Literature DB >> 18537641

Ion channel screening technology.

Michael A Dabrowski1, Kim Dekermendjian, Per-Eric Lund, Johannes J Krupp, Jon Sinclair, Olof Larsson.   

Abstract

Ion channels are at present the third biggest target class in drug discovery. Primary research is continually uncovering potential new ion channel targets in indications such as cancer, diabetes and respiratory diseases, as well as the more established fields of pain, cardiovascular disease, and neurological disorders. Despite the physiological significance and therapeutic relevance in a wide variety of biological systems, ion channels still remain under exploited as drug targets. This is to a large extent resulting from the historical lack of screening technologies to provide the throughput and quality of data required to support medicinal chemistry. Although technical challenges still lie ahead, this historic bottleneck in ion channel drug discovery is now being overcome by novel technologies that can be integrated into lead generation stages of ion channel drug discovery to allow the development of novel therapeutic agents. This review describes the variety of technologies available for ion channel screening and discusses the opportunities these technologies provide. The challenges that remain to be addressed are highlighted.

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Year:  2008        PMID: 18537641     DOI: 10.2174/187152708784083867

Source DB:  PubMed          Journal:  CNS Neurol Disord Drug Targets        ISSN: 1871-5273            Impact factor:   4.388


  5 in total

Review 1.  Discovery of KV 1.3 ion channel inhibitors: Medicinal chemistry approaches and challenges.

Authors:  Špela Gubič; Louise A Hendrickx; Žan Toplak; Maša Sterle; Steve Peigneur; Tihomir Tomašič; Luis A Pardo; Jan Tytgat; Anamarija Zega; Lucija P Mašič
Journal:  Med Res Rev       Date:  2021-05-01       Impact factor: 12.944

Review 2.  Role of TRPM7 in cerebral ischaemia and hypoxia.

Authors:  Hong-Shuo Sun
Journal:  J Physiol       Date:  2017-02-08       Impact factor: 5.182

Review 3.  Voltage-gated potassium channels as therapeutic targets.

Authors:  Heike Wulff; Neil A Castle; Luis A Pardo
Journal:  Nat Rev Drug Discov       Date:  2009-12       Impact factor: 84.694

4.  Waixenicin A, a marine-derived TRPM7 inhibitor: a promising CNS drug lead.

Authors:  Hong-Shuo Sun; F David Horgen; Daniel Romo; Kenneth G Hull; Sigrid A Kiledal; Andrea Fleig; Zhong-Ping Feng
Journal:  Acta Pharmacol Sin       Date:  2020-09-29       Impact factor: 6.150

Review 5.  Role of TRPM2 in brain tumours and potential as a drug target.

Authors:  Delphine Ji; Zheng-Wei Luo; Andrea Ovcjak; Rahmah Alanazi; Mei-Hua Bao; Zhong-Ping Feng; Hong-Shuo Sun
Journal:  Acta Pharmacol Sin       Date:  2021-06-09       Impact factor: 6.150

  5 in total

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