Carboxylesterase 1 and Precision Pharmacotherapy: Pharmacogenetics and Nongenetic Regulators

• Published in: Drug metabolism and disposition Vol. 48; no. 3; pp. 230 - 244
• Main Authors: Her, Lucy, Zhu, Hao-Jie
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 01.03.2020; American Society for Pharmacology and Experimental Therapeutics, Inc; The American Society for Pharmacology and Experimental Therapeutics
• Subjects: Biomarkers; Carboxylesterase; Carboxylic Ester Hydrolases - genetics; Chemical compounds; Copy number; DNA Copy Number Variations - genetics; Drug therapy; Drugs; Humans; Liver; Nucleotides; Pesticides; Pharmaceutical Preparations - administration & dosage; Pharmaceutical Preparations - metabolism; Pharmacodynamics; Pharmacogenetics; Pharmacogenetics - methods; Pharmacokinetics; Pharmacology; Pollutants; Polymorphism, Single Nucleotide; Precision Medicine; Prodrugs; Proteomes; Regulators; Single-nucleotide polymorphism; Substrates; ADHD; FDA; CBD; M1; M2; CNV; PNPA; ADP; CBN; THC; AUC; PAPI; SNP; ACEI; CYP; ID; DME; DABE; AA; LOF; CI; CES; AT; BCS; MAF; PD; PK; VASP-PRI; UGT1A

Carboxylesterase (CES) 1 is the most abundant drug-metabolizing enzyme in human livers, comprising approximately 1% of the entire liver proteome. CES1 is responsible for 80%–95% of total hydrolytic activity in the liver and plays a crucial role in the metabolism of a wide range of drugs (especially...