Skip to main content
. Author manuscript; available in PMC: 2015 Mar 1.
Published in final edited form as: Medchemcomm. 2014 Mar;5(3):268–276. doi: 10.1039/C3MD00333G

Figure 6. Triazole urea covalent APT inhibitors.

Figure 6

(A) Mechanism of triazole urea inactivation of APT enzymes. The APT nucleophilic serine hydroxyl attacks the urea, releasing the triazole and leaving a stable carbamate adduct, inactivating the enzyme. (B) Selectivity and potency of optimized triazole urea inhibitors determined by gel-based competitive ABPP. AA64-2 is highly potent and selective for APT enzymes, with the exception of the uncharacterized hydrolase ABHD11. AA44-1 is highly selective for ABHD11, and can be used as a control probe.