, Arnaud Bourin, Tom Holvoet, Pieter Hindryckx, Martine De Vos, Sophie Van Welden, Debby Laukens
Publikováno v:
Gastroenterology 153 (2017) 4
Gastroenterology, 153(4), 1054-1067
Gastroenterology, 153(4), 1054-1067
Background Intestinal fibrosis resulting in (sub)obstruction is a common complication of Crohn's disease (CD). Rho kinases (ROCKs) play multiple roles in TGFβ-induced myofibroblast activation that could be therapeutic targets. Because systemic ROCK
Publikováno v:
MedChemComm. 7:478-483
Extensive structure–activity studies on three different modification sites resulted in a series of LIM kinase inhibitors, containing a novel tricyclic hinge-binding motif based on the pyrrolopyrimidine scaffold. The compounds display a superior sel
Autor:
Karolien Castermans, Jessica Vanormelingen, Sarah Van de Velde, Nele Kindt, Arnaud Bourin, Jo Alen, Silke Fransen, Nicki Boumans, Jacques Geraets, Olivier Defert, Pieter Schroeders, Laura Panitti, Sandro Boland
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 25:4005-4010
Inhibitors of LIM kinases are considered of interest for several indications, including elevated intraocular pressure (IOP), cancer, or infection by HIV-1. LX-7101 (Lexicon Pharmaceuticals) was advanced to Phase-I clinical trials as an IOP-lowering a
Autor:
Sandro Boland, Olivier Defert
Publikováno v:
Expert opinion on therapeutic patents. 27(4)
The Rho-kinases (ROCK), ROCK1 and ROCK2, are potent, widespread biochemical modulators which have been extensively studied. Due to the involvement of ROCKs in multiple biological processes, ROCK inhibitors have pleiotropic actions and may be of relev
Autor:
Jessica Vanormelingen, Nicki Boumans, Arnaud Bourin, Sandro Boland, Olivier Defert, Dirk Leysen, Jo Alen, Karolien Castermans, Laura Panitti
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 24:4594-4597
PDE4 inhibitors are of high interest for treatment of a wide range of inflammatory or autoimmune diseases. Their potential however has not yet been realized due to target-associated side effects, resulting in a low therapeutic window. We herein repor
Autor:
Caroline Phillips, R. Armer, N Hawkins, C Jones, Dirk Leysen, Debby Laukens, Tom Holvoet, K Eckersley, Yves-Paul Vandewynckel, Pieter Hindryckx, M. De Vos, Lindsey Devisscher, Olivier Defert, Karel Geboes, Karolien Castermans, M. Bingham, P Bunyard, Sandro Boland, R. De Rycke, Melissa Dullaers, Roosmarijn E. Vandenbroucke, Sarah Devriese, L. Van den Bossche, S. Van Welden, Arnaud Bourin
Publikováno v:
Journal of Crohn's and Colitis. 12:S100-S101
Publikováno v:
Journal of medicinal chemistry. 59(6)
Rho kinases (ROCKs) belong to the serine–threonine family, the inhibition of which affects the function of many downstream substrates. As such, ROCK inhibitors have potential therapeutic applicability in a wide variety of pathological conditions in
Autor:
Olivier Defert, Sandro Boland
Publikováno v:
Drug discovery today. Technologies. 18
Protein kinases represent one of the largest superfamilies of drugable targets and a major research area for both the pharmaceutical industry and academic groups. This has resulted in the emergence of numerous screening technologies and services dedi