Zobrazeno 1 - 10 of 111 pro vyhledávání: '"Constant A A van Boeckel"'
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Akademický článek
A monoacylglycerol lipase inhibitor showing therapeutic efficacy in mice without central side effects or dependence
Autor: Ming Jiang, Mirjam C. W. Huizenga, Jonah L. Wirt, Janos Paloczi, Avand Amedi, Richard J. B. H. N. van den Berg, Joerg Benz, Ludovic Collin, Hui Deng, Xinyu Di, Wouter F. Driever, Bogdan I. Florea, Uwe Grether, Antonius P. A. Janssen, Thomas Hankemeier, Laura H. Heitman, Tsang-Wai Lam, Florian Mohr, Anto Pavlovic, Iris Ruf, Helma van den Hurk, Anna F. Stevens, Daan van der Vliet, Tom van der Wel, Matthias B. Wittwer, Constant A. A. van Boeckel, Pal Pacher, Andrea G. Hohmann, Mario van der Stelt
Publikováno v: Nature Communications, Vol 14, Iss 1, Pp 1-19 (2023)
Abstract Monoacylglycerol lipase (MAGL) regulates endocannabinoid 2-arachidonoylglycerol (2-AG) and eicosanoid signalling. MAGL inhibition provides therapeutic opportunities but clinical potential is limited by central nervous system (CNS)-mediated s
Externí odkaz: https://doaj.org/article/fdb22352db0b4e3798c8149c29653a5f
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3
Structure–Activity Relationship Studies of Pyrimidine-4-Carboxamides as Inhibitors of N-Acylphosphatidylethanolamine Phospholipase D
Autor: Mario van der Stelt, Constant A. A. van Boeckel, Wouter P F Driever, Elliot D. Mock, Ioli Kotsogianni, Jelle M Vooijs, Carmen S Fonseca, Hans den Dulk
Publikováno v: Journal of Medicinal Chemistry
N-Acylphosphatidylethanolamine phospholipase D (NAPE-PLD) is regarded as the main enzyme responsible for the biosynthesis of N-acylethanolamines (NAEs), a family of bioactive lipid mediators. Previously, we reported N-(cyclopropylmethyl)-6-((S)-3-hyd
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::f5513884dbdf20fac82a3386e83884af
https://doi.org/10.1021/acs.jmedchem.0c01441
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4
Comprehensive structure-activity-relationship of azaindoles as highly potent FLT3 inhibitors
Autor: Sebastian H. Grimm, Eelke B. Lenselink, Adriaan W. Tuin, Constant A. A. van Boeckel, Adrianus M. C. H. van den Nieuwendijk, Ruud H. Wijdeven, Jordi F. Keijzer, Mario van der Stelt, Herman S. Overkleeft, Jacques Neefjes, Nora Liu, Gerard J. P. van Westen, Berend Gagestein
Publikováno v: Bioorganic and Medicinal Chemistry
Bioorganic and Medicinal Chemistry, 27(5), 692-699
Acute myeloid leukemia (AML) is characterized by fast progression and low survival rates, in which Fms-like tyrosine kinase 3 (FLT3) receptor mutations have been identified as a driver mutation in cancer progression in a subgroup of AML patients. Cli
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8645479c35cd969df474b85b828fdea0
https://doi.org/10.1016/j.bmc.2019.01.006
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5
Structure-Activity Relationship Studies of Pyrimidine-4-Carboxamides as Inhibitors of
Autor: Elliot D, Mock, Ioli, Kotsogianni, Wouter P F, Driever, Carmen S, Fonseca, Jelle M, Vooijs, Hans, den Dulk, Constant A A, van Boeckel, Mario, van der Stelt
Publikováno v: Journal of Medicinal Chemistry
N-Acylphosphatidylethanolamine phospholipase D (NAPE-PLD) is regarded as the main enzyme responsible for the biosynthesis of N-acylethanolamines (NAEs), a family of bioactive lipid mediators. Previously, we reported N-(cyclopropylmethyl)-6-((S)-3-hyd
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::b75a1634a1c7ec431ec30ad31452d417
https://pubmed.ncbi.nlm.nih.gov/33382264
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7
Akademický článek
Org 214007-0: a novel non-steroidal selective glucocorticoid receptor modulator with full anti-inflammatory properties and improved therapeutic index.
