This site uses cookies to improve your experience. To help us insure we adhere to various privacy regulations, please select your country/region of residence. If you do not select a country, we will assume you are from the United States. Select your Cookie Settings or view our Privacy Policy and Terms of Use.
Cookie Settings
Cookies and similar technologies are used on this website for proper function of the website, for tracking performance analytics and for marketing purposes. We and some of our third-party providers may use cookie data for various purposes. Please review the cookie settings below and choose your preference.
Used for the proper function of the website
Used for monitoring website traffic and interactions
Cookie Settings
Cookies and similar technologies are used on this website for proper function of the website, for tracking performance analytics and for marketing purposes. We and some of our third-party providers may use cookie data for various purposes. Please review the cookie settings below and choose your preference.
Strictly Necessary: Used for the proper function of the website
Performance/Analytics: Used for monitoring website traffic and interactions
In December 2023, we introduced the pharmacogenetics widget in the Open Targets Platform, which brings in data from PharmGKB on the influence of genetic variation on drug responses. Pharmacogenetics examines the link between genetics and drug response, helping in the prioritisation of drug targets that minimise the risk of adverse effects.
Introduction to Pharmacogenetics By Rose Circeo May 30, 2024 Breadcrumb Home Introduction to Pharmacogenetics The Primer on Medical and Population Genetics is a series of weekly lectures on genetics topics related to human populations and disease.
Proinflammatory cytokines, elevated during inflammation caused by infection and/or autoimmune disorders, result in reduced clearance of drugs eliminated primarily by cytochrome P450 enzymes (CYPs). However, the effect of cytokines on hepatic drug transporter expression or activity has not been well-studied.
Histone deacetylase expression and activity are often dysregulated in central nervous system (CNS) tumors, providing a rationale for investigating histone deacetylase inhibitors (HDACIs) in selected brain tumor patients. Although many HDACIs have shown potential in in vitro studies, they have had modest efficacy in vivo.
Panobinostat is a potent pan-HDAC inhibitor that has been tested in multiple studies for the treatment of brain tumors. There have been contrasting views surrounding its efficacy for the treatment of tumors in the CNS following systemic administration when examined in different models or species.
2023.12.016 Data updates Target safety We used pharmacogenetics data that informs about adverse drug response as an additional source of information on target safety. We have also introduced a pharmacogenetics widget integrating data from PharmGKB. DOI: 10.1016/j.ccell.2023.12.016 It was introduced in our 23.12
Organic anions (OA) are compounds including drugs or toxicants that are negatively charged at physiological pH and are typically transported by Organic Anion Transporters (OATs). Human OAT4 (SLC22A11) is expressed in the apical membrane of renal proximal tubules.
This study aimed to evaluate the effects of cytochrome P450 3A4 (CYP3A4) gene polymorphism and drug interaction on the metabolism of blonanserin. Human recombinant CYP3A4 was prepared using the Bac-to-Bac baculovirus expression system.
Achieving adequate exposure of a therapeutic agent at the target is a critical determinant of efficacious chemotherapy. With this in mind, a major challenge in developing therapies for central nervous system (CNS) tumors is to overcome barriers to delivery, including the blood-brain barrier (BBB).
Lenacapavir (LEN), a long-acting injectable, is the first approved human immunodeficiency virus type 1 capsid inhibitor and one of a few FDA-approved drugs that exhibit atropisomerism.
Neuroblastoma (NB) is a pediatric cancer with low survival rates in high-risk patients. 131 I-mIBG has emerged as a promising therapy for high-risk NB and kills tumor cells by radiation. Consequently, 131 I-mIBG tumor uptake and retention are major determinants for its therapeutic efficacy.
Glioblastoma (GBM) is a disease of the whole brain, with infiltrative tumor cells protected by an intact BBB. GBM has a poor prognosis despite aggressive treatment, in part due to lack of adequate drug permeability at the BBB. Standard of care GBM therapies include radiation and cytotoxic chemotherapy that lead to DNA damage.
The organic anion transporting polypeptide (OATP) 2B1 (gene name SLCO2B1 ) is an uptake transporter that facilitates cellular accumulation of its substrates. In order to assess the in vivo relevance of the transporter, we applied SLCO2B1 +/+ knock-in and Slco2b1 -/- knock-out rats.
Radiation therapy, a standard treatment option for many cancer patients, induces DNA double strand breaks (DSBs), leading to cell death. Ataxia telangiectasia mutated (ATM) kinase is a key regulator of DSB repair, and ATM inhibitors are being explored as radiosensitizers for various tumors, including primary and metastatic brain tumors.
Introducing pharmacogenetics data to the Platform This release introduces a new datasource to the Platform: the pharmacogenetics widget will incorporate data about the impact of human genetic variation on drug responses. You can find this data on the target and drug profile pages.
We recently showed that riboflavin is a selected substrate of BCRP over P-gp and demonstrated its prediction performance in preclinical DDI studies. The aim of this study was to investigate the suitability of riboflavin to assess BCRP inhibition in humans.
Creatinine, a clinical marker for kidney function, is predominantly cleared by glomerular filtration, with active tubular secretion contributing to about 30% of its renal clearance.
The natural product goldenseal is a clinical inhibitor of CYP3A activity, as evidenced by a 40-60% increase in midazolam AUC after coadministration with goldenseal. The predominant goldenseal alkaloids berberine and (-)-β-hydrastine were previously identified as time-dependent CYP3A inhibitors using human liver microsomes.
The system is a highly sensitive, cost-effective, mass spectrometry-based platform for high-throughput genetic analysis and is used globally in diverse research fields such as cancer profiling for solid tumors and liquid biopsies, inherited genetic disease testing, pharmacogenetics, agricultural genomics, and clinical research.
In recent years, pharmacogenetics research has shown significant differences in the pharmacokinetics among Caucasians, African Americans, Hispanics, and Asians, or at individual levels by stratifying groups based on genetic analysis.
Collaborators today include Synlab, PathGroup (US), SRL Diagnostics (Asia), Fundación Jimenez Díaz, The Royal Marsden NHS Foundation Trust, Istituto Nazionale Tumori Regina Elena Roma and Diatech Pharmacogenetics (EU). Two global pharmaceutical clients are also piloting the technology.
million GWAS credible sets identified are contextualised with results from gene burden analysis, pharmacogenetics or predominantly rare variation resources, drawing a richer map of the phenotypic effects of a broader range of variation. The more than 2.6
This includes L2G, rare disease clinical annotations, and pharmacogenetics annotations. This includes GWAS credible sets, molQTL credible sets, ClinVar clinical submissions, Uniprot curated variants, and pharmacogenetics annotations from PharmGKB. The Platform provides functional context for 6.5
We organize all of the trending information in your field so you don't have to. Join 15,000+ users and stay up to date on the latest articles your peers are reading.
You know about us, now we want to get to know you!
Let's personalize your content
Let's get even more personalized
We recognize your account from another site in our network, please click 'Send Email' below to continue with verifying your account and setting a password.
Let's personalize your content