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Title: Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton?s Tyrosine Kinase

Journal Article · · J. Med. Chem.

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
DOE - Office Of Science; INDUSTRY
OSTI ID:
1902355
Journal Information:
J. Med. Chem., Vol. 65, Issue (21)
Country of Publication:
United States
Language:
ENGLISH

References (31)

Tec Kinases Mediate Sustained Calcium Influx via Site-specific Tyrosine Phosphorylation of the Phospholipase Cγ Src Homology 2-Src Homology 3 Linker journal June 2004
Second-generation inhibitors of Bruton tyrosine kinase journal September 2016
Spebrutinib (CC-292) Affects Markers of B Cell Activation, Chemotaxis, and Osteoclasts in Patients with Rheumatoid Arthritis: Results from a Mechanistic Study journal November 2019
Bruton's Tyrosine Kinase mediates platelet receptor-induced generation of microparticles: A potential mechanism for amplification of inflammatory responses in rheumatoid arthritis synovial joints journal February 2013
Bruton's tyrosine kinase (Btk) inhibitor tirabrutinib suppresses osteoclastic bone resorption journal June 2019
The Src, Syk, and Tec family kinases: Distinct types of molecular switches journal August 2010
Targeting Bruton's tyrosine kinase in B cell malignancies journal March 2014
Mechanisms of B-cell lymphoma pathogenesis journal April 2005
Cutting Edge: Constitutive B Cell Receptor Signaling Is Critical for Basal Growth of B Lymphoma journal May 2006
Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma journal January 2010
The lymph node microenvironment promotes B-cell receptor signaling, NF-κB activation, and tumor proliferation in chronic lymphocytic leukemia journal January 2011
The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo journal February 2012
Discovery of Selective Irreversible Inhibitors for Bruton’s Tyrosine Kinase journal January 2007
Acalabrutinib (ACP-196) in Relapsed Chronic Lymphocytic Leukemia journal January 2016
Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase journal August 2019
Bruton’s tyrosine kinase (BTK) inhibitors in treating cancer: a patent review (2010-2018) journal March 2019
Btk Inhibitors: A Medicinal Chemistry and Drug Delivery Perspective journal July 2021
A Fast and Clean BTK Inhibitor journal May 2020
Medicinal Chemistry Strategies for the Development of Bruton’s Tyrosine Kinase Inhibitors against Resistance journal May 2022
Discovery of Reversible Covalent Bruton’s Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib) journal March 2022
Discovery of Pteridine-7(8H)-one Derivatives as Potent and Selective Inhibitors of Bruton’s Tyrosine Kinase (BTK) journal January 2022
Bruton Tyrosine Kinase Inhibitors journal November 2019
Combining BTK inhibitors with BCL2 inhibitors for treating chronic lymphocytic leukemia and mantle cell lymphoma journal April 2022
Developing Irreversible Inhibitors of the Protein Kinase Cysteinome journal February 2013
Discovery of the Bruton’s Tyrosine Kinase Inhibitor Clinical Candidate TAK-020 (S)-5-(1-((1-Acryloylpyrrolidin-3-yl)oxy)isoquinolin-3-yl)-2,4-dihydro-3H-1,2,4-triazol-3-one, by Fragment-Based Drug Design journal August 2021
Discovery of LOU064 (Remibrutinib), a Potent and Highly Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase journal February 2020
Pharmacodynamic Analysis of BTK Inhibition in Patients with Chronic Lymphocytic Leukemia Treated with Acalabrutinib journal February 2020
Discovery of a Potent and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase with Oral Anti-Inflammatory Activity journal April 2021
Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success journal November 2009
Regioselective Derivatizations of a Tribrominated Atropisomeric Benzamide Scaffold journal January 2015
Simultaneous Inhibition of PI3Kδ and PI3Kα Induces ABC-DLBCL Regression by Blocking BCR-Dependent and -Independent Activation of NF-κB and AKT journal January 2017

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