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. Author manuscript; available in PMC: 2019 Jun 19.
Published in final edited form as: Biochemistry. 2018 Apr 30;57(24):3326–3337. doi: 10.1021/acs.biochem.8b00315

Figure 12.

Figure 12

Soft Drug Form of a Covalent Inhibitor. This classical affinity label bearing a fumarate ester reactive group covalently modifies a Cys in Bruton’s tyrosine kinase (BTK), but hydrolysis of the ester by human carboxylesterase-1 (CES1) results in rapid deactivation of the reactive group, improving selectivity.