Discovery of 1-Amino-1H-imidazole-5-carboxamide Derivatives as Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitors
C Ma, Q Li, M Zhao, G Fan, J Zhao… - Journal of Medicinal …, 2021 - ACS Publications
… To confirm that the compound really binds covalently to BTK, we … The results indicated that
our compound bound covalently to … of NH 2 in the carboxamide group of compound 26 with an …
our compound bound covalently to … of NH 2 in the carboxamide group of compound 26 with an …
Aminopyrazole carboxamide Bruton's tyrosine kinase inhibitors. Irreversible to reversible covalent reactive group tuning
ME Schnute, SE Benoit, IP Buchler… - ACS Medicinal …, 2018 - ACS Publications
… covalent inhibitors of Bruton’s tyrosine kinase (BTK) based on an aminopyrazole carboxamide
… Compared to acrylamide-based covalent reactive groups leading to irreversible protein …
… Compared to acrylamide-based covalent reactive groups leading to irreversible protein …
Discovery of Covalent Bruton's Tyrosine Kinase Inhibitors with Decreased CYP2C8 Inhibitory Activity
H Qiu, Z Ali, J Bowlan, R Caldwell, A Gardberg… - …, 2021 - Wiley Online Library
… Bruton's tyrosine kinase (BTK) is a member of the Tec kinase … of potent and selective covalent
irreversible BTK inhibitors. … Bruton's tyrosine kinase (BTK) is a member of the Tec family …
irreversible BTK inhibitors. … Bruton's tyrosine kinase (BTK) is a member of the Tec family …
Ibrutinib, a Carboxylic Acid Amide Inhibitor of B ruton's Tyrosine Kinase
TD Owens - Bioactive Carboxylic Compound Classes …, 2016 - Wiley Online Library
… Bruton’s tyrosine kinase (Btk) is a critical enzyme for the development and function of B
cells… form a covalent bond to a specific cysteine present in Btk, and the carboxylic acid amide …
cells… form a covalent bond to a specific cysteine present in Btk, and the carboxylic acid amide …
Discovery of a novel series of pyridine and pyrimidine carboxamides as potent and selective covalent inhibitors of Btk
R Caldwell, L Liu-Bujalski, H Qiu, I Mochalkin… - Bioorganic & Medicinal …, 2018 - Elsevier
… The Bruton's tyrosine kinase gene is expressed throughout B cell differentiation, from early
precursor B cell stages preceding immunoglobulin gene rearrangement up to mature B cell …
precursor B cell stages preceding immunoglobulin gene rearrangement up to mature B cell …
Merits and pitfalls in the characterization of covalent inhibitors of bruton's tyrosine kinase
CM Harris, SE Foley, ER Goedken… - … Life Sciences R&D, 2018 - journals.sagepub.com
… covalent inhibitors of Bruton’s tyrosine kinase (BTK), we evaluated multiple techniques
for characterizing covalent inhibitors. Several methods qualitatively support the covalent …
for characterizing covalent inhibitors. Several methods qualitatively support the covalent …
Discovery of a potent and selective covalent inhibitor of Bruton's tyrosine kinase with oral anti-inflammatory activity
MS Tichenor, JJM Wiener, NL Rao… - ACS Medicinal …, 2021 - ACS Publications
… selective covalent 4-oxo-4,5-dihydro-3H-1-thia-3,5,8-triazaacenaphthylene-2-carboxamide
BTK … a noncatalytic cysteine residue (Cys481) for covalent bond formation. Compound 27 is …
BTK … a noncatalytic cysteine residue (Cys481) for covalent bond formation. Compound 27 is …
Structure-activity relationship investigation for imidazopyrazole-3-carboxamide derivatives as novel selective inhibitors of Bruton's tyrosine kinase
D Zhang, G Xu, J Zhao, Y Wang, X Wu, X He… - European Journal of …, 2021 - Elsevier
… It selectively binds to Cys481 of the target BTK via a covalent bond, thereby inhibits its
autophosphorylation to block the BCR signaling pathway [17]. Unfortunately, owing to multiple …
autophosphorylation to block the BCR signaling pathway [17]. Unfortunately, owing to multiple …
Discovery of 4-aminoquinoline-3-carboxamide derivatives as potent reversible Bruton's tyrosine kinase inhibitors for the treatment of rheumatoid arthritis
X Yao, X Sun, S Jin, L Yang, H Xu… - Journal of Medicinal …, 2019 - ACS Publications
… of BTK that covalently binds to Cys481 in the kinase domain. Though covalent BTK inhibitors,
such … For instance, the Michael receptor portions of covalent inhibitors raise the concern of …
such … For instance, the Michael receptor portions of covalent inhibitors raise the concern of …
Exploring 2-Sulfonylpyrimidine Warheads as Acrylamide Surrogates for Targeted Covalent Inhibition: A BTK Story
R Moraru, B Valle-Argos, A Minton… - Journal of Medicinal …, 2024 - ACS Publications
… We selected the Bruton Tyrosine Kinase (BTK) as a particularly relevant test case to assess
the suitability of 2-SP warheads in TCI design. BTK plays a key role in signal transduction …
the suitability of 2-SP warheads in TCI design. BTK plays a key role in signal transduction …
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