Zobrazeno 1 - 10
of 23
pro vyhledávání: '"Dominique Swinnen"'
Autor:
Martyn D. Wood, Anna Kolobova, Florence Moureau, Glen Ernst, Daniel Akuma, Ingrid P. Buchler, Florian Montel, James C. Barrow, Huijun Wei, Dominique Swinnen, Gregory V. Carr, Michael S. Poslusney, Emilie Jigorel, Vinh Au, Pablo De León, Michael DePasquale, Martha Kimos, Monika Sarah E.D. Schulze, Yifang Huang
Publikováno v:
Journal of Medicinal Chemistry. 61:9647-9665
A series of 8-hydroxy quinolines were identified as potent inhibitors of catechol O-methyltransferase (COMT) with selectivity for the membrane-bound form of the enzyme. Small substituents at the 7-position of the quinoline were found to increase meta
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0548e3750c7972bb8419983749ba6e77
https://doi.org/10.1021/acs.jmedchem.8b01126
https://doi.org/10.1021/acs.jmedchem.8b01126
Autor:
Ingrid P. Buchler, Noelle White, Florian Montel, Florence Moureau, Gregory V. Carr, Thierry Demaude, Véronique Durieu, Daniel Akuma, James C. Barrow, Pablo De León, Martyn D. Wood, Nathalie Van houtvin, Vinh Au, Huijun Wei, Marie Christine Vandergeten, Emilie Jigorel, Yifang Huang, Dominique Swinnen, Anna Kolobova, Michael S. Poslusney, Martha Kimos, Glen Ernst, Michael DePasquale, Spencer Byers, Sabine Defays
Publikováno v:
ACS Medicinal Chemistry Letters
A series of bicyclic pyridones were identified as potent inhibitors of catechol O-methyltransferase (COMT). Substituted benzyl groups attached to the basic nitrogen of the core scaffold gave the most potent inhibitors within this series. Rat pharmaco
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f9cf6bbaad26b38d002dd4bc88ec3368
https://pubmed.ncbi.nlm.nih.gov/32038769
https://pubmed.ncbi.nlm.nih.gov/32038769
Autor:
Zara A. Sands, Brice Mullier, Isabelle Niespodziany, Eric Jnoff, David Moreno-Delgado, Christian Wolff, Dominique Swinnen, Véronique M. André, Philippe Ghisdal, Martyn Wood
Publikováno v:
CNS neurosciencetherapeutics. 25(4)
Aims Kv1.1 (KCNA1) channels contribute to the control of neuronal excitability and have been associated with epilepsy. Kv1.1 channels can associate with the cytoplasmic Kvβ1 subunit resulting in rapid inactivating A-type currents. We hypothesized th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f50a77db6a8848dd800a28d64f3db11d
https://pubmed.ncbi.nlm.nih.gov/30242974
https://pubmed.ncbi.nlm.nih.gov/30242974
Autor:
Kuniko Kohyama, Hong Ji, Thomas Rückle, Xiaoli Guo, Yoh Matsumoto, Hidenori Ichijo, Chikako Harada, Montserrat Camps, Kazuhiko Namekata, Atsushi Matsuzawa, Mathilde Muzerelle, Atsuko Kimura, Catherine Jorand-Lebrun, Takayuki Harada, Dominique Swinnen, Pierre Alain Vitte
Publikováno v:
EMBO Molecular Medicine
Apoptosis signal-regulating kinase 1 (ASK1) is an evolutionarily conserved mitogen-activated protein kinase (MAPK) kinase kinase which plays important roles in stress and immune responses. Here, we show that ASK1 deficiency attenuates neuroinflammati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cdb4677f8836c9979f3b28a364555c08
https://doi.org/10.1002/emmm.201000103
https://doi.org/10.1002/emmm.201000103
Autor:
Anthony Nichols, David Covini, Anna Quattropani, Jean-François Arrighi, Yves Cambet, Maurizio Maio, Thierry Martin, Olivier Schott, Bernard Françon, Laurence Novo-Perez, Don Simpson, Delphine Marin, Delphine Rivron, Cristina Donini, Agnes Bombrun, Pierre-Alain Vitte, Stefano Crosignani, Wolfgang H. B. Sauer, Isabelle Martinou, Dominique Swinnen, Valerie Eligert, Fabienne Burgat-Charvillon
