Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia
Byrd, John C, Harrington, Bonnie, O’Brien, Susan, Jones, Jeffrey A, Schuh, Anna, Devereux, Steve, Chaves, Jorge, Wierda, William G, Awan, Farrukh T, Brown, Jennifer R, Hillmen, Peter, Stephens, Deborah M, Ghia, Paolo, Barrientos, Jacqueline C, Pagel, John M, Woyach, Jennifer, Johnson, Dave, Huang, Jane, Wang, Xiaolin, Kaptein, Allard, Lannutti, Brian J, Covey, Todd, Fardis, Maria, McGreivy, Jesse, Hamdy, Ahmed, Rothbaum, Wayne, Izumi, Raquel, Diacovo, Thomas G, Johnson, Amy J, Furman, Richard R
Published in The New England journal of medicine (28.01.2016)
Published in The New England journal of medicine (28.01.2016)
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Journal Article
The Bruton Tyrosine Kinase (BTK) Inhibitor Acalabrutinib Demonstrates Potent On-Target Effects and Efficacy in Two Mouse Models of Chronic Lymphocytic Leukemia
Herman, Sarah E M, Montraveta, Arnau, Niemann, Carsten U, Mora-Jensen, Helena, Gulrajani, Michael, Krantz, Fanny, Mantel, Rose, Smith, Lisa L, McClanahan, Fabienne, Harrington, Bonnie K, Colomer, Dolors, Covey, Todd, Byrd, John C, Izumi, Raquel, Kaptein, Allard, Ulrich, Roger, Johnson, Amy J, Lannutti, Brian J, Wiestner, Adrian, Woyach, Jennifer A
Published in Clinical cancer research (01.06.2017)
Published in Clinical cancer research (01.06.2017)
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Chemical genetics strategy to profile kinase target engagement reveals role of FES in neutrophil phagocytosis
van der Wel, Tom, Hilhorst, Riet, den Dulk, Hans, van den Hooven, Tim, Prins, Nienke M., Wijnakker, Joost A. P. M., Florea, Bogdan I., Lenselink, Eelke B., van Westen, Gerard J. P., Ruijtenbeek, Rob, Overkleeft, Herman S., Kaptein, Allard, Barf, Tjeerd, van der Stelt, Mario
Published in Nature communications (25.06.2020)
Published in Nature communications (25.06.2020)
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Journal Article
Preclinical Evaluation of the Novel BTK Inhibitor Acalabrutinib in Canine Models of B-Cell Non-Hodgkin Lymphoma
Harrington, Bonnie K, Gardner, Heather L, Izumi, Raquel, Hamdy, Ahmed, Rothbaum, Wayne, Coombes, Kevin R, Covey, Todd, Kaptein, Allard, Gulrajani, Michael, Van Lith, Bart, Krejsa, Cecile, Coss, Christopher C, Russell, Duncan S, Zhang, Xiaoli, Urie, Bridget K, London, Cheryl A, Byrd, John C, Johnson, Amy J, Kisseberth, William C
Published in PloS one (19.07.2016)
Published in PloS one (19.07.2016)
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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
Inhibition of cyclo-oxygenase 2 expression in colon cells by the chemopreventive agent curcumin involves inhibition of NF-κB activation via the NIK/IKK signalling complex
PLUMMER, S. M, HOLLOWAY, K. A, MANSON, M. M, MUNKS, R. J. L, KAPTEIN, A, FARROW, S, HOWELLS, L
Published in Oncogene (28.10.1999)
Published in Oncogene (28.10.1999)
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In vivo knockdown of TAK1 accelerates bone marrow proliferation/differentiation and induces systemic inflammation
Vink, Paul M, Smout, Wendy M, Driessen-Engels, Lilian J, de Bruin, Alex M, Delsing, Dianne, Krajnc-Franken, Magda A, Jansen, Aswin J, Rovers, Eric F, van Puijenbroek, André A, Kaptein, Allard, Nolte, Martijn A, Garritsen, Anja, van Eenennaam, Hans
Published in PloS one (07.03.2013)
Published in PloS one (07.03.2013)
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Journal Article
Acalabrutinib (ACP-196): A Covalent Bruton Tyrosine Kinase Inhibitor with a Differentiated Selectivity and In Vivo Potency Profile
Barf, Tjeerd, Covey, Todd, Izumi, Raquel, van de Kar, Bas, Gulrajani, Michael, van Lith, Bart, van Hoek, Maaike, de Zwart, Edwin, Mittag, Diana, Demont, Dennis, Verkaik, Saskia, Krantz, Fanny, Pearson, Paul G, Ulrich, Roger, Kaptein, Allard
