Reversible inhibition of enzyme, an activity in which the inhibiting molecular entity (often a small chemical called ligand or inhibitor) can associate and dissociate from the protein's binding site, ...

THE mode of action of low-molecular weight enzyme inhibitors has been intensively studied. This does not, however, apply to high-molecular weight enzyme inhibitors. So far as we are aware, no work has ...

Reversibly targeting noncatalytic cysteine residues could lead to covalent drug molecules with improved potency and selectivity but with less potential for off-target adducts, Jack Taunton of the ...

Jaypirca is the first BTK inhibitor of any kind specifically approved for patients with mantle cell lymphoma previously treated with a covalent BTK inhibitor In the BRUIN Phase 1/2 trial, covalent BTK ...

As scientists race to discover new and effective antiviral drugs against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), many novel approaches are being utilized. Now, a new study ...

Researchers describe slow-binding inhibition of cholinesterases and present their pharmacological advantages over classical reversible inhibitors (e.g. long target-residence times, resulting in ...