Method of providing aripiprazole to patients having impaired CYP2D6 or CYP3A4 enzyme functionThe disclosed embodiments relate to methods of initiating aripiprazole treatment in a patient who is a CYP2D6 poor metabolizer or a CYP3A4 poor metabolizer, or both.Arash Raoufinia...
Enzyme kinetics for ART hydroxylation in HLMs The formation rate of ART-M as a function of ART concentrations (1–32 μM) followed Michaelis–Menten kinetics (Fig. 2), which showed the CLint,H of 27.6 μL/min/mg. The CLint,H derived from the substrate depletion was 30.3 μL/min/mg,...
(MAF=2.6%;Table 1). Notably,CYP3A5constitutes a unique case among theCYPnomenclature system in that the major allele disrupts enzyme function and is designated as∗3and not∗1.CYP3A5∗3is highly prevalent, particularly in Europeans, with MAFs up to 94.3%. As such, only the minority ...
Enzyme kinetics for ART hydroxylation in HLMs The formation rate of ART-M as a function of ART concentrations (1–32 μM) followed Michaelis–Menten kinetics (Fig. 2), which showed the CLint,H of 27.6 μL/min/mg. The CLint,H derived from the substrate depletion was 30.3 μL/min/mg,...
Therefore, HepaRG-derived HLCs will provide an alternative to human hepatocytes with high levels of CYP3A4 enzyme activity even under 2D culture conditions. This will improve a variety of drug screening methods.doi:10.1002/prp2.652John Wiley & Sons, LtdPharmacology Research & Perspectives...
The novel nonsynonymous SNP altering enzyme function The substitution of Cys for Tyr in codon 319 (Y319C) lies on the helix I,42 a domain which flanks the heme group and contains a substrate recognition site (SRS4).58 As shown in the Supplementary Table S2, Tyr319 is a highly conserved...
Pharmacokinetic and pharmacodynamic alterations of 3-hydroxy-3-methylglutaryl coenzyme a (Hmg-Coa) reductase inhibitors: drug-drug interactions and interindividual differences in transporter and metabolic enzyme functions. Pharmacol Ther. 2006;112:71–105. Article PubMed CAS Google Scholar ...
(HbA1c) level > 9.0% were not included. Additionally, individuals with uncontrolled hypothyroidism (thyroid stimulating hormone (TSH) > 4 µIU/L) and patients whose liver function was poor (aspartate aminotransferase (AST) or ALT > 1.4 ULN) were excluded. In addition, pregnant ...
展开 关键词: Humans Prostatic Neoplasms Prostatic Hyperplasia Cytochrome P-450 Enzyme System Mixed Function Oxygenases Odds Ratio Risk Factors Case-Control Studies Genotype Alleles DOI: 10.3892/or.9.3.653 被引量: 88 年份: 2002 收藏 引用 批量引用 报错 分享 全部...
The substrates for CYP3A4 enzyme are drugs and endogenous substances. Therefore, allelic changes in the coding regions of CYP3A4, increases the risk of developing cancers. CYP3A5 is expressed polymorphically in human liver, but consistently in lung, colon, and kidney.The purpose of this study ...