The Alkyne Moiety as a Latent Electrophile in Irreversible Covalent Small Molecule Inhibitors of Cathepsin K
Mons, Elma, Jansen, Ineke D. C, Loboda, Jure, van Doodewaerd, Bjorn R, Hermans, Jill, Verdoes, Martijn, van Boeckel, Constant A. A, van Veelen, Peter A, Turk, Boris, Turk, Dusan, Ovaa, Huib
Published in Journal of the American Chemical Society (27.02.2019)
Published in Journal of the American Chemical Society (27.02.2019)
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A Natural-Product Switch for a Dynamic Protein Interface
Scheepstra, Marcel, Nieto, Lidia, Hirsch, Anna K. H., Fuchs, Sascha, Leysen, Seppe, Lam, Chan Vinh, in het Panhuis, Leslie, van Boeckel, Constant A. A., Wienk, Hans, Boelens, Rolf, Ottmann, Christian, Milroy, Lech-Gustav, Brunsveld, Luc
Published in Angewandte Chemie (International ed.) (16.06.2014)
Published in Angewandte Chemie (International ed.) (16.06.2014)
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A Modular Strategy Toward the Synthesis of Heparin-like Oligosaccharides Using Monomeric Building Blocks in a Sequential Glycosylation Strategy
Codée, Jeroen D. C, Stubba, Bas, Schiattarella, Marialuisa, Overkleeft, Herman S, van Boeckel, Constant A. A, van Boom, Jacques H, van der Marel, Gijsbert A
Published in Journal of the American Chemical Society (23.03.2005)
Published in Journal of the American Chemical Society (23.03.2005)
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Drug Discovery Maps, a Machine Learning Model That Visualizes and Predicts Kinome–Inhibitor Interaction Landscapes
Janssen, Antonius P. A, Grimm, Sebastian H, Wijdeven, Ruud H. M, Lenselink, Eelke B, Neefjes, Jacques, van Boeckel, Constant A. A, van Westen, Gerard J. P, van der Stelt, Mario
Published in Journal of chemical information and modeling (25.03.2019)
Published in Journal of chemical information and modeling (25.03.2019)
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From heparin to EP217609: the long way to a new pentasaccharide-based neutralisable anticoagulant with an unprecedented pharmacological profile
Petitou, Maurice, Nancy-Portebois, Vanessa, Dubreucq, Guy, Motte, Vincent, Meuleman, Dick, de Kort, Martin, van Boeckel, Constant A A, Vogel, Gerard M T, Wisse, Jeffry A J
Published in Thrombosis and haemostasis (01.11.2009)
Published in Thrombosis and haemostasis (01.11.2009)
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Journal Article
Discovery of isoquinoline sulfonamides as allosteric gyrase inhibitors with activity against fluoroquinolone-resistant bacteria
Bakker, Alexander T., Kotsogianni, Ioli, Avalos, Mariana, Punt, Jeroen M., Liu, Bing, Piermarini, Diana, Gagestein, Berend, Slingerland, Cornelis J., Zhang, Le, Willemse, Joost J., Ghimire, Leela B., van den Berg, Richard J. H. B. N., Janssen, Antonius P. A., Ottenhoff, Tom H. M., van Boeckel, Constant A. A., van Wezel, Gilles P., Ghilarov, Dmitry, Martin, Nathaniel I., van der Stelt, Mario
Published in Nature chemistry (01.09.2024)
Published in Nature chemistry (01.09.2024)
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Journal Article
A Synthetic Antithrombin III Binding Pentasaccharide Is Now a Drug! What Comes Next?
Petitou, Maurice, van Boeckel, Constant A. A.
