Zobrazeno 1 - 10
of 44
pro vyhledávání: '"Frederik J R, Rombouts"'
Autor:
Frederik J. R. Rombouts, Richard Alexander, Erna Cleiren, Alex De Groot, Michel Carpentier, Joyce Dijkmans, Katleen Fierens, Stefan Masure, Diederik Moechars, Martina Palomino-Schätzlein, Antonio Pineda-Lucena, Andrés A. Trabanco, Daan Van Glabbeek, Ann Vos, Gary Tresadern
Publikováno v:
ACS Omega, Vol 2, Iss 2, Pp 685-697 (2017)
Externí odkaz:
https://doaj.org/article/b8afeb20f88a4af39591a00477541482
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
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
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
Autor:
Herman Borghys, Fetene Tekle, Astrid Bottelbergs, Deborah Dhuyvetter, Rob J. Vreeken, Maxim Nazarov, Ilse Lenaerts, Frederik J. R. Rombouts
Publikováno v:
Drug Delivery
article-version (VoR) Version of Record
Drug Delivery, Vol 27, Iss 1, Pp 1597-1607 (2020)
article-version (VoR) Version of Record
Drug Delivery, Vol 27, Iss 1, Pp 1597-1607 (2020)
The blood–brain barrier (BBB) is often a limiting factor for getting drugs in the brain. Bypassing the BBB by intranasal (IN), or also called nose to brain (NTB), route is an interesting and frequently investigated concept for brain drug delivery.
Autor:
David S. Russell, Cristian Constantinescu, Olivier Barret, Mark E. Schmidt, Diederik Moechars, Maarten Timmers, Frederik J. R. Rombouts, Hartmuth C. Kolb, Luc Janssens, Christine M. Sandiego, Jennifer Madonia
Publikováno v:
European Journal of Nuclear Medicine and Molecular Imaging. 47:3176-3185
Purpose The accumulation of misfolded tau is a common feature of several neurodegenerative disorders, with Alzheimer’s disease (AD) being the most common. Earlier we identified JNJ-64326067, a novel isoquinoline derivative with high affinity and se
Autor:
Demin Samuël Dominique, Carolina Martinez-Lamenca, Kevin Lam, Mary-Ambre Carvalho, Frederik J. R. Rombouts, Morgan Lecomte, Fedor Romanov-Michailidis
Nitriles are recurring motifs in bioactive molecules and versatile functional groups in synthetic chemistry. Despite recent progress, direct introduction of a nitrile moiety in heteroarenes remains challenging. Recent developments in electrochemical
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::38b9a70091dae3594763da883216d9c5
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
Autor:
Hartmuth C. Kolb, Stijn Wuyts, Cindy Wintmolders, Leenaerts Joseph Elisabeth, Astrid Bottelbergs, Lieven Declercq, Fengbin Song, Paula te Riele, Chunfang A. Xia, Laura Iturrino, Frederik J. R. Rombouts, José-Ignacio Andrés, Diederik Moechars, Jonas Mariën, Lu Chen, Guy Bormans, Rik Vandenberghe
Publikováno v:
Journal of Medicinal Chemistry. 62:2974-2987
In Alzheimer’s disease, the density and spread of aggregated tau protein track well with neurodegeneration and cognitive decline, making the imaging of aggregated tau a compelling biomarker. A structure–activity relationship exploration around an
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