Drug discovery considerations in the development of covalent inhibitors

R Mah, JR Thomas, CM Shafer - Bioorganic & medicinal chemistry letters, 2014 - Elsevier
Bioorganic & medicinal chemistry letters, 2014Elsevier
In recent years, the number of drug candidates with a covalent mechanism of action
progressing through clinical trials or being approved by the FDA has increased significantly.
And as interest in covalent inhibitors has increased, the technical challenges for
characterizing and optimizing these inhibitors have become evident. A number of new tools
have been developed to aid this process, but these have not gained wide-spread use. This
review will highlight a number of methods and tools useful for prosecuting covalent inhibitor …
Abstract
In recent years, the number of drug candidates with a covalent mechanism of action progressing through clinical trials or being approved by the FDA has increased significantly. And as interest in covalent inhibitors has increased, the technical challenges for characterizing and optimizing these inhibitors have become evident. A number of new tools have been developed to aid this process, but these have not gained wide-spread use. This review will highlight a number of methods and tools useful for prosecuting covalent inhibitor drug discovery programs.
Elsevier
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