Published in Angewandte Chemie (International ed.) (14.06.2004)
Published in Angewandte Chemie (International ed.) (14.06.2004)
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Journal Article
Identification and Development of Biphenyl Substituted Iminosugars as Improved Dual Glucosylceramide Synthase/Neutral Glucosylceramidase Inhibitors
Ghisaidoobe, Amar T, van den Berg, Richard J. B. H. N, Butt, Saleem S, Strijland, Anneke, Donker-Koopman, Wilma E, Scheij, Saskia, van den Nieuwendijk, Adrianus M. C. H, Koomen, Gerrit-Jan, van Loevezijn, Arnold, Leemhuis, Mark, Wennekes, Tom, van der Stelt, Mario, van der Marel, Gijsbert A, van Boeckel, Constant A. A, Aerts, Johannes M. F. G, Overkleeft, Herman S
Published in Journal of medicinal chemistry (13.11.2014)
Published in Journal of medicinal chemistry (13.11.2014)
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Journal Article
Epi-Cyclophellitol Cyclosulfate, a Mechanism-Based Endoplasmic Reticulum α‑Glucosidase II Inhibitor, Blocks Replication of SARS-CoV‑2 and Other Coronaviruses
Thaler, Melissa, Ofman, Tim P., Kok, Ken, Heming, Jurriaan J. A., Moran, Elisha, Pickles, Isabelle, Leijs, Anouk A., van den Nieuwendijk, Adrianus M. C. H., van den Berg, Richard J. B. H. N., Ruijgrok, Gijs, Armstrong, Zachary, Salgado-Benvindo, Clarisse, Ninaber, Dennis K., Snijder, Eric J., van Boeckel, Constant A. A., Artola, Marta, Davies, Gideon J., Overkleeft, Herman S., van Hemert, Martijn J.
Published in ACS central science (28.08.2024)
Published in ACS central science (28.08.2024)
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Conjugation of ATIII-Binding Pentasaccharides to Extend the Half-Life of Proteins: Long-Acting Insulin
de Kort, Martin, Gianotten, Bas, Wisse, Jeffry A. J., Bos, Ebo S., Eppink, Michel H. M., Mattaar, Ellen, Vogel, Gerard M. T., Dokter, Wim H. A., Honing, Maarten, Vonsovic, Stanislava, Smit, Martin-Jan, Wijkmans, Jac C. H. M., van Boeckel, Constant A. A.
Published in ChemMedChem (18.08.2008)
Published in ChemMedChem (18.08.2008)
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Journal Article
Structure–Activity Relationship Studies of Aryl Sulfoxides as Reversible Monoacylglycerol Lipase Inhibitors
Jiang, Ming, Huizenga, Mirjam C. W., Mohr, Florian, Amedi, Avand, Bakker, Renze, van den Berg, Richard J. B. H. N., Deng, Hui, van der Wel, Tom, van Boeckel, Constant A.A., van der Stelt, Mario
Published in Journal of medicinal chemistry (25.07.2024)
Published in Journal of medicinal chemistry (25.07.2024)
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Journal Article
Discovery of a NAPE-PLD inhibitor that modulates emotional behavior in mice
Mock, Elliot D., Mustafa, Mohammed, Gunduz-Cinar, Ozge, Cinar, Resat, Petrie, Gavin N., Kantae, Vasudev, Di, Xinyu, Ogasawara, Daisuke, Varga, Zoltan V., Paloczi, Janos, Miliano, Cristina, Donvito, Giulia, van Esbroeck, Annelot C. M., van der Gracht, Anouk M. F., Kotsogianni, Ioli, Park, Joshua K., Martella, Andrea, van der Wel, Tom, Soethoudt, Marjolein, Jiang, Ming, Wendel, Tiemen J., Janssen, Antonius P. A., Bakker, Alexander T., Donovan, Colleen M., Castillo, Laura I., Florea, Bogdan I., Wat, Jesse, van den Hurk, Helma, Wittwer, Matthias, Grether, Uwe, Holmes, Andrew, van Boeckel, Constant A. A., Hankemeier, Thomas, Cravatt, Benjamin F., Buczynski, Matthew W., Hill, Matthew N., Pacher, Pal, Lichtman, Aron H., van der Stelt, Mario
Published in Nature chemical biology (01.06.2020)
