Characterization of the CYP2C8 Active Site by Homology Modeling
To compare the features of the active sites of CYP2C8, CYP2C9, and CYP2C19, homology modeling was performed based on the crystallographic coordinates of mammalian CYP2C5. It was found that CYP2C8 has a much larger pocket than the other forms due to the existence of an additional pocket.
Toshimasa, Tanaka +3 more
openaire +3 more sources
Current evidence for a modulation of low back pain by human genetic variants [PDF]
The manifestation of chronic back pain depends on structural, psychosocial, occupational and genetic influences. Heritability estimates for back pain range from 30% to 45%. Genetic influences are caused by genes affecting intervertebral disc degeneration
Aberle +200 more
core +1 more source
Impact of variation in CYP3A and CYP2C8 on tucatinib metabolic clearance in human liver microsomes [PDF]
Bethany D. Latham +4 more
openalex +3 more sources
In Vitro Model for Hepatotoxicity Studies Based on Primary Human Hepatocyte Cultivation in a Perfused 3D Bioreactor System [PDF]
Accurate prediction of the potential hepatotoxic nature of new pharmaceuticals remains highly challenging. Therefore, novel in vitro models with improved external validity are needed to investigate hepatic metabolism and timely identify any toxicity ...
Damm, Georg +11 more
core +2 more sources
Cyp2c70 is responsible for the species difference in bile acid metabolism between mice and humans [PDF]
Bile acids are synthesized from cholesterol in the liver and subjected to multiple metabolic biotransformations in hepatocytes, including oxidation by cytochromes P450 (CYPs) and conjugation with taurine, glycine, glucuronic acid, and sulfate.
Botham +45 more
core +2 more sources
Pharmacokinetics and pharmacodynamics of rosiglitazone in relation to CYP2C8 genotype
Rosiglitazone is metabolically inactivated predominantly via the cytochrome P450 (CYP) enzyme CYP2C8. The functional impact of the CYP2C8*3 allele coding for the Arg139Lys and Lys399Arg amino acid substitutions is controversial. The purpose of this was to clarify the role of this polymorphism with regard to the pharmacokinetics and clinical effects of ...
Kirchheiner, Julia +11 more
openaire +3 more sources
Renal drug metabolism in humans: the potential for drug–endobiotic interactions involving cytochrome P450 (CYP) and UDP-glucuronosyltransferase (UGT) [PDF]
This item is under embargo for a period of 12 months from the date of publication, in accordance with the publisher's policy. ‘This is the peer reviewed version of the following article: Knights, K. M., Rowland, A. and Miners, J. O.
Knights, Kathleen Mary +2 more
core +1 more source
Lidia Habtemikael,1 Mulugeta Russom,2 Iyassu Bahta,2 Selam Mihreteab,3 Araia Berhane,4 Andreas Mårtensson,1 Jose Pedro Gil1,5,6 1Department of Women’s and Children’s Health, International Maternal and Child Health (IMCH), Uppsala ...
Habtemikael L +6 more
doaj
Benzbromarone (Urinorm®)の代謝・毒性および薬理作用に関する研究 [PDF]
Sporadic reports of mild hepatic dysfunction as an adverse reaction of Benzbromarone have appeared in recent years, and in some cases, fulminant hepatitis has developed. We first investigated metabolites of Benzbromarone, using LC/MS, and identified the
井上 郁夫 +3 more
core
Genetic polymorphism of cytochrome p450 (2C19) enzyme in Iranian Turkman ethnic group [PDF]
Objective: Different findings indicate that CYP2C plays a clinical role in determining interindividual and interethnic differences in drug effectiveness. The ethnic differences in the frequency of CYP2C19 mutant alleles continue to be a significant study
Ataby, O.A. +4 more
core +2 more sources

