Amelioration of autoimmunity with an inhibitor selectively targeting all active centres of the immunoproteasome
Basler, Michael, Maurits, Elmer, Bruin, Gerjan, Koerner, Julia, Overkleeft, Herman S, Groettrup, Marcus
Published in British journal of pharmacology (01.01.2018)
Published in British journal of pharmacology (01.01.2018)
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Journal Article
A Set of Activity-Based Probes to Visualize Human (Immuno)proteasome Activities
de Bruin, Gerjan, Xin, Bo Tao, Kraus, Marianne, van der Stelt, Mario, van der Marel, Gijsbert A., Kisselev, Alexei F., Driessen, Christoph, Florea, Bogdan I., Overkleeft, Herman S.
Published in Angewandte Chemie (International ed.) (18.03.2016)
Published in Angewandte Chemie (International ed.) (18.03.2016)
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Journal Article
Proteasome Subunit Selective Activity-Based Probes Report on Proteasome Core Particle Composition in a Native Polyacrylamide Gel Electrophoresis Fluorescence-Resonance Energy Transfer Assay
de Bruin, Gerjan, Xin, Bo-Tao, Florea, Bogdan I, Overkleeft, Herman S
Published in Journal of the American Chemical Society (10.08.2016)
Published in Journal of the American Chemical Society (10.08.2016)
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Journal Article
Two‐Step Bioorthogonal Activity‐Based Protein Profiling of Individual Human Proteasome Catalytic Sites
Xin, Bo‐Tao, Espinal, Christofer, Bruin, Gerjan, Filippov, Dmitri V., Marel, Gijsbert A., Florea, Bogdan I., Overkleeft, Herman S.
Published in Chembiochem : a European journal of chemical biology (15.01.2020)
Published in Chembiochem : a European journal of chemical biology (15.01.2020)
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Journal Article
Proteasome Inhibition in Multiple Myeloma: Head-to-Head Comparison of Currently Available Proteasome Inhibitors
Besse, Andrej, Besse, Lenka, Kraus, Marianne, Mendez-Lopez, Max, Bader, Jürgen, Xin, Bo-Tao, de Bruin, Gerjan, Maurits, Elmer, Overkleeft, Herman S, Driessen, Christoph
Published in Cell chemical biology (21.03.2019)
Published in Cell chemical biology (21.03.2019)
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Journal Article
Inhibition of the Proteasome β2 Site Sensitizes Triple-Negative Breast Cancer Cells to β5 Inhibitors and Suppresses Nrf1 Activation
Weyburne, Emily S., Wilkins, Owen M., Sha, Zhe, Williams, David A., Pletnev, Alexandre A., de Bruin, Gerjan, Overkleeft, Hermann S., Goldberg, Alfred L., Cole, Michael D., Kisselev, Alexei F.
Published in Cell chemical biology (16.02.2017)
Published in Cell chemical biology (16.02.2017)
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Journal Article
The novel β2-selective proteasome inhibitor LU-102 synergizes with bortezomib and carfilzomib to overcome proteasome inhibitor resistance of myeloma cells
Kraus, Marianne, Bader, Juergen, Geurink, Paul P, Weyburne, Emily S, Mirabella, Anne C, Silzle, Tobias, Shabaneh, Tamer B, van der Linden, Wouter A, de Bruin, Gerjan, Haile, Sarah R, van Rooden, Eva, Appenzeller, Christina, Li, Nan, Kisselev, Alexei F, Overkleeft, Herman, Driessen, Christoph
Published in Haematologica (Roma) (01.10.2015)
Published in Haematologica (Roma) (01.10.2015)
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Journal Article
Potency and Selectivity of BTK Inhibitors in Clinical Development for B-Cell Malignancies
Kaptein, Allard, de Bruin, Gerjan, Emmelot-van Hoek, Maaike, van de Kar, Bas, de Jong, Anouk, Gulrajani, Michael, Demont, Dennis, Covey, Todd, Mittag, Diana, Barf, Tjeerd
Published in Blood (29.11.2018)
Published in Blood (29.11.2018)
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Journal Article
A Set of Activity-Based Probes to Visualize Human (Immuno)proteasome Activities
de Bruin, Gerjan, Xin, Bo Tao, Kraus, Marianne, van der Stelt, Mario, van der Marel, Gijsbert A., Kisselev, Alexei F., Driessen, Christoph, Florea, Bogdan I., Overkleeft, Herman S.