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1516-1519
The discovery of a novel series of S1P1 agonists is described. Starting from a micromolar HTS positive, iterative optimization gave rise to several single-digit nanomolar S1P1 agonists. The compounds were able to induce internalization of the S1P1 re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::016d011f2a43aa5c6d794dc932148d8b
https://doi.org/10.1016/j.bmcl.2010.01.102
https://doi.org/10.1016/j.bmcl.2010.01.102
Autor:
Timothy N. C. Wells, Rob Hooft van Huijsduijnen, Christine L. Gee, Christoph Grundner, Jerome Gonzalez, Dominique Swinnen, Dominique Perrin, Tom Alber
Publikováno v:
Structure. 15:499-509
SummaryTyrosine kinases and phosphatases establish the crucial balance of tyrosine phosphorylation in cellular signaling, but creating specific inhibitors of protein Tyr phosphatases (PTPs) remains a challenge. Here, we report the development of a po
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::23bbe9e1e1cbd569500c04b2a8261c90
https://doi.org/10.1016/j.str.2007.03.003
https://doi.org/10.1016/j.str.2007.03.003
Publikováno v:
Drug Discovery Today. 7:1013-1019
Protein tyrosine phosphatases (PTPs) have emerged as a new and promising class of signaling targets, since the discovery of PTP1B as a major drug target for diabetes and obesity. Blocking individual PTPs results in the activation of specific tyrosine
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b7bd26b63f0d0f1d9fe38feac27ffcc3
https://doi.org/10.1016/s1359-6446(02)02438-8
https://doi.org/10.1016/s1359-6446(02)02438-8
Autor:
Junya Mizukami, Takehiro Sato, Dominique Swinnen, Thomas Rueckle, Kohsuke Takeda, Ryoji Tsuboi, Hidenori Ichijo, Hong Ji, Montserrat Camps
Publikováno v:
Scientific Reports
Contact hypersensitivity (CHS) is a form of delayed-type hypersensitivity triggered by the response to reactive haptens (sensitization) and subsequent challenge (elicitation). Here, we show that ASK1 promotes CHS and that suppression of ASK1 during t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7d4d6eca55b7bdc7b688c9d10200b116
https://pubmed.ncbi.nlm.nih.gov/24736726
https://pubmed.ncbi.nlm.nih.gov/24736726
Autor:
Dominique Swinnen, Donald Hilvert
Publikováno v:
Organic Letters. 2:2439-2442
A short route to peptide C-terminal thioesters was developed that does not require the use of special linkers or resins and is compatible with standard Fmoc chemistry. Following conventional solid-phase peptide synthesis, an excess of Me(2)AlCl and E
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a33cd63a29247f95b84ec55a86b2a954
https://doi.org/10.1021/ol0060836
https://doi.org/10.1021/ol0060836
Autor:
Alain Krief, Dominique Swinnen
Publikováno v:
Tetrahedron Letters. 37(39):7123-7126
Reaction of sulfur ylides with suitably 4-functionalized-5,5-dimethyl-2-cyclopentenones allows an efficient entry to the bicyclo[3.1.0]hexan-2-one skeleton which proved to be a valuable precursor of vinyl cyclopropane carboxylic acids. Application to
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ad79ee35e843d8acdb377d65eeb01cc
https://researchportal.unamur.be/en/publications/ceef48bd-1f3f-4c41-aca0-4cad80a72fcc
https://researchportal.unamur.be/en/publications/ceef48bd-1f3f-4c41-aca0-4cad80a72fcc