The DOI matches its Crossref record; 4 of the 4 references it cites were found in a registry or an index.
Ion Channels as Therapeutic Targets: A Drug Discovery Perspective
Open accessAbstract
Ion channels are membrane proteins expressed in almost all living cells. The sequencing of the human genome has identified more than 400 putative ion channels, but only a fraction of these have been cloned and functionally tested. The widespread tissue distribution of ion channels, coupled with the plethora of physiological consequences of their opening and closing, makes ion-channel-targeted drug discovery highly compelling. However, despite some important drugs in clinical use today, as a class, ion channels remain underexploited in drug discovery and many existing drugs are poorly selective with significant toxicities or suboptimal efficacy. This Perspective seeks to review the ion channel family, its structural and functional features, and the diseases that are known to be modulated by members of the family. In particular, we will explore the structure and properties of known ligands and consider the future prospects for drug discovery in this challenging but high potential area.
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Cites
Glutamate Receptor Ion Channels: Structure, Regulation, and Function
Traynelis, S. F., Wollmuth, L. P., McBain, C. J., Menniti, F. S., Vance, K. M., Ogden, K. K., Hansen, K. B., Yuan, H., Myers, S. J., & Dingledine, R. (2010) · Pharmacological Reviews · doi:10.1124/pr.109.002451 · Cited by 3,568
Mutations of SCN1A, encoding a neuronal sodium channel, in two families with GEFS+2
Escayg, A., MacDonald, B. T., Meisler, M. H., Baulac, S., Huberfeld, G., An-Gourfinkel, I., Brice, A., LeGuern, E., Moulard, B., Chaigne, D., et al. (2000) · Nature Genetics · doi:10.1038/74159 · Cited by 996
Varenicline: An α4β2 Nicotinic Receptor Partial Agonist for Smoking Cessation
Coe, J. W., Brooks, P. R., Vetelino, M. G., Wirtz, M. C., Arnold, E. P., Huang, J., Sands, S. B., Davis, T. I., Lebel, L. A., Fox, C. B., et al. (2005) · Journal of Medicinal Chemistry · doi:10.1021/jm050069n · Cited by 930
Gavva, N. R., Bannon, A. W., Hovland, D. N., Lehto, S. G., Klionsky, L., Surapaneni, S., Immke, D. C., Henley, C., Arik, L., Bak, A., et al. (2007) · The Journal of Pharmacology and Experimental Therapeutics · doi:10.1124/jpet.107.125674 · Cited by 180
Cited by
Rouillard, A. D., Gundersen, G. W., Fernandez, N. F., Wang, Z., Monteiro, C. D., McDermott, M. G., & Ma’ayan, A. (2016) · Database · doi:10.1093/database/baw100 · Cited by 1,515
Transient receptor potential (TRP) channels: a clinical perspective
Kaneko, Y., & Szallasi, A. (2014) · British Journal of Pharmacology · doi:10.1111/bph.12414 · Cited by 370
Membrane Protein Structure, Function, and Dynamics: a Perspective from Experiments and Theory
Cournia, Z., Allen, T. W., Andricioaei, I., Antonny, B., Baum, D., Brannigan, G., Buchete, N.-V., Deckman, J. T., Delemotte, L., del Val, C., et al. (2015) · The Journal of Membrane Biology · doi:10.1007/s00232-015-9802-0 · Cited by 235
Chemical modulation of Kv7 potassium channels
Borgini, M., Mondal, P., Liu, R., & Wipf, P. (2021) · RSC Medicinal Chemistry · doi:10.1039/d0md00328j · Cited by 37
Lopez-Mateos, D., Narang, K., & Yarov-Yarovoy, V. (2024) · doi:10.1101/2024.10.15.618559 · Cited by 5
Metadata
- Authors
- Bagal, S. K., Brown, A. D., Cox, P. J., Omoto, K., Owen, R. M., Pryde, D. C., Sidders, B., Skerratt, S. E., Stevens, E. B., Storer, R. I., & Swain, N. A.
- Venue
- Journal of Medicinal Chemistry
- Publisher
- American Chemical Society (ACS)
- Published
- 2012-11-29
- Volume
- 56
- Issue
- 3
- Pages
- 593-624
- ISSN
- 0022-2623 (ISSN-L)
- 1520-4804
- OpenAlex
- W2051476546
- Cited by
- 316
- References
- 4
- FWCI
- 5.46
- Type
- journal article
- Language
- en
- Open access
- green
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