Allard Kaptein
Overview
Explore the profile of Allard Kaptein including associated specialties, affiliations and a list of published articles.
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Articles
19
Citations
827
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0
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Recent Articles
1.
Podoll T, Pearson P, Kaptein A, Evarts J, de Bruin G, Emmelot-van Hoek M, et al.
J Pharmacol Exp Ther
. 2022 Oct;
384(1):173-186.
PMID: 36310034
Acalabrutinib is a covalent Bruton tyrosine kinase (BTK) inhibitor approved for relapsed/refractory mantle cell lymphoma and chronic lymphocytic leukemia/small lymphocytic lymphoma. A major metabolite of acalabrutinib (M27, ACP-5862) was observed...
2.
Hoogenboom N, Demont D, de Zwart E, Verkaik S, Emmelot M, van de Kar B, et al.
Bioorg Med Chem Lett
. 2021 Oct;
52:128406.
PMID: 34624491
Epidermal growth factor receptor (EGFR) inhibitors have clinical utility in the treatment of non-small cell lung cancer (NSCLC) patients. Despite encouraging clinical efficacy with these agents, many patients develop resistance...
3.
van der Wel T, Hilhorst R, den Dulk H, van den Hooven T, Prins N, Wijnakker J, et al.
Nat Commun
. 2020 Jun;
11(1):3216.
PMID: 32587248
Chemical tools to monitor drug-target engagement of endogenously expressed protein kinases are highly desirable for preclinical target validation in drug discovery. Here, we describe a chemical genetics strategy to selectively...
4.
de Bruin G, Demont D, de Zwart E, Verkaik S, Hoogenboom N, van de Kar B, et al.
Bioorg Med Chem Lett
. 2020 Jun;
30(14):127261.
PMID: 32527559
Bruton tyrosine kinase (BTK) is an important target in oncology and (auto)immunity. Various BTK inhibitors have been approved or are currently in clinical development. A novel BTK inhibitor series was...
5.
Rip J, de Bruijn M, Kaptein A, Hendriks R, Corneth O
J Immunol
. 2020 Apr;
204(10):2852-2863.
PMID: 32253241
BCR signaling, involving phosphorylation of various downstream molecules, including kinases, lipases, and linkers, is crucial for B cell selection, survival, proliferation, and differentiation. Phosphoflow cytometry (phosphoflow) is a single-cell-based technique...
6.
Barf T, Covey T, Izumi R, van de Kar B, Gulrajani M, van Lith B, et al.
J Pharmacol Exp Ther
. 2017 Sep;
363(2):240-252.
PMID: 28882879
Several small-molecule Bruton tyrosine kinase (BTK) inhibitors are in development for B cell malignancies and autoimmune disorders, each characterized by distinct potency and selectivity patterns. Herein we describe the pharmacologic...
7.
Herman S, Montraveta A, Niemann C, Mora-Jensen H, Gulrajani M, Krantz F, et al.
Clin Cancer Res
. 2016 Dec;
23(11):2831-2841.
PMID: 27903679
Acalabrutinib (ACP-196) is a novel, potent, and highly selective Bruton tyrosine kinase (BTK) inhibitor, which binds covalently to Cys481 in the ATP-binding pocket of BTK. We sought to evaluate the...
8.
Harrington B, Gardner H, Izumi R, Hamdy A, Rothbaum W, Coombes K, et al.
PLoS One
. 2016 Jul;
11(7):e0159607.
PMID: 27434128
Acalabrutinib (ACP-196) is a second-generation inhibitor of Bruton agammaglobulinemia tyrosine kinase (BTK) with increased target selectivity and potency compared to ibrutinib. In this study, we evaluated acalabrutinib in spontaneously occurring...
9.
Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Babu Boga S, et al.
ACS Med Chem Lett
. 2016 Mar;
7(2):198-203.
PMID: 26985298
Bruton's tyrosine kinase (BTK) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) pathway. It has become an attractive kinase target for selective B...
10.
Byrd J, Harrington B, OBrien S, Jones J, Schuh A, Devereux S, et al.
N Engl J Med
. 2015 Dec;
374(4):323-32.
PMID: 26641137
Background: Irreversible inhibition of Bruton's tyrosine kinase (BTK) by ibrutinib represents an important therapeutic advance for the treatment of chronic lymphocytic leukemia (CLL). However, ibrutinib also irreversibly inhibits alternative kinase...