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Integrating pharmacogenetics data: a new lens for target prioritisation

The Open Targets Blog

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.

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Introduction to Pharmacogenetics

Broad Institute

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.

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Open Targets Platform 24.03 has been released!

The Open Targets Blog

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

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Dysregulation of Human Hepatic Drug Transporters by Proinflammatory Cytokines [Metabolism, Transport, and Pharmacogenetics]

ASPET

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.

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Pharmacokinetics of panobinostat: Inter-species difference in metabolic stability [Metabolism, Transport, and Pharmacogenetics]

ASPET

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.

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Central Nervous System Distributional Kinetics of Selected Histone Deacetylase Inhibitors [Metabolism, Transport, and Pharmacogenetics]

ASPET

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.

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Characterization of hOAT4 and mOat5 as functional orthologs for renal anion uptake and efflux transport [Metabolism, Transport, and Pharmacogenetics]

ASPET

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.