Discovery of Covalent Bruton's Tyrosine Kinase Inhibitors with Decreased CYP2C8 Inhibitory Activity

Bruton's tyrosine kinase (BTK) is a member of the Tec kinase family that is expressed in cells of hematopoietic lineage. Evidence has shown that inhibition of BTK has clinical benefit for the treatment of a wide array of autoimmune and inflammatory diseases. Previously we reported the discovery...

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Veröffentlicht in:	ChemMedChem 2021-12, Vol.16 (24), p.3653-3662
Hauptverfasser:	Qiu, Hui, Ali, Zahid, Bowlan, Julian, Caldwell, Richard, Gardberg, Anna, Glaser, Nina, Goutopoulos, Andreas, Head, Jared, Johnson, Theresa, Maurer, Christine, Georgi, Katrin, Grenningloh, Roland, Fang, Zhizhou, Morandi, Federica, Rohdich, Felix, Schmidt, Ralf, Follis, Ariele Viacava, Sherer, Brian
Format:	Artikel
Sprache:	eng
Schlagworte:	Acrylamide Agammaglobulinaemia Tyrosine Kinase - antagonists & inhibitors Agammaglobulinaemia Tyrosine Kinase - metabolism Bruton's tyrosine kinase covalent BTK inhibitor Crystal structure cyanamide CYP2C8 Cytochrome P-450 CYP2C8 - metabolism Cytochrome P-450 CYP2C8 Inhibitors - chemical synthesis Cytochrome P-450 CYP2C8 Inhibitors - chemistry Cytochrome P-450 CYP2C8 Inhibitors - pharmacology Dose-Response Relationship, Drug Drug Discovery Ether-A-Go-Go Potassium Channels - antagonists & inhibitors Ether-A-Go-Go Potassium Channels - metabolism Humans Inflammatory diseases Kinases Liability Molecular Structure Nicotinamide Optimization Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Selectivity Structure-Activity Relationship Transposition Tyrosine Tyrosine kinase inhibitors Warheads
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