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Irreversible protein kinase inhibitors: balancing the benefits and risks

Barf, Tjeerd ; Kaptein, Allard

Journal of medicinal chemistry, 26 July 2012, Vol.55(14), pp.6243-62 [Peer Reviewed Journal]

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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

PloS one, 2013, Vol.8(3), pp.e57348 [Peer Reviewed Journal]

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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 Richards, Kristy L. (editor)

PLoS ONE, 2016, Vol.11(7) [Peer Reviewed Journal]

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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

Clinical cancer research : an official journal of the American Association for Cancer Research, 01 June 2017, Vol.23(11), pp.2831-2841 [Peer Reviewed Journal]

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Severity of murine collagen‐induced arthritis correlates with increased CYP7B activity: Enhancement of dehydroepiandrosterone metabolism by interleukin‐1β

Dulos, John ; Verbraak, Evert ; Bagchus, Wilma M. ; Boots, Annemieke M. H. ; Kaptein, Allard

Arthritis & Rheumatism, October 2004, Vol.50(10), pp.3346-3353 [Peer Reviewed Journal]

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Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series

Oubrie, Arthur ; Kaptein, Allard ; de Zwart, Edwin ; Hoogenboom, Niels ; Goorden, Rianne ; van de Kar, Bas ; van Hoek, Maaike ; de Kimpe, Vera ; van Der Heijden, Ruud ; Borsboom, Judith ; Kazemier, Bert ; de Roos, Jeroen ; Scheffers, Michiel ; Lommerse, Jos ; Schultz-Fademrecht, Carsten ; Barf, Tjeerd

Bioorganic & Medicinal Chemistry Letters, 01 January 2012, Vol.22(1), pp.613-618 [Peer Reviewed Journal]

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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

The Journal of pharmacology and experimental therapeutics, November 2017, Vol.363(2), pp.240-252 [Peer Reviewed Journal]

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Tumour necrosis factor-alpha stimulates dehydroepiandrosterone metabolism in human fibroblast-like synoviocytes: a role for nuclear factor-kappaB and activator protein-1 in the regulation of expression of cytochrome p450 enzyme 7b

Dulos, John ; Kaptein, Allard ; Kavelaars, Annemieke ; Heijnen, Cobi ; Boots, Annemieke

Arthritis research & therapy, 2005, Vol.7(6), pp.R1271-80 [Peer Reviewed Journal]

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The IL1 receptor accessory protein is responsible for the recruitment of the interleukin-1 receptor associated kinase to the IL1/IL1 receptor I complex

Volpe, Filippo ; Clatworthy, Jonathan ; Kaptein, Allard ; Maschera, Barbara ; Griffin, Anne-Marie ; Ray, Keith

FEBS Letters, 1997, Vol.419(1), pp.41-44 [Peer Reviewed Journal]

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10
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Discovery of 8-Amino-imidazo[1,5- a ]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis

Liu, Jian ; Guiadeen, Deodial ; Krikorian, Arto ; Gao, Xiaolei ; Wang, James ; Boga, Sobhana Babu ; Alhassan, Abdul-Basit ; Yu, Younong ; Vaccaro, Henry ; Liu, Shilan ; Yang, Chundao ; Wu, Hao ; Cooper, Alan ; de Man, Jos ; Kaptein, Allard ; Maloney, Kevin ; Hornak, Viktor ; Gao, Ying-Duo ; Fischmann, Thierry O ; Raaijmakers, Hans ; Vu-Pham, Diep ; Presland, Jeremy ; Mansueto, My ; Xu, Zangwei ; Leccese, Erica ; Zhang-Hoover, Jie ; Knemeyer, Ian ; Garlisi, Charles G ; Bays, Nathan ; Stivers, Peter ; Brandish, Philip E ; Hicks, Alexandra ; Kim, Ronald ; Kozlowski, Joseph A Argonne National Lab. (Anl), Argonne, Il (United States). Advanced Photon Source (APS) (Corporate Author)

ACS Medicinal Chemistry Letters, 11 February 2016, Vol.7(2) [Peer Reviewed Journal]

