Related Experiment Video
Updated: Aug 19, 2026

Protein Target Prediction and Validation of Small Molecule Compound
Published on: February 23, 2024
Mammalian carboxylesterases: from drug targets to protein therapeutics
Matthew R Redinbo1, Philip M Potter
1Department of Chemistry, Department of Biochemistry and Biophysics, University of North Carolina, Chapel Hill, NC 27599-3290, USA. redinbo@unc.edu
Abstract:
Our understanding of the detailed recognition and processing of clinically useful therapeutic agents has grown rapidly in recent years, and we are now able to begin to apply this knowledge to the rational treatment of disease. Mammalian carboxylesterases (CEs) are enzymes with broad substrate specificities that have key roles in the metabolism of a wide variety of clinical drugs, illicit narcotics and chemical nerve agents. Here, the functions, mechanism of action and structures of human CEs are reviewed, with the goal of understanding how these proteins are able to act in such a non-specific fashion, yet catalyze a remarkably specific chemical reaction. Current approaches to harness these enzymes as protein-based therapeutics for drug and chemical toxin clearance are described, as well as their uses for targeted chemotherapeutic prodrug activation. Also included is an outline of how selective CE inhibitors could be used as co-drugs to improve the efficacy of clinically approved agents.
Related Concept Videos
Pharmacogenomics: Identification of New Drug Targets
Alkylation of β-Diester Enolates: Malonic Ester Synthesis
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
Targets for Drug Action: Overview
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
Esters to Carboxylic Acids: Saponification
The reaction requires a base in stoichiometric amounts, which participates in the reaction and is not regenerated later. So, the base acts as a...

