scholarly journals Pregnane X Receptor (PXR) Polymorphisms and Cancer Treatment

Biomolecules ◽  
2021 ◽  
Vol 11 (8) ◽  
pp. 1142
Author(s):  
Aikaterini Skandalaki ◽  
Panagiotis Sarantis ◽  
Stamatios Theocharis
Keyword(s):  
Personalized Medicine ◽  
Nuclear Receptors ◽  
Antineoplastic Agents ◽  
Pregnane X Receptor ◽  
Chemotherapeutic Agents ◽  
Drug Metabolizing Enzymes ◽  
Chemotherapeutic Drugs ◽  
Metabolizing Enzymes ◽  
And Personalized Medicine ◽  
Selection Of

Pregnane X Receptor (PXR) belongs to the nuclear receptors’ superfamily and mainly functions as a xenobiotic sensor activated by a variety of ligands. PXR is widely expressed in normal and malignant tissues. Drug metabolizing enzymes and transporters are also under PXR’s regulation. Antineoplastic agents are of particular interest since cancer patients are characterized by significant intra-variability to treatment response and severe toxicities. Various PXR polymorphisms may alter the function of the protein and are linked with significant effects on the pharmacokinetics of chemotherapeutic agents and clinical outcome variability. The purpose of this review is to summarize the roles of PXR polymorphisms in the metabolism and pharmacokinetics of chemotherapeutic drugs. It is also expected that this review will highlight the importance of PXR polymorphisms in selection of chemotherapy, prediction of adverse effects and personalized medicine.

Regulation of brain drug metabolizing enzymes and transporters by nuclear receptors

2018 ◽  
Vol 50 (4) ◽  
pp. 407-414 ◽  
Author(s):  
Dan Xu ◽  
Songqiang Huang ◽  
Hui Wang ◽  
Wen Xie
Keyword(s):  
Nuclear Receptors ◽  
Drug Metabolizing Enzymes ◽  
Metabolizing Enzymes

scholarly journals The Affymetrix DMET Plus Platform Reveals Unique Distribution of ADME-Related Variants in Ethnic Arabs

2015 ◽  
Vol 2015 ◽  
pp. 1-8 ◽  
Author(s):  
Salma M. Wakil ◽  
Cao Nguyen ◽  
Nzioka P. Muiya ◽  
Editha Andres ◽  
Agnieszka Lykowska-Tarnowska ◽  
...  
Keyword(s):  
Personalized Medicine ◽  
Cytochrome P450s ◽  
Drug Metabolizing Enzymes ◽  
Gene Variants ◽  
Clinical Routine ◽  
Metabolizing Enzymes ◽  
Ethnic Populations ◽  
Unique Distribution ◽  
Clinical Potential ◽  
Distribution Trends

Background. The Affymetrix Drug Metabolizing Enzymes and Transporters (DMET) Plus Premier Pack has been designed to genotype 1936 gene variants thought to be essential for screening patients in personalized drug therapy. These variants include the cytochrome P450s (CYP450s), the key metabolizing enzymes, many other enzymes involved in phase I and phase II pharmacokinetic reactions, and signaling mediators associated with variability in clinical response to numerous drugs not only among individuals, but also between ethnic populations.Materials and Methods. We genotyped 600 Saudi individuals for 1936 variants on the DMET platform to evaluate their clinical potential in personalized medicine in ethnic Arabs.Results. Approximately 49% each of the 437 CYP450 variants, 56% of the 581 transporters, 56% of 419 transferases, 48% of the 104 dehydrogenases, and 58% of the remaining 390 variants were detected. Several variants, such as rs3740071, rs6193, rs258751, rs6199, rs11568421, and rs8187797, exhibited significantly either higher or lower minor allele frequencies (MAFs) than those in other ethnic groups.Discussion. The present study revealed some unique distribution trends for several variants in Arabs, which displayed partly inverse allelic prevalence compared to other ethnic populations. The results point therefore to the need to verify and ascertain the prevalence of a variant as a prerequisite for engaging it in clinical routine screening in personalized medicine in any given population.

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