UDP-glucuronosyltransferases: Structure, Function and Drug Design Studies

Current Medicinal Chemistry
Erica Candido Costa ManoKathia M Honorio

Abstract

UDP-glucuronosyltransferases (UGTs) are important phase II metabolic enzymes responsible for approximately 40-70% of endo and xenobiotic reactions. It catalyzes the transfer of glucuronic acid to lipophilic substrates, converting them into hydrophilic compounds that are excreted. There are 22 active human UGTs that belong to 4 families. This review focuses on human UGTs, highlighting the most current issues in order to connect all information available and allowing a discussion on the challenges already solved and those in which we need to move forward. Although, several UGTs studies have been conducted, the most recent ones addressing drug-drug interactions and polymorphism issues, there are still bottlenecks to overcome. Tridimensional structure is difficult to obtain due to overexpression, purification, and crystallization problems as well as the action mechanism - since overlapping of substrate specificities renders impasses on the identification of which isoform is responsible for a particular drug metabolic pathway. For this reason, bioinformatic tools are gaining more space, since it is a faster and less expensive reliable methodology that complements in vitro and in vivo researches. Combinations of quantum and molecular...Continue Reading

Citations

Nov 30, 2018·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Qiang FuXibo Zhang
Jul 17, 2020·Pharmaceutical Biology·Yang LiHaiping Wang
Dec 18, 2020·Pharmaceutical Biology·Hao WangYuzhu Li
Dec 24, 2019·Acta Pharmaceutica Sinica. B·Yuhua LiHuichang Bi
Jul 23, 2021·Food and Chemical Toxicology : an International Journal Published for the British Industrial Biological Research Association·Shanoo SuroowanMohamad Fawzi Mahomoodally
Oct 17, 2021·ChemMedChem·Simone Q PantaleãoKathia Maria Honorio
Dec 11, 2021·Frontiers in Pharmacology·MengLin ChenBaojian Wu

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