The resurgence of covalent drugs
Citations
1,290 citations
1,191 citations
1,120 citations
Cites background from "The resurgence of covalent drugs"
...Usually, covalent inhibitors bind to their molecular targets with high affinity, leading to a long-lasting pharmacological response, and consequently requiring less frequent administration [89]....
[...]
724 citations
Cites background from "The resurgence of covalent drugs"
...This type of kinase inhibition takes place via trapping of a solvent-exposed cysteine residue either by SN2 displacement of a leaving group or by reacting with a Michael acceptor incorporated within the kinase inhibitor [113, 120, 121]....
[...]
709 citations
Cites background from "The resurgence of covalent drugs"
...Newer chemical entities targeting ErbB receptors were designed to covalently engage their targets characterized by cysteine residues in the active site, assuming that this might translate into higher selectivity and longer residence time and, ultimately, into better efficacy (Copeland et al., 2006; Singh et al., 2011)....
[...]
...…targeting ErbB receptors were designed to covalently engage their targets characterized by cysteine residues in the active site, assuming that this might translate into higher selectivity and longer residence time and, ultimately, into better efficacy (Copeland et al., 2006; Singh et al., 2011)....
[...]
References
5,977 citations
3,390 citations
2,008 citations
1,741 citations
1,633 citations