Carboxylesterase (CES) Inhibitors

Carboxylesterases are a crucial class of enzymes that play a pivotal role in the metabolism of various drugs, xenobiotics, and endogenous compounds. These enzymes, collectively referred to as carboxylesterases, are responsible for catalyzing the hydrolysis of ester and amide bonds in a wide range of substrates. Through their activity, carboxylesterases contribute to the detoxification and clearance of foreign compounds from the body, helping to maintain cellular homeostasis. Moreover, carboxylesterases are involved in the activation or inactivation of prodrugs, which are compounds that require enzymatic conversion to their active form. The diverse substrates and roles of carboxylesterases underscore their significance in metabolism, as well as their potential impact on efficacy, safety, and interactions.

The development of carboxylesterase inhibitors holds substantial potential. Carboxylesterase inhibitors are compounds that modulate the activity of these enzymes, either by directly binding to their active sites or by influencing their expression and function. Inhibition of carboxylesterases can have several valuable applications. For instance, targeted inhibition of specific carboxylesterases can control the release of active molecules, enhancing delivery and efficacy.