Extensive genetic polymorphism in the human CYP2B6 gene with impact on expression and function in human liver.
Significant reduced CYP2B6 protein expression and S-mephenytoin N-demethylase activity were found in carriers of the C1459T (R487C) mutation, demonstrating that the extensive interindividual variability of CYP 2B6 expression and function is not only due to regulatory phenomena, but also caused by a common genetic polymorphism.
Metformin improves healthspan and lifespan in mice
- A. Martín-Montalvo, E. Mercken, R. de Cabo
- Medicine, BiologyNature Communications
- 26 July 2013
It is shown that long-term treatment with metformin starting at middle age extends healthspan and lifespan in male mice, while a higher dose (1% w/w) was toxic.
Frequency of single nucleotide polymorphisms in the P‐glycoprotein drug transporter MDR1 gene in white subjects
- I. Cascorbi, T. Gerloff, I. Roots
- Biology, MedicineClinical pharmacology and therapy
- 1 March 2001
P‐glycoprotein, the gene product of MDR1, confers multidrug resistance against antineoplastic agents but also plays an important role in the bioavailability of common drugs in medical treatment.…
Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation
- U. Zanger, M. Turpeinen, K. Klein, M. Schwab
- Biology, MedicineAnalytical and Bioanalytical Chemistry
- 10 August 2008
The elimination routes for the 200 drugs that are sold most often by prescription count in the United States were investigated and Clinically well-established polymorphic CYPs were involved in the metabolism of approximately half of those drugs, including NSAIDs metabolized mainly by CYP2C9, proton-pump inhibitors metabolized by CYD2C19, and beta blockers and several antipsychotics and antidepressants metabolizing by CYB2D6.
Clinical Pharmacogenetics Implementation Consortium (CPIC) Guideline for Dihydropyrimidine Dehydrogenase Genotype and Fluoropyrimidine Dosing: 2017 Update
- U. Amstutz, L. M. Henricks, M. Schwab
- Medicine, BiologyClinical pharmacology and therapy
- 1 February 2018
The purpose of this guideline is to provide information for the interpretation of clinical dihydropyrimidine dehydrogenase (DPYD) genotype tests so that the results can be used to guide dosing of…
Activity Levels of Tamoxifen Metabolites at the Estrogen Receptor and the Impact of Genetic Polymorphisms of Phase I and II Enzymes on Their Concentration Levels in Plasma
- T. Mürdter, W. Schroth, H. Brauch
- Biology, MedicineClinical pharmacology and therapy
- 1 May 2011
Among the poor metabolizers, 93% had (Z)‐endoxifen levels below IC90 values, underscoring the role of CYP2D6 deficiency in compromised tamoxIFen bioactivation, and carriers of reduced‐function CYp2C9 (*2, *3) alleles had lower plasma concentrations of active metabolites (P < 0.004), pointing to the roleof additional pathways.
Predictive Value of Known and Novel Alleles of CYP2B6 for Efavirenz Plasma Concentrations in HIV‐infected Individuals
CYP2B6 poor metabolizer genotypes explain to a large extent EFV pharmacokinetics and identify individuals at risk of extremely elevated EFV plasma levels.
Reduced Paneth cell alpha-defensins in ileal Crohn's disease.
- J. Wehkamp, N. Salzman, C. Bevins
- Biology, MedicineProceedings of the National Academy of Sciences…
- 2005
It is reported that patients with CD of the ileum have reduced antibacterial activity in their intestinal mucosal extracts, and changes in HD5 expression levels, comparable to those observed in CD, had a pronounced impact on the luminal microbiota.
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