Results 201 to 210 of about 187,458 (237)

Screening and Characterization of Allosteric Small Molecules Targeting Bruton's Tyrosine Kinase. [PDF]

open access: yesBiochemistry
Kueffer LE   +6 more
europepmc   +1 more source
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Discovery of Reversible Covalent Bruton's Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib).

Journal of Medicinal Chemistry, 2022
Bruton's tyrosine kinase (BTK), a Tec family tyrosine kinase, is critical in immune pathways as an essential intracellular signaling element, participating in both adaptive and immune responses. Currently approved BTK inhibitors are irreversible covalent
T. D. Owens   +23 more
semanticscholar   +1 more source

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

Journal of Medicinal Chemistry, 2019
Aberrant activation of Bruton's tyrosine kinase (BTK) plays an important role in pathogenesis of B-cell lymphomas suggesting that inhibition of BTK is useful in the treatment of hematological malignancies.
Yunhang Guo   +39 more
semanticscholar   +1 more source

Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation.

Biochemistry, 2018
Inhibition of Bruton's tyrosine kinase (BTK) with the irreversible inhibitor ibrutinib has emerged as a transformative treatment option for patients with chronic lymphocytic leukemia (CLL) and other B-cell malignancies, yet >80% of CLL patients develop ...
A. Buhimschi   +9 more
semanticscholar   +1 more source

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

Journal of Medicinal Chemistry, 2020
Bruton's tyrosine kinase (BTK), a cytoplasmic tyrosine kinase, plays a central role in immunity and is considered an attractive target for treating autoimmune diseases.
D. Angst   +16 more
semanticscholar   +1 more source

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