Quantitative Characterization of Drug Metabolizing Enzymes and Drug Transporters in Preclinical Species and Human

Dear Colleagues,

Drug-metabolizing enzymes and membrane transporters (DMET) play important roles in the absorption, distribution, metabolism, and excretion processes that determine the pharmacokinetics of drugs. Protein abundance data of drug-metabolizing enzymes and transporters (DMETs) are broadly applicable to the characterization of in vitro and in vivo models, in vitro to in vivo extrapolation (IVIVE), and interindividual variability prediction. Liquid chromatography–tandem mass spectrometry (LC-MS/MS)-based proteomics is a powerful tool for identifying and quantifying proteins in biological samples, outperforming conventional antibody-based methods in many aspects. LC-MS/MS-based proteomics studies have revealed the protein abundances of many drug-metabolizing enzymes and transporters (DMETs) in tissues relevant to drug metabolism and disposition, as well as in liquid biopsies.

However, due to the trace amount of some of these proteins and complex sample matrices, it is challenging to quantify and compare the abundance of these DMET proteins in tissue. Moreover, there is a lack of quantitative data from extrahepatic tissue and its comparison with hepatic abundance. Additionally, there is a knowledge gap with respect to quantitative DMET abundance data from preclinical species that is important for extrapolation of drug disposition from animal models to human.

Given the importance of DMET proteins in drug development and the complexity of proteomics quantification, improvement in LC-MS/MS approaches is needed to quantify the DMET protein abundance and reduce inter-lab variability. Therefore, this Special Issue of Metabolites on “Quantitative characterization of Drug-Metabolizing Enzymes and Drug Transporters in Preclinical Species and Humans” will be dedicated to publishing current advances and improvement in LC-MS/MS-based proteomics quantification of DMET proteins in human and preclinical species. This issue will also welcome comparative data obtained from targeted and shotgun proteomics with emphasis on the DIA/SWATH-MS approach.

Dr. Abdul Basit
Guest Editor

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• drug metabolizing enzymes
• drug transporters
• quantitative proteomics
• LC-MS/MS proteomics
• shotgun proteomics
• non-CYP enzymes