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11
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Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors

Kaptein, Allard ; Oubrie, Arthur ; Zwart, Edwin de ; Hoogenboom, Niels ; Wit, Joeri de ; Kar, Bas van de ; Hoek, Maaike van ; Vogel, Gerard ; Kimpe, Vera de ; Schultz-Fademrecht, Carsten ; Borsboom, Judith ; Zeeland, Mario van ; Versteegh, Judith ; Kazemier, Bert ; Roos, Jeroen de ; Wijnands, Frank ; Dulos, John ; Jaeger, Martin ; Leandro-Garcia, Paula ; Barf, Tjeerd

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(12), pp.3823-3827 [Peer Reviewed Journal]

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12
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Structure-based lead identification of ATP-competitive MK2 inhibitors

Barf, Tjeerd ; Kaptein, Allard ; Wilde, Sander de ; Heijden, Ruud van Der ; Someren, Richard van ; Demont, Dennis ; Schultz-Fademrecht, Carsten ; Versteegh, Judith ; Zeeland, Mario van ; Seegers, Nicole ; Kazemier, Bert ; Kar, Bas van de ; Hoek, Maaike van ; Roos, Jeroen de ; Klop, Henri ; Smeets, Ruben ; Hofstra, Claudia ; Hornberg, Jorrit ; Oubrie, Arthur

Bioorganic & Medicinal Chemistry Letters, 2011, Vol.21(12), pp.3818-3822 [Peer Reviewed Journal]

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13
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6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile as cathepsin S inhibitors

Cai, Jiaqiang ; Baugh, Mark ; Black, Darcey ; Long, Clive ; Jonathan Bennett, D ; Dempster, Maureen ; Fradera, Xavier ; Gillespie, Jonathan ; Andrews, Fiona ; Boucharens, Sylviane ; Bruin, John ; Cameron, Kenneth S ; Cumming, Iain ; Hamilton, William ; Jones, Philip S ; Kaptein, Allard ; Kinghorn, Emma ; Maidment, Maurice ; Martin, Iain ; Mitchell, Ann

Bioorganic & Medicinal Chemistry Letters, 01 August 2010, Vol.20(15), pp.4350-4354 [Peer Reviewed Journal]

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14
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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

FEBS Letters, 2000, Vol.485(2), pp.135-141 [Peer Reviewed Journal]

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15
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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

The New England journal of medicine, 28 January 2016, Vol.374(4), pp.323-32 [Peer Reviewed Journal]

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16
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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

Clinical Lymphoma, Myeloma and Leukemia, September 2019, Vol.19, pp.S316-S317 [Peer Reviewed Journal]

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17
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No Effect of Fibrates on Synthesis of Apolipoprotein(a) in Primary Cultures of Cynomolgus Monkey and Human Hepatocytes: Apolipoprotein A-I Synthesis Increased

Neele, Diana M ; Kaptein, Allard ; Huisman, Holger ; de Wit, Elly C.M ; Princen, Hans M.G

Biochemical and Biophysical Research Communications, 17 March 1998, Vol.244(2), pp.374-378 [Peer Reviewed Journal]

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18
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Apolipoprotein E polymorphism affects plasma levels of lipoprotein(a)

de Knijff, Peter ; Kaptein, Allard ; Boomsma, Dorret ; Princen, Hans M.G ; Frants, Rune R ; Havekes, Louis M

Atherosclerosis, 1991, Vol.90(2), pp.169-174 [Peer Reviewed Journal]

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19
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Butyrate stimulates the secretion of apolipoprotein B-100-containing lipoproteins from HepG2 cells by inhibiting the intracellular degradation

Kaptein, Allard ; de Wit, Elly C.M ; Princen, Hans M.G

Biochimica et Biophysica Acta (BBA)/Lipids and Lipid Metabolism, 1994, Vol.1213(3), pp.349-356

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20
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U.S. Patent and Trademark Office Receives Patent Application for Method for Inhibiting Binding to B-Cell Receptor from Farrow Stuart Neville, Kaptein Allard, Kitson Jeremy David Alisdair, Winder Alison Janet and Glaxo Group Limited