Published in Angewandte Chemie (18.03.2016)
Published in Angewandte Chemie (18.03.2016)
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Journal Article
Identification and Characterization of ACP-5862, the Major Circulating Active Metabolite of Acalabrutinib: Both Are Potent and Selective Covalent Bruton Tyrosine Kinase Inhibitors
Podoll, Terry, Pearson, Paul G, Kaptein, Allard, Evarts, Jerry, de Bruin, Gerjan, Emmelot-van Hoek, Maaike, de Jong, Anouk, van Lith, Bart, Sun, Hao, Byard, Stephen, Fretland, Adrian, Hoogenboom, Niels, Barf, Tjeerd, Slatter, J Greg
Published in The Journal of pharmacology and experimental therapeutics (01.01.2023)
Published in The Journal of pharmacology and experimental therapeutics (01.01.2023)
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Journal Article
Structure-Based Design of beta 1i or beta 5i Specific Inhibitors of Human Immunoproteasomes
de Bruin, Gerjan, Huber, Eva M., Xin, Bo-Tao, van Rooden, Eva J., Al-Ayed, Karol, Kim, Kyung-Bo, Kisselev, Alexei F., Driessen, Christoph, van der Stelt, Mario, van der Marel, Gijsbert A., Groll, Michael, Overkleeft, Herman S.
Published in Journal of medicinal chemistry (24.07.2014)
Published in Journal of medicinal chemistry (24.07.2014)
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Journal Article
Mutational profile in previously treated patients with chronic lymphocytic leukemia progression on acalabrutinib or ibrutinib
Woyach, Jennifer A., Jones, Daniel, Jurczak, Wojciech, Robak, Tadeusz, Illés, Árpád, Kater, Arnon P., Ghia, Paolo, Byrd, John C., Seymour, John F., Long, Susan, Mohamed, Nehad, Benrashid, Samon, Lai, Tzung-Huei, De Jesus, Gary, Lai, Richard, de Bruin, Gerjan, Rule, Simon, Munugalavadla, Veerendra
Published in Blood (05.09.2024)
Published in Blood (05.09.2024)
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Journal Article
Structure-Based Design of Inhibitors Selective for Human Proteasome beta 2c or beta 2i Subunits
Xin, Bo-Tao, Huber, Eva M., de Bruin, Gerjan, Heinemeyer, Wolfgang, Maurits, Elmer, Espinal, Christofer, Du, Yimeng, Janssens, Marissa, Weyburne, Emily S., Kisselev, Alexei F., Florea, Bogdan I., Driessen, Christoph, van der Marel, Gijsbert A., Groll, Michael, Overkleeft, Herman S.
Published in Journal of medicinal chemistry (14.02.2019)
Published in Journal of medicinal chemistry (14.02.2019)
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Journal Article
Systematic Analyses of Substrate Preferences of 20S Proteasomes Using Peptidic Epoxyketone Inhibitors
Huber, Eva M, de Bruin, Gerjan, Heinemeyer, Wolfgang, Paniagua Soriano, Guillem, Overkleeft, Herman S, Groll, Michael
Published in Journal of the American Chemical Society (24.06.2015)
Published in Journal of the American Chemical Society (24.06.2015)
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Journal Article
Defining the Most Effective Proteasome Inhibition in Multiple Myeloma: Head-to-Head Comparison of Currently Available Proteasome Inhibitors
Besse, Andrej, Besse, Lenka, Kraus, Marianne, Bader, Juergen, de Bruin, Gerjan, Overkleeft, Herman S, Driessen, Christoph
Published in Blood (08.12.2017)
Published in Blood (08.12.2017)
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Journal Article
Structure-Based Design of β1i or β5i Specific Inhibitors of Human Immunoproteasomes
de Bruin, Gerjan, Huber, Eva M, Xin, Bo-Tao, van Rooden, Eva J, Al-Ayed, Karol, Kim, Kyung-Bo, Kisselev, Alexei F, Driessen, Christoph, van der Stelt, Mario, van der Marel, Gijsbert A, Groll, Michael, Overkleeft, Herman S
Published in Journal of medicinal chemistry (24.07.2014)
Published in Journal of medicinal chemistry (24.07.2014)
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Journal Article
Immunoproteasomal Inhibition With ONX-0914 Attenuates Atherosclerosis and Reduces White Adipose Tissue Mass and Metabolic Syndrome in Mice
Schaftenaar, Frank H, van Dam, Andrea D, de Bruin, Gerjan, Depuydt, Marie A C, de Mol, Jill, Amersfoort, Jacob, Douna, Hidde, Meijer, Menno, Kröner, Mara J, van Santbrink, Peter J, Bernabé Kleijn, Mireia N A, van Puijvelde, Gijs H M, Florea, Bogdan I, Slütter, Bram, Foks, Amanda C, Bot, Ilze, Rensen, Patrick C N, Kuiper, Johan
Published in Arteriosclerosis, thrombosis, and vascular biology (01.06.2024)
Published in Arteriosclerosis, thrombosis, and vascular biology (01.06.2024)
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Journal Article
Structure-Based Design of Inhibitors Selective for Human Proteasome β2c or β2i Subunits
Xin, Bo-Tao, Huber, Eva M, de Bruin, Gerjan, Heinemeyer, Wolfgang, Maurits, Elmer, Espinal, Christofer, Du, Yimeng, Janssens, Marissa, Weyburne, Emily S, Kisselev, Alexei F, Florea, Bogdan I, Driessen, Christoph, van der Marel, Gijsbert A, Groll, Michael, Overkleeft, Herman S
Published in Journal of medicinal chemistry (14.02.2019)
Published in Journal of medicinal chemistry (14.02.2019)
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Journal Article