Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Francois Paul Bischoff"'
Autor:
Yasuyoshi Iso, Shigeru Ando, Harrie J.M. Gijsen, Yasuto Kido, Shinji Suzuki, Herman Borghys, Kenji Morimoto, Vijay Urmaliya, Deborah Dhuyvetter, Takahiko Yamamoto, Ard Teisman, Gaku Sakaguchi, Naoki Kanegawa, Nigel Austin, Eriko Matsuoka, An Van Den Bergh, Hisanori Ito, Takuya Oguma, Francois Paul Bischoff, Tamio Fukushima, Peter Verboven, Tomoyuki Kawachi, Kenji Nakahara, Yoshinori Yamano, Kosuke Anan, Ken-ichi Kusakabe
Publikováno v:
ChemMedChem. 14:1894-1910
The β-site amyloid precursor protein cleaving enzyme 1 (BACE1, also known as β-secretase) is a promising target for the treatment of Alzheimer's disease. A pKa lowering approach over the initial leads was adopted to mitigate hERG inhibition and P-g
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::985639c1cf0555b69c371d024a0d30ea
https://doi.org/10.1002/cmdc.201900478
https://doi.org/10.1002/cmdc.201900478
Autor:
Manuel Hitzenberger, Francois Paul Bischoff, Marc Mercken, Sam Lismont, Katarzyna Marta Zoltowska, Natalie S. Ryan, Martin Zacharias, Dieter Petit, Lucía Chávez-Gutiérrez
Publikováno v:
The EMBO Journal
γ-Secretase complexes (GSECs) are multimeric membrane proteases involved in a variety of physiological processes and linked to Alzheimer's disease (AD). Presenilin (PSEN, catalytic subunit), Nicastrin (NCT), Presenilin Enhancer 2 (PEN-2), and Anteri
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::60075822ea25a5936594d3aafd319d16
https://lirias.kuleuven.be/handle/123456789/654197
https://lirias.kuleuven.be/handle/123456789/654197
Autor:
Garrett Berlond Minne, Michel Surkyn, Harrie J.M. Gijsen, Francois Paul Bischoff, Nigel Austin, Marc Mercken, Didier Berthelot, Chiara Zavattaro, Ishtiyaque Ahmad, Gregor James Macdonald, Adriana Ingrid Velter, Michel Anna Jozef De Cleyn, Deborah Dhuyvetter, Sven Franciscus Anna Van Brandt, Serge Maria Aloysius Pieters, Yves Emiel Maria Van Roosbroeck, Swapan Kumar Samanta, Herman Borghys
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(14)
The discovery, design and synthesis of a new series of GSMs is described. The classical imidazole heterocycle has been replaced by a cyano group attached to an indole nucleus. The exploration of this series has led to compound 26-S which combined hig
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8d9f458af2fb6e368fbdd2185f1f9926
https://pubmed.ncbi.nlm.nih.gov/31122869
https://pubmed.ncbi.nlm.nih.gov/31122869
Autor:
Brian Lord, Jason C. Rech, Brian Scott, Kirsten L. Morton, Nicholas I. Carruthers, Victor Contreras, Natalie A. Hawryluk, Qi Wang, Xiaohui Jiang, Francois Paul Bischoff, Michael A. Letavic, Alan D. Wickenden, Pascal Bonaventure, Hong Ao, Serge Maria Aloysius Pieters, Zachary S. Sales, Anindya Bhattacharya, Adriana Ingrid Velter
Publikováno v:
ACS Medicinal Chemistry Letters. 4:419-422
The synthesis and preclinical characterization of two novel, brain penetrating P2X7 compounds will be described. Both compounds are shown to be high potency P2X7 antagonists in human, rat, and mouse cell lines and both were shown to have high brain c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4c778658858962a1ac276dc8d4cd5e98
https://doi.org/10.1021/ml400040v
https://doi.org/10.1021/ml400040v
Autor:
Harrie J.M. Gijsen, Francois Paul Bischoff, Serge Maria Aloysius Pieters, Yves Emiel Maria Van Roosbroeck, Didier Berthelot, Chantal Masungi, Andrés A. Trabanco, Garrett Berlond Minne, Gary Tresadern, Adriana Ingrid Velter, Frederik J. R. Rombouts, Michel Anna Jozef De Cleyn, Libuse Jaroskova, Michel Surkyn, Tongfei Wu, Sven Franciscus Anna Van Brandt, Daniel Oehlrich, Gregor James Macdonald, Herman Borghys, Marc Mercken
Publikováno v:
Bioorganicmedicinal chemistry letters. 24(24)
The design and synthesis of a novel series of potent gamma secretase modulators is described. Exploration of various spacer groups between the triazole ring and the aromatic appendix in 2 has led to anilinotriazole 28, which combined high in vitro an
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b96513d173e9cb95fe1640d86f6c253a
https://pubmed.ncbi.nlm.nih.gov/25454273
https://pubmed.ncbi.nlm.nih.gov/25454273
Autor:
Anton Megens, Frans A. F. Van den Keybus, Love Christopher John, Francois Paul Bischoff, Serge Maria Aloysius Pieters, Josée E. Leysen, Mertens Josephus Carolus, Mirielle Braeken, Ludo Edmond Josephine Kennis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:71-74
The synthesis and biological activity of a series of benzofuro[3,2- c ]pyridines and a benzothieno[3,2- c ]pyridine are described. These compounds exhibit high affinity for the α 2 -adrenoceptor, with high selectivity versus the α 1 -receptor. Comp
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a94288f6519da6e706464dc316766598
https://doi.org/10.1016/s0960-894x(99)00591-0
https://doi.org/10.1016/s0960-894x(99)00591-0
Autor:
Adriana Ingrid Velter, Michel Anna Jozef De Cleyn, Frederik J. R. Rombouts, Sven Franciscus Anna Van Brandt, Didier Berthelot, Andrés A. Trabanco, Marc Mercken, Francois Paul Bischoff, Harrie J.M. Gijsen, Michel Surkyn, Tongfei Wu, Daniel Oehlrich, Libuse Jaroskova, Gregor James Macdonald, Gary Tresadern
Publikováno v:
Bioorganicmedicinal chemistry letters. 23(17)
The evolution of amide 3 into conformationally restricted bicyclic triazolo-piperidine 14-S as a γ-secretase modulator is described. This is a potential disease modifying anti-Alzheimer’s drug which demonstrated high in vitro and in vivo potency a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ccc1057bc559feaab7c8e5c34446e9c
https://pubmed.ncbi.nlm.nih.gov/23890837
https://pubmed.ncbi.nlm.nih.gov/23890837