Abstract
There is wide interpatient variability in drug response and toxicity to standard doses of most anticancer medications. Genetic polymorphisms in genes encoding metabolic enzymes, receptors and drug transporters targeted by anticancer medications are often found, in part, to be responsible for the observed variability. Approximately 80% of all sequence variations residing in genes is in the form of single nucleotide polymorphisms or SNPs. The location of SNPs can be in the protein coding sequence, regulatory regions or at exon-intron boundaries of genes. Adverse drug reactions resulting from these sequence variations are due to changes in the activity of the encoded protein (in many instances the protein is non-functional) or perturbations in the level of gene expression. The goal of pharmacogenetic testing is to identify genetic polymorphisms that predispose patients to an adverse drug reaction, thereby allowing the health care provider to make informed decisions pertaining to the type of drug, dosage and dosage scheduling to be administered.
Keywords: Pharmacogenetics, single nucleotide polymorphisms, genetic variation, thiopurine S-methyltransferase, thymidylate synthase, dihydropyrimidine dehydrogenase, ATP-binding cassette transporters, multidrug resistance-associated protein, cancer health disparities.
Anti-Cancer Agents in Medicinal Chemistry
Title: Pharmacogenetics of Drug Metabolizing Enzymes and Transporters: Effects on Pharmacokinetics and Pharmacodynamics of Anticancer Agents
Volume: 10 Issue: 8
Author(s): Norman H. Lee
Affiliation:
Keywords: Pharmacogenetics, single nucleotide polymorphisms, genetic variation, thiopurine S-methyltransferase, thymidylate synthase, dihydropyrimidine dehydrogenase, ATP-binding cassette transporters, multidrug resistance-associated protein, cancer health disparities.
Abstract: There is wide interpatient variability in drug response and toxicity to standard doses of most anticancer medications. Genetic polymorphisms in genes encoding metabolic enzymes, receptors and drug transporters targeted by anticancer medications are often found, in part, to be responsible for the observed variability. Approximately 80% of all sequence variations residing in genes is in the form of single nucleotide polymorphisms or SNPs. The location of SNPs can be in the protein coding sequence, regulatory regions or at exon-intron boundaries of genes. Adverse drug reactions resulting from these sequence variations are due to changes in the activity of the encoded protein (in many instances the protein is non-functional) or perturbations in the level of gene expression. The goal of pharmacogenetic testing is to identify genetic polymorphisms that predispose patients to an adverse drug reaction, thereby allowing the health care provider to make informed decisions pertaining to the type of drug, dosage and dosage scheduling to be administered.
Export Options
About this article
Cite this article as:
H. Lee Norman, Pharmacogenetics of Drug Metabolizing Enzymes and Transporters: Effects on Pharmacokinetics and Pharmacodynamics of Anticancer Agents, Anti-Cancer Agents in Medicinal Chemistry 2010; 10 (8) . https://dx.doi.org/10.2174/187152010794474019
DOI https://dx.doi.org/10.2174/187152010794474019 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
Call for Papers in Thematic Issues
Induction of cell death in cancer cells by modulating telomerase activity using small molecule drugs
Telomeres are distinctive but short stretches present at the corners of chromosomes and aid in stabilizing chromosomal makeup. Resynthesis of telomeres supported by the activity of reverse transcriptase ribonucleoprotein complex telomerase. There is no any telomerase activity in human somatic cells, but the stem cells and germ cells undergone telomerase ...read more
Role of natural compounds as anti anti-cancer agents
Cancer is considered the leading cause of worldwide mortality, accounting for nearly 10 million deaths in 2022. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy remains an important approach in treatment o f several types of cancers, even though ...read more
Signaling and enzymatic modulators in cancer treatment
Cancer accounts for nearly 10 million deaths in 2022 and is considered the leading cause of worldwide mortality. Cancer outcome can be improved through an appropriate screening and early detection and through an efficient clinical treatment. Chemotherapy, radiotherapy and surgery are the most important approach for the treatment of several ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Diabetes and Antioxidants: Myth or Reality?
Current Vascular Pharmacology Editorial [Hot Topic: Advanced Imagings of Wallerian Degeneration, Pancreatobiliary System, Uterine Cervical Cancer, Periventricular Leukomalacia, Living Cells as well as MR Contrast Agent and QC of SPECT/CT]
Current Medical Imaging Electrochemical Nucleic Acid-Based Biosensing of Drugs of Abuse and Pharmaceuticals
Current Medicinal Chemistry Histone Deacetylases as Targets for Dietary Cancer Preventive Agents: Lessons Learned with Butyrate, Diallyl Disulfide, and Sulforaphane
Current Drug Targets Editorial:[Special Issue: Post-Translational Proteomics and its Application (Guest Editor: Qing-Yu He)]
Current Proteomics Nonsteroidal Aromatase Inhibitors for the Treatment of Breast Cancer: An Update
Anti-Cancer Agents in Medicinal Chemistry The Role of STAT3 Signaling in Mediating Tumor Resistance to Cancer Therapy
Current Drug Targets Antibodies in Single-Chain Format Against Tumour-Associated Antigens:Present and Future Applications
Current Medicinal Chemistry Dual-target Inhibitors Based on BRD4: Novel Therapeutic Approaches for Cancer
Current Medicinal Chemistry PI3K Signaling in Chronic Obstructive Pulmonary Disease: Mechanisms, Targets, and Therapy
Current Medicinal Chemistry Synthesis and Biological Interest of Structured Docosahexaenoic Acid–Containing Triacylglycerols and Phospholipids
Current Organic Chemistry Exploring Energy Profiles of Protein-Protein Interactions (PPIs) Using DFT Method
Letters in Drug Design & Discovery Molecular and Cellular Activities of Vitamin E Analogues
Mini-Reviews in Medicinal Chemistry Biomaterials for Gene Delivery Atelocollagen-mediated Controlled Release of Molecular Medicines
Current Gene Therapy The First Total Synthesis of Tarennane, a Potent Antioxidant Chalcone Constituent from Tarenna Attenuate or Magnolia Officinalis
Letters in Organic Chemistry New Features in the Treatment of Androgen-Independent Prostate Cancer
Current Pharmaceutical Design Use of Nanotechnology in Diagnosis and Treatment of Hepatic Fibrosis: A Review
Current Drug Delivery Lung Nodule Detection Using Polygon Approximation and Hybrid Features from CT Images
Current Medical Imaging Dendrimer-Curcumin Conjugate: A Water Soluble and Effective Cytotoxic Agent Against Breast Cancer Cell Lines
Anti-Cancer Agents in Medicinal Chemistry Antioxidant Supplements, Genetics and Chemotherapy Outcomes
Current Cancer Therapy Reviews