![Covalent Inhibitors Library Covalent Inhibitors Library](/images/rx_pageimages/Covalent_Inhibitors_Library.png)
Covalent Inhibitors Library
Covalent inhibitors targeting enzymes such as kinases or proteases for a long time were set aside due to the high reactivity and potential toxicity. However, covalent kinase inhibitors were recently successfully introduced as cancer therapeutics agents. Thus, the benefits of irreversible kinase inhibition appeared to surpass the potential risks of such drugs. Traditionally, the most targeted residue in the protein kinase active site is cysteine. Due to the low abundance of this residue, drugs targeting cysteine appear to be more selective and have a lower chance of appearing to be toxic. All covalent enzyme inhibitors must contain specific reactive group (covalent "warhead"), and alternatively to cysteine, other amino acid residues were proposed as targets for reactive small molecules as well.