期刊
NEUROSCIENCE LETTERS
卷 557, 期 -, 页码 27-36出版社
ELSEVIER IRELAND LTD
DOI: 10.1016/j.neulet.2013.06.057
关键词
Neuropathic pain; Calcium channels; Peptide; Anti-nociceptive; CRMP2
资金
- Indiana Clinical and Translational Sciences Institute (CTSI)
- National Institutes of Health, National Center for Research Resources, Clinical and Translational Sciences Award [RR025761]
- Indiana State Department of Health - Spinal Cord and Brain Injury Fund [A70-9-079138]
- Indiana University Biomedical Committee - Research Support Funds [2286501]
- National Scientist Development American Heart Association [SDG5280023]
- Research Inventions and Scientific Commercialization grant Indiana CTSI
- Elwert Award in Medicine
- BioCrossroads New Venture competition
- Sophia Therapeutics, LLC
- Opportunities for Research Commercialization and Economic Success (FORCES) grant initiative from the Indiana CTSI
Chronic neuropathic pain management is a worldwide concern. Pharmaceutical companies globally have historically targeted ion channels as the therapeutic catechism with many blockbuster successes. Remarkably, no new pain therapeutic has been approved by European or American regulatory agencies over the last decade. This article will provide an overview of an alternative approach to ion channel drug discovery: targeting regulators of ion channels, specifically focusing on voltage-gated calcium channels. We will highlight the discovery of an anti-nociceptive peptide derived from a novel calcium channel interacting partner - the collapsin response mediator protein 2 (CRMP2). In vivo administration of this peptide reduces pain behavior in a number of models of neuropathic pain without affecting sympathetic-associated cardiovascular activity, memory retrieval, sensorimotor function, or depression. A CRMP2-derived peptide analgesic, with restricted access to the CNS, represents a completely novel approach to the treatment of severe pain with an improved safety profile. As peptides now represent one of the fastest growing classes of new drugs, it is expected that peptide targeting of protein interactions within the calcium channel complex may be a paradigm shift in ion channel drug discovery. (C) 2013 Elsevier Ireland Ltd. All rights reserved.
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