Discovery of a Potent BTK Inhibitor with a Novel Binding Mode by Using Parallel Selections with a DNA‐Encoded Chemical Library
Sign Up to like & getrecommendations! Published in 2017 at "ChemBioChem"
DOI: 10.1002/cbic.201600573
Abstract: We have identified and characterized novel potent inhibitors of Bruton's tyrosine kinase (BTK) from a single DNA‐encoded library of over 110 million compounds by using multiple parallel selection conditions, including variation in target concentration and… read more here.
Keywords: potent; novel binding; btk; dna encoded ... See more keywords
Semi-mechanistic PK/PD modeling and simulation of irreversible BTK inhibition to support dose selection of tirabrutinib in subjects with RA.
Sign Up to like & getrecommendations! Published in 2021 at "Clinical pharmacology and therapeutics"
DOI: 10.1002/cpt.2439
Abstract: Tirabrutinib is an irreversible, small-molecule Bruton's tyrosine kinase (BTK) inhibitor, which was approved in Japan (VELEXBRU® ) to treat B-cell malignancies and is in clinical development for inflammatory diseases. As an application of model-informed drug… read more here.
Keywords: tirabrutinib; semi mechanistic; model; btk ... See more keywords
Selective BTK inhibition improves bendamustine therapy response and normalizes immune effector functions in chronic lymphocytic leukemia
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DOI: 10.1002/ijc.32010
Abstract: The Bruton's tyrosine kinase (BTK) inhibitor ibrutinib has been shown to be highly effective in patients with chronic lymphocytic leukemia (CLL) and is approved for CLL treatment. Unfortunately, resistance and intolerance to ibrutinib has been… read more here.
Keywords: cll; lymphocytic leukemia; inhibition; btk ... See more keywords
Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.12.079
Abstract: Bruton's tyrosine kinase (Btk) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) and Fcγ receptor (FcR) signaling pathways, which makes it a uniquely attractive target for the treatment… read more here.
Keywords: pyrimidin amine; treatment; pyrrolo pyrimidin; btk ... See more keywords
The development of Bruton's tyrosine kinase (BTK) inhibitors from 2012 to 2017: A mini-review.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.03.062
Abstract: Bruton's tyrosine kinase (BTK) has emerged as a promising drug target for multiple diseases, particularly haematopoietic malignancies and autoimmune diseases related to B lymphocytes. This review focuses on the diverse, small-molecule inhibitors of BTK kinase… read more here.
Keywords: btk; kinase btk; btk inhibitors; bruton tyrosine ... See more keywords
Discovery of potent and highly selective covalent inhibitors of Bruton's tyrosine kinase bearing triazine scaffold.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2020.112339
Abstract: Bruton's tyrosine kinase (BTK), as a key regulator of the B cell receptor (BCR) signaling pathway, is an attractive therapeutic target for the treatment of various diseases such as leukemia and B-cell malignancies. Herein, a… read more here.
Keywords: bearing triazine; discovery potent; kinase; btk ... See more keywords
Emerging small-molecule inhibitors of the Bruton's tyrosine kinase (BTK): Current development.
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DOI: 10.1016/j.ejmech.2021.113329
Abstract: Therapy based on Bruton's tyrosine kinase (BTK) inhibitors one of the major treatment options currently recommended for lymphoma patients. The first generation of BTK inhibitor, Ibrutinib, achieved remarkable progress in the treatment of B-cell malignancies,… read more here.
Keywords: development; btk; kinase btk; btk inhibitors ... See more keywords
Concentration of evobrutinib, a BTK inhibitor, in cerebrospinal fluid during treatment of patients with relapsing multiple sclerosis in a phase 2 study
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DOI: 10.1016/j.msard.2021.103001
Abstract: Background Evobrutinib, a highly selective Bruton's tyrosine kinase (BTK) inhibitor, demonstrated a low annualized relapse rate (75mg twice-daily: 0.11, 95%CI 0.04–0.25) in a phase 2 randomized controlled trial in patients with relapsing multiple sclerosis (RMS;… read more here.
Keywords: phase; study; multiple sclerosis; btk ... See more keywords
Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase Using PROTAC-Mediated Degradation.
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DOI: 10.1021/acs.biochem.8b00391
Abstract: 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… read more here.
Keywords: degradation; protac; btk; bruton tyrosine ... See more keywords
A Fast and Clean BTK Inhibitor
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DOI: 10.1021/acs.jmedchem.0c00597
Abstract: Bruton’s tyrosine kinase (BTK) is a major drug target for B-cell related malignancies; however, existing BTK inhibitors approved for cancer treatment have significant off-targets that limit their use for autoimmune and inflammatory diseases. Remibrutinib (LOU064)… read more here.
Keywords: clean btk; chemistry; btk; fast clean ... See more keywords
Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00926
Abstract: Multiple Sclerosis is a chronic autoimmune neurodegenerative disorder of the central nervous system (CNS) that is characterized by inflammation, demyelination, and axonal injury leading to permeant disability. In the early stage of MS, inflammation is… read more here.
Keywords: biib091; sclerosis; inhibitor; discovery ... See more keywords