Zobrazeno 1 - 10
of 47
pro vyhledávání: '"J.M. Gijsen"'
Autor:
J.M. Gijsen
Publikováno v:
Studies over de sociaaleconomische geschiedenis van Limburg/Jaarboek van het Sociaal Historisch Centrum voor Limburg. 40:1-74
Studie waarin wordt geschetst hoe Mgr. H.J. Kerens (1725-1792), achtereenvolgens 'bisschop van Roermond, Wiener Neustadt en Sankt Pöiten, als adviseur van het Oostenrijkse hof bijdragen leverde aan een toenemende bemoeienis van de keizerlijke regeri
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::d83c335ef7c16bbfbf7bd924a166245d
https://doi.org/10.58484/ssegl.v40i12639
https://doi.org/10.58484/ssegl.v40i12639
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:
Ann Vos, Frederik Jan Rita Rombouts, Andrés A. Trabanco, Daniel Oehlrich, Harrie J.M. Gijsen, Diederik Moechars, Sven Franciscus Anna Van Brandt, Aldo Peschiulli, Gregor James Macdonald, Michel Surkyn, Gary Tresadern, Michiel Van Gool, Nigel E. Austin, Michel Anna Jozef De Cleyn
Publikováno v:
ACS Med Chem Lett
[Image: see text] We recently disclosed a set of heteroaryl-fused piperazine inhibitors of BACE1 that combined nanomolar potency with good intrinsic permeability and low Pgp-mediated efflux. Herein we describe further work on two prototypes of this f
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1a245817121859b9f393819774f0f13
https://doi.org/10.1021/acsmedchemlett.1c00445
https://doi.org/10.1021/acsmedchemlett.1c00445
Autor:
Naoya Asada, Tatsuhiko Ueno, Shiho Yamamoto, Ken-ichi Kusakabe, Diederik Moechars, Naoki Kanegawa, Harrie J.M. Gijsen, Frederik J. R. Rombouts, Mana Ito, Eriko Matsuoka, Hisanori Ito
Publikováno v:
Journal of Medicinal Chemistry. 64:14165-14174
β-Site amyloid precursor protein-cleaving enzyme 1 (BACE1) is considered to be a promising target for treating Alzheimer's disease. However, all clinical BACE1 inhibitors have failed due to lack of efficacy, and some have even led to cognitive worse
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f3fba8f14de84d333a48c575bf1fbb2e
https://doi.org/10.1021/acs.jmedchem.1c00359
https://doi.org/10.1021/acs.jmedchem.1c00359
Autor:
Ann Vos, Lieve Lammens, Richard Alexander, Frederik J. R. Rombouts, Michel Surkyn, Kenji Morimoto, Laurent Leclercq, Nigel Austin, Koichi Tsubone, Tatsuhiko Ueno, Michel Anna Jozef De Cleyn, Deborah Dhuyvetter, Ken-ichi Kusakabe, Ard Teisman, Diederik Moechars, Tom Jacobs, An Van Den Bergh, Hirokazu Sumiyoshi, Herman Borghys, Shunsuke Einaru, Soufyan Jerhaoui, Brian Joel Hrupka, Harrie J.M. Gijsen
Publikováno v:
Journal of Medicinal Chemistry. 64:14175-14191
The discovery of a novel 2-aminotetrahydropyridine class of BACE1 inhibitors is described. Their pKa and lipophilicity were modulated by a pending sulfonyl group, while good permeability and brain penetration were achieved via intramolecular hydrogen
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8b24d041c262542cc337ea98b8c94c5e
https://doi.org/10.1021/acs.jmedchem.1c00935
https://doi.org/10.1021/acs.jmedchem.1c00935
Publikováno v:
Expert Opinion on Therapeutic Patents. 31:25-52
Inhibition of β-site amyloid precursor protein cleaving enzyme 1 (BACE1) has been extensively pursued as potential disease-modifying treatment for Alzheimer's disease (AD). Clinical failures with BACE inhibitors have progressively raised the bar for
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::28f2d045cdaeb68e3483add2843c535d
https://doi.org/10.1080/13543776.2021.1832463
https://doi.org/10.1080/13543776.2021.1832463
Autor:
Ann Vos, Aldo Peschiulli, Frederik J. R. Rombouts, Sven Franciscus Anna Van Brandt, Pauline Heckmann, Michel Anna Jozef De Cleyn, Solène Bache, Carolina Martinez-Lamenca, Jos Leenaerts, Harrie J.M. Gijsen, Chien-Chi Hsiao
Publikováno v:
European journal of medicinal chemistry. 228
A common challenge for medicinal chemists is to reduce the pKa of strongly basic groups' conjugate acids into a range that preserves the desired effects, usually potency and/or solubility, but avoids undesired effects like high volume of distribution
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e41dc8a2b5e76fa00d5c7ba322fab75
https://pubmed.ncbi.nlm.nih.gov/34920170
https://pubmed.ncbi.nlm.nih.gov/34920170
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:
Kazuki Fujimoto, Shigeru Ando, Yutaka Tonomura, Shuhei Yoshida, Harrie J.M. Gijsen, Shiho Yamamoto, Diederik Moechars, Naoki Kanegawa, Frederik J. R. Rombouts, Hisanori Ito, Kouki Fuchino, Shinji Suzuki, Takahiko Yamamoto, Eriko Matsuoka, Genta Tadano, Naoya Asada, Ken-ichi Kusakabe
Publikováno v:
Journal of medicinal chemistry. 64(6)
BACE1 is an attractive target for disease-modifying treatment of Alzheimer's disease. BACE2, having high homology around the catalytic site, poses a critical challenge to identifying selective BACE1 inhibitors. Recent evidence indicated that BACE2 ha
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8b448c0a6e751ca694511c7b88065fd2
https://pubmed.ncbi.nlm.nih.gov/33719429
https://pubmed.ncbi.nlm.nih.gov/33719429
Autor:
Sergio A. Alonso de Diego, Daniel Oehlrich, Harrie J.M. Gijsen, Andrés A. Trabanco, Hana Prokopcová, Nigel Austin, Michel Surkyn, Dries Van den Bossche, Frederik J. R. Rombouts, Deborah Dhuyvetter, Gregor James Macdonald, Sven Franciscus Anna Van Brandt, Herman Borghys, Michiel Van Gool, Diederik Moechars, Aránzazu García-Molina, Michel Anna Jozef De Cleyn, Carolina Martinez-Lamenca
Publikováno v:
Journal of Medicinal Chemistry. 61:5292-5303
In previous studies, the introduction of electron withdrawing groups to 1,4-oxazine BACE1 inhibitors reduced the pKa of the amidine group, resulting in compound 2 that showed excellent in vivo efficacy, lowering Aβ levels in brain and CSF. However,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b82fa110d3c2cadb8d001203f372949b
https://doi.org/10.1021/acs.jmedchem.8b00304
https://doi.org/10.1021/acs.jmedchem.8b00304