Global IP News. Pharmaceutical Patent News, Mar 7, 2014

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21
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Acerta Pharma BV Files Taiwan Patent Application for Therapeutic Combinations of a BTK Inhibitor, a Pi3k Inhibitor and/or a Jak-2 Inhibitor

Global IP News. Pharmaceutical Patent News, Oct 5, 2016

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22
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U.S. Patent and Trademark Office Publishes Acerta Pharma's Patent Application for Therapeutic Combinations of an Irak4 Inhibitor and a BTK Inhibitor

Global IP News. Pharmaceutical Patent News, Mar 8, 2020

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23
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Acerta Pharma BV Submits Patent Application for Methods of Treating Chronic Lymphocytic Leukemia and Small Lymphocytic Leukemia Using a BTK Inhibitor

Global IP News. Pharmaceutical Patent News, Sep 24, 2016

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24
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Merck Sharp & Dohme and Merck Sharp & Dohme File Australian Patent Application for Btk Inhibitors

Global IP News. Pharmaceutical Patent News, Feb 7, 2014

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25
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Taiwan Patent Office Publishes Acerta Pharma BV's Patent Application for Therapeutic Combination of a Pi3k Inhibitor and a BTK Inhibitor

Global IP News. Pharmaceutical Patent News, Nov 28, 2016

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26
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Acerta Pharma BV Seeks Patent for Methods of Using BTK Inhibitors to Treat Solid Tumors and Other Diseases Through Modulation of the Tumor Microenvironment

Global IP News. Pharmaceutical Patent News, Dec 13, 2016

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27
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Acerta Pharma Seeks Patent for Methods of Treating Cancers, Immune and Autoimmune Diseases and Inflammatory Diseases Based on BTK Occupancy and BTK Resynthesis Rate

Global IP News. Information Technology Patent News, Mar 26, 2018

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28
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U.S. Patent and Trademark Office Receives Acerta Pharma's Patent Application for Therapeutic Combinations of a Proteasome Inhibitor and a BTK Inhibitor

Global IP News. Pharmaceutical Patent News, Mar 18, 2017

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29
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Australian Patent Office Releases Merck Sharp & Dohme BV's Patent Application for MK2 Inhibitors

Global IP News. Pharmaceutical Patent News, Feb 23, 2015

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30
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U.S. Patent and Trademark Office Releases Acerta Pharma's Patent Application for Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor and/or a BCL-2 Inhibitor

Global IP News. Pharmaceutical Patent News, Sep 7, 2018

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31
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Acerta Pharma BV Files Taiwan Patent Application for Compositions and Methods for Treatment of Chronic Lymphocytic Leukemia and Small Lymphocytic Leukemia Using a Btk Inhibitor

Global IP News. Pharmaceutical Patent News, Feb 11, 2017

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32
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Acerta Pharma Seeks Patent for Therapeutic Combinations of an IRAK4 Inhibitor and a BTK Inhibitor

Global IP News. Pharmaceutical Patent News, Feb 10, 2017

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33
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U.S. Patent and Trademark Office Releases Merck Sharp & Dohme's Patent Application for MK2 Inhibitors

Global IP News. Pharmaceutical Patent News, Jun 10, 2016

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34
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U.S. Patent and Trademark Office Publishes Acerta Pharma's Patent Application for Therapeutic Combination of PI3K Inhibitor and a BTK Inhibitor

Global IP News. Pharmaceutical Patent News, Sep 24, 2017

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35
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Merck Sharp & Dohme Corp and Merck Sharp & Dohme BV File Patent Application for BTK Inhibitors

Indian Patents News, Jan 24, 2015

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36
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Acerta Pharma Applies for Patent on Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor and/or a CDK4/6 Inhibitor

Global IP News. Pharmaceutical Patent News, Sep 7, 2018

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37
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Taiwan Patent Office Publishes Acerta Pharma BV's Patent Application for Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor and/or a CDK4/6 Inhibitor

Global IP News. Pharmaceutical Patent News, Dec 13, 2016

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