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Ion Channel Research

Ion Channel Research



Ion Channel Screening Ion channel screening technologies are no longer limited to high throughput instrumentation, and now include developments in reagents, cell lines and off-the-shelf assays. Research and development continues to progress at a very fast pace - theoretically, new technological breakthroughs will remove existing impediments preventing pharmaceutical companies from discovering ion channel targeted drugs. New screening technologies and resources continue to revolutionize the marketplace and promise to decrease bottlenecks while increasing output. As drugs go off-patent and pharmaceutical companies strive to find novel therapeutic solutions, automation will continue to lower costs and improve efficacy and drug safety.

Aurora Biomed focuses on ion channel screening services for drug discovery and innovative high-throughput ion channel screening technology designed to address the recent shift of resources in the pharmaceutical industry towards addressing drug safety issues earlier in the discovery process. Drug-induced QT-prolongation and cardiac arrhythmias have resulted in the emergence of the S7B, E14 guidance documents for drug safety assessment. It is of great importance to identify drug safety issues as early as possible so as to minimize investment risks. High-throughput screening (HTS) of test compounds early in the discovery process decreases costs.

The importance of hERG ion channel and hH1A screening to drug development and the discovery of human ion channel genes through the Human Genome Project created significant interest in other ion channel targets. Important contributions have been made to the knowledge of the structure and function of various ion channels through the use of ion channel mutations and next generation sequencing technologies. Ion channel dysfunction has been implicated in diseases and disorders such as cystic fibrosis, diabetes, erectile dysfunction, epilepsy, heart failure, hypertension, muscular sclerosis, obesity, schizophrenia, and sickle cell anemia. As a result, over 6 billion dollars in yearly sales and 15% of the top selling drugs are targeted at ion channels. In addition, over 500 human ion channel genes have been identified, yet only around 40 have been targeted for therapeutic effects. This suggests that the field of ion channel drug discovery will continue to attract ion channel researchers.

Aurora Biomed’s annual Ion Channel Retreat keeps the drug discovery community apprised of recent trends and developments in the field of ion channel research. Since the inaugural meeting in 2003 this yearly conference has consistently provided an environment for researchers and industry leaders to exchange ideas, discuss future collaborations and consider future research proposals and trends.

Ion channel research applications of the ICR 8000 and ICR 12000 include diverse voltage-gated potassium channels such as hERG, Kv1.1, Kv1.4 and Kv1.5, stretch-activated potassium channels, voltage-gated sodium channels such as NaV1.2, NaV1.5 and NaV1.7, ligand gated channels such as GABAA, P2X, KATP, SKCa, BKCa, and nAChR, and transporters such as Na/K-ATPase and the K-Cl Co-Transporter. Aurora Biomed’s Ion Channel Reader technology is not only limited to ion channel targets expressed in cells but also works well with synthetic vesicles constituted in the presence of ion transporting channels or pore forming proteins.

Publications:

1. High-Throughput Screening for Kv1.3 Channel Blockers Using an Improved FLIPR-Based Membrane-Potential Assay

2. Strategies for the real-time detection of Ca2+ channel events of single cells: recent advances and new possibilities