Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase

2020 ◽  
Vol 63 (10) ◽  
pp. 5102-5118 ◽  
Author(s):  
Daniela Angst ◽  
François Gessier ◽  
Philipp Janser ◽  
Anna Vulpetti ◽  
Rudolf Wälchli ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Bruton’S Tyrosine Kinase ◽  
Bruton's Tyrosine Kinase ◽  
Covalent Inhibitor

scholarly journals A phase I trial of PRN1008, a novel reversible covalent inhibitor of Bruton's tyrosine kinase, in healthy volunteers

2017 ◽  
Vol 83 (11) ◽  
pp. 2367-2376 ◽  
Author(s):  
Patrick F. Smith ◽  
Janakan Krishnarajah ◽  
Philip A. Nunn ◽  
Ron J. Hill ◽  
Dane Karr ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Phase I ◽  
Healthy Volunteers ◽  
Phase I Trial ◽  
Bruton’S Tyrosine Kinase ◽  
Bruton's Tyrosine Kinase ◽  
Reversible Covalent ◽  
Covalent Inhibitor

scholarly journals Mechanism of covalent binding of ibrutinib to Bruton’s tyrosine kinase revealed by QM/MM calculations

2021 ◽  
Author(s):  
Angus Voice ◽  
Gary Tresdern ◽  
Rebecca M Twidale ◽  
Herman Van Vlijmen ◽  
Adrian John Mulholland
Keyword(s):  
Tyrosine Kinase ◽  
B Cell ◽  
Covalent Binding ◽  
Bruton’S Tyrosine Kinase ◽  
Bruton's Tyrosine Kinase ◽  
Covalent Inhibition ◽  
Covalent Inhibitor

Ibrutinib is the first covalent inhibitor of Bruton’s tyrosine kinase (BTK) to be used in the treatment of B-cell cancers. Understanding the mechanism of covalent inhibition will aid in the...

Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase

2019 ◽  
Vol 62 (17) ◽  
pp. 7923-7940 ◽  
Author(s):  
Yunhang Guo ◽  
Ye Liu ◽  
Nan Hu ◽  
Desheng Yu ◽  
Changyou Zhou ◽  
...  
Keyword(s):  
Tyrosine Kinase ◽  
Bruton’S Tyrosine Kinase ◽  
Bruton's Tyrosine Kinase ◽  
Covalent Inhibitor
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