Autor: Marie-José C van Lierop, Wynand Alkema, Anke J Laskewitz, Rein Dijkema, Hans M van der Maaden, Martin J Smit, Ralf Plate, Paolo G M Conti, Christan G J M Jans, C Marco Timmers, Constant A A van Boeckel, Scott J Lusher, Ross McGuire, Rene C van Schaik, Jacob de Vlieg, Ruben L Smeets, Claudia L Hofstra, Annemieke M H Boots, Marcel van Duin, Benno A Ingelse, Willem G E J Schoonen, Aldo Grefhorst, Theo H van Dijk, Folkert Kuipers, Wim H A Dokter
Publikováno v: PLoS ONE, Vol 7, Iss 11, p e48385 (2012)
Glucocorticoids (GCs) such as prednisolone are potent immunosuppressive drugs but suffer from severe adverse effects, including the induction of insulin resistance. Therefore, development of so-called Selective Glucocorticoid Receptor Modulators (SGR
Externí odkaz: https://doaj.org/article/6e9843e211b74a5b893e7e79339992e9
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8
Asymmetric Synthesis of Lysine Analogues with Reduced Basicity, and their Incorporation into Proteasome Inhibitors
Autor: Christoph Driessen, Eva J. van Rooden, Charlotte M J Wesseling, David Ward, Herman S. Overkleeft, Gerjan de Bruin, Constant A. A. van Boeckel, Bogdan I. Florea, Mario van der Stelt, Alexei F. Kisselev, Adrianus M. C. H. van den Nieuwendijk
Publikováno v: European Journal of Organic Chemistry. 2017:5921-5934
Most known β2 selective proteasome inhibitor suffer from relatively poor cell permeability as the result of a net positive charge caused by the basic moiety at P1. Here we describe the synthesis of oligopeptide vinyl sulfones that contain different
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ca695825f8341cd5419b9d728ca47238
https://doi.org/10.1002/ejoc.201701174
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9
The alkyne moiety as a latent electrophile in irreversible covalent small molecule inhibitors of Cathepsin K
Autor: Jure Loboda, Huib Ovaa, Elma Mons, Jill Hermans, Martijn Verdoes, Peter A. van Veelen, Boris Turk, Ineke D. C. Jansen, Dušan Turk, Bjorn R. van Doodewaerd, Constant A. A. van Boeckel
Publikováno v: Journal of the American Chemical Society, 141(8), 3507-3514. American Chemical Society
Journal of the American Chemical Society
Mons, E, Jansen, I D C, Loboda, J, van Doodewaerd, B R, Hermans, J, Verdoes, M, van Boeckel, C A A, van Veelen, P A, Turk, B, Turk, D & Ovaa, H 2019, ' The alkyne moiety as a latent electrophile in irreversible covalent small molecule inhibitors of Cathepsin K ', Journal of the American Chemical Society, vol. 141, no. 8, pp. 3507-3514 . https://doi.org/10.1021/jacs.8b11027
Journal of the American Chemical Society, 141, 8, pp. 3507-3514
Journal of the American Chemical Society, 141, 3507-3514
Journal of the American Chemical Society, 141(8), 3507-3514
Irreversible covalent inhibitors can have a beneficial pharmacokinetic/pharmacodynamics profile but are still often avoided due to the risk of indiscriminate covalent reactivity and the resulting adverse effects. To overcome this potential liability,
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::34621c0b43c4eedbb885bb9f31641ab6
https://dare.uva.nl/personal/pure/en/publications/the-alkyne-moiety-as-a-latent-electrophile-in-irreversible-covalent-small-molecule-inhibitors-of-cathepsin-k(c6648de6-11fb-4e6e-b618-732d075f73d1).html
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10
Drug Discovery Maps, a Machine Learning Model That Visualizes and Predicts Kinome–Inhibitor Interaction Landscapes
Autor: Mario van der Stelt, Ruud H. Wijdeven, Sebastian H. Grimm, Eelke B. Lenselink, Gerard J. P. van Westen, Constant A. A. van Boeckel, Jacques Neefjes, Antonius P A Janssen
Publikováno v: Journal of Chemical Information and Modeling, 59(3), 1221-1229
Journal of Chemical Information and Modeling
The interpretation of high-dimensional structure-activity data sets in drug discovery to predict ligand-protein interaction landscapes is a challenging task. Here we present Drug Discovery Maps (DDM), a machine learning model that maps the activity p
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bcedc0d253974eb16b4a35cae9de6692
http://hdl.handle.net/1887/75291
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