… toward the rational design of inhibitors and considering the … covalent and non-covalent
inhibition, we opted to provide a detailed understanding of covalent and non-covalent inhibition. …

… helpful (eg, targeted covalent inhibitors, which target a poorly … to classify enzyme inhibitors
that use covalent bond formation … We recommend categorizing covalent enzyme inhibitors by …

… Covalent inhibitors and clickable covalent probes … an enzyme inhibitor in native biological
systems by measuring the ability of an inhibitor to slow the rate of reaction of the enzyme with a …

… been employed to design covalent target binding into enzyme inhibitors or receptor ligands.
… , covalent binding event. We will apply these findings in targeted covalent inhibitors that are …

… Irreversible enzyme inhibitors and covalent chemical biology probes often utilize the …
enzyme, DcpS) using inhibitors armed with a sulfonyl fluoride electrophile. These inhibitors …

… and the development of safe and efficient covalent enzyme inhibitors. All stages of a drug …
Our major focus will be on covalent enzyme inhibitors, although other classes of covalent …

… target proteins that covalently bind to the probe within the cell. Examples of programs where
proteomic methods have been used to interrogate covalent enzyme inhibitor selectivity are …

… enzyme inhibitors. We have also demonstrated that the addition of an external enzyme inhibitor
… select a range of inhibitors that bind in different areas of the enzyme, and examine their …

… generation” kinase inhibitors will enter development. More challenging goals include the
design of allosteric covalent enzyme inhibitors, 122 as well as covalent modulators of receptor …

… of several covalent … enzymes that can be targeted by covalent inhibitors for the treatment
of human diseases. We focus on protein kinases, RAS proteins, and a few other enzymes that …