Relative Selectivity of Covalent Inhibitors Requires Assessment of Inactivation Kinetics and Cellular Occupancy: A Case Study of Ibrutinib and Acalabrutinib
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Last updated 28 maio 2024
Toward Atomistic Modeling of Irreversible Covalent Inhibitor Binding Kinetics
Frontiers Structure-Function Relationships of Covalent and Non-Covalent BTK Inhibitors
Selective Inhibition of Bruton's Tyrosine Kinase by a Designed Covalent Ligand Leads to Potent Therapeutic Efficacy in Blood Cancers Relative to Clinically Used Inhibitors
Structural and biophysical insights into the mode of covalent binding of rationally designed potent BMX inhibitors - RSC Chemical Biology (RSC Publishing) DOI:10.1039/D0CB00033G
Relative Selectivity of Covalent Inhibitors Requires Assessment of Inactivation Kinetics and Cellular Occupancy: A Case Study of Ibrutinib and Acalabrutinib
PDF) Mechanism of covalent binding of ibrutinib to Bruton's tyrosine kinase revealed by QM/MM calculations
Structure of BTK kinase domain with the second-generation inhibitors acalabrutinib and tirabrutinib
Deciding between one-step and two-step irreversible inhibition mechanisms on the basis of “kobs” data: A statistical approach
Haematologica, Volume 106, Issue 9 by Haematologica - Issuu
A Perspective on the Kinetics of Covalent and Irreversible Inhibition
Case Study - COVALfinder to Study Irreversible EGFR Drugs
Pharmaceuticals, Free Full-Text
Sigmoidal correlation between Btk occupancy and experimentally observed
Proteomics and Beyond: Cell Decision-Making Shaped by Reactive Electrophiles: Trends in Biochemical Sciences
PDF] Relative Selectivity of Covalent Inhibitors Requires Assessment of Inactivation Kinetics and Cellular Occupancy: A Case Study of Ibrutinib and Acalabrutinib
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