Published in The Journal of pharmacology and experimental therapeutics (01.11.2017)
Published in The Journal of pharmacology and experimental therapeutics (01.11.2017)
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Journal Article
Studies on the interaction between TWEAK and the death receptor WSL-1/TRAMP (DR3)
Kaptein, Allard, Jansen, Mieke, Dilaver, Gonul, Kitson, Jeremy, Dash, Laura, Wang, Edward, Owen, Michael J, Bodmer, Jean-Luc, Tschopp, Jurg, Farrow, Stuart N
Published in FEBS letters (24.11.2000)
Published in FEBS letters (24.11.2000)
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Journal Article
Discovery and optimization of covalent EGFR T790M/L858R mutant inhibitors
Hoogenboom, Niels, Demont, Dennis, de Zwart, Edwin, Verkaik, Saskia, Emmelot, Maaike, van de Kar, Bas, Kaptein, Allard, Barf, Tjeerd
Published in Bioorganic & medicinal chemistry letters (15.11.2021)
Published in Bioorganic & medicinal chemistry letters (15.11.2021)
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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
Discovery of quinoline-based irreversible BTK inhibitors
de Bruin, Gerjan, Demont, Dennis, de Zwart, Edwin, Verkaik, Saskia, Hoogenboom, Niels, van de Kar, Bas, van Lith, Bart, Emmelot- van Hoek, Maaike, Gulrajani, Michael, Covey, Todd, Kaptein, Allard, Barf, Tjeerd
Published in Bioorganic & medicinal chemistry letters (15.07.2020)
Published in Bioorganic & medicinal chemistry letters (15.07.2020)
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Journal Article
Abstract 2194: Preclinical pharmacological profiling of ACP-5862, the major metabolite of the covalent BTK inhibitor acalabrutinib, displays intrinsic BTK inhibitory activity
Kaptein, Allard, Podoll, Terry, Bruin, Gerjan de, Hoek, Maaike Emmelot-van, Jong, Anouk de, Lith, Bart van, Hoogenboom, Niels, Barf, Tjeerd, Ware, Joseph, Slatter, J. Greg
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Journal Article
Abstract 4049: Preclinical pharmacology profile of GTX-0196: A novel, potent and highly selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of hematologic malignancies
Kaptein, Allard, Lain, Sonia, Brunen, Diede, van Wezel, Edward, Barf, Tjeerd
Published in Cancer research (Chicago, Ill.) (15.06.2022)
Published in Cancer research (Chicago, Ill.) (15.06.2022)
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Journal Article
Direct and two-step bioorthogonal probes for Bruton's tyrosine kinase based on ibrutinib: a comparative study
Liu, Nora, Hoogendoorn, Sascha, van de Kar, Bas, Kaptein, Allard, Barf, Tjeerd, Driessen, Christoph, Filippov, Dmitri V., van der Marel, Gijsbert A., van der Stelt, Mario, Overkleeft, Herman S.
Published in Organic & biomolecular chemistry (14.05.2015)
Published in Organic & biomolecular chemistry (14.05.2015)
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Journal Article
Pharmacodynamic Evaluation of Acalabrutinib in Relapsed/Refractory and Treatment-Naive Patients with Chronic Lymphocytic Leukemia (CLL) in the Phase 1/2 ACE-CL-001 Study
Covey, Todd, Gulranjani, Michael, Cheung, Jean, Bibikova, Elena, Clevenger, Tracy, Krantz, Fanny, Pan, Karen, Yamaguchi, Kyoko, De Jong, Anouk, Van Lith, Bart, Mittag, Diana, Izumi, Raquel, Byrd, John C., Wierda, William G, O'Brien, Susan M., Furman, Richard R., Kaptein, Allard
Published in Blood (08.12.2017)
Published in Blood (08.12.2017)
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Journal Article
Potency and Selectivity of BTK Inhibitors in Clinical Development for B-Cell Malignancies
Kaptein, Allard, de Bruin, Gerjan, Hoek, Maaike Emmelot-van, van de Kar, Bas, de Jong, Anouk, Gulrajani, Michael, Demont, Dennis, Covey, Todd, Mittag, Diana, Barf, Tjeerd
Published in Clinical lymphoma, myeloma and leukemia (01.09.2019)
Published in Clinical lymphoma, myeloma and leukemia (01.09.2019)
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