Published in Nature chemical biology (01.06.2020)
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Journal Article
Structure-Activity Relationship Studies of Pyrimidine-4-Carboxamides as Inhibitors of N-Acylphosphatidylethanolamine Phospholipase D
Mock, Elliot D., Kotsogianni, Ioli, Driever, Wouter P. F., Fonseca, Carmen S., Vooijs, Jelle M., den Dulk, Hans, van Boeckel, Constant A. A., van der Stelt, Mario
Published in Journal of medicinal chemistry (14.01.2021)
Published in Journal of medicinal chemistry (14.01.2021)
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Journal Article
Comprehensive structure-activity-relationship of azaindoles as highly potent FLT3 inhibitors
Grimm, Sebastian H., Gagestein, Berend, Keijzer, Jordi F., Liu, Nora, Wijdeven, Ruud H., Lenselink, Eelke B., Tuin, Adriaan W., van den Nieuwendijk, Adrianus M.C.H., van Westen, Gerard J.P., van Boeckel, Constant A.A., Overkleeft, Herman S., Neefjes, Jacques, van der Stelt, Mario
Published in Bioorganic & medicinal chemistry (01.03.2019)
Published in Bioorganic & medicinal chemistry (01.03.2019)
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Journal Article
Surface Plasmon Resonance Evaluation of Various Aminoglycoside-RNA Hairpin Interactions Reveals Low Degree of Selectivity
Verhelst, Steven H.L, Michiels, Paul J.A, van der Marel, Gijsbert A, van Boeckel, Constant A.A, van Boom, Jacques H
Published in Chembiochem : a European journal of chemical biology (05.07.2004)
Published in Chembiochem : a European journal of chemical biology (05.07.2004)
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Journal Article
Asymmetric Synthesis of Lysine Analogues with Reduced Basicity, and their Incorporation into Proteasome Inhibitors
de Bruin, Gerjan, van Rooden, Eva J., Ward, David, Wesseling, Charlotte, van den Nieuwendijk, Adrianus M. C. H., van Boeckel, Constant A. A., Driessen, Christoph, Kisselev, Alexei F., Florea, Bogdan I., van der Stelt, Mario, Overkleeft, Herman S.
Published in European journal of organic chemistry (25.10.2017)
Published in European journal of organic chemistry (25.10.2017)
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Journal Article
Synthetic heparin derivatives as new anticoagulant drugs
de Kort, Martin, Buijsman, Rogier C., van Boeckel, Constant A.A.
Published in Drug discovery today (01.06.2005)
Published in Drug discovery today (01.06.2005)
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Journal Article
Unique Overlap in the Prerequisites for Thrombin Inhibition and Oral Bioavailability Resulting in Potent Oral Antithrombotics
Adang, Anton E. P, de Man, Adrianus P. A, Vogel, Gerard M. T, Grootenhuis, Peter D. J, Smit, Martin J, Peters, Co A. M, Visser, Arie, Rewinkel, Jos B. M, van Dinther, Theo, Lucas, Hans, Kelder, Jan, van Aelst, Sjoerd, Meuleman, Dick G, van Boeckel, Constant A. A
Published in Journal of medicinal chemistry (26.09.2002)
Published in Journal of medicinal chemistry (26.09.2002)
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Journal Article
Fondaparinux, a Synthetic Pentasaccharide: The First in a New Class of Antithrombotic Agents — The Selective Factor Xa Inhibitors
Bauer, Kenneth A., Hawkins, David W., Peters, Paul C., Petitou, Maurice, Herbert, Jean‐Marc, Boeckel, Constant A. A., Meuleman, Dirk G.
Published in Cardiovascular drug reviews (01.03.2002)
Published in Cardiovascular drug reviews (01.03.2002)
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