Recent progress in the discovery and development of N-type calcium channel modulators for the treatment of pain.

Abstract

The importance of voltage-gated calcium channels (VGCCs) in basic physiological processes such as cardiac and neurological function has generated intense interest in these proteins as targets of pharmacological intervention. N-type calcium channels are a subset of VGCCs distinguished by their physiology, pharmacology and significance to the pathology of chronic pain. Despite decades of investigation, only a single drug targeting N-type channel function has entered the marketplace. This review will summarize our current understanding of the biology, physiology and pharmacology of N-type calcium channels and the implication of these features for therapeutic intervention. From this basis of understanding, recent efforts to discover and develop peptide based and small molecule modulators of N-type calcium channel function will be discussed.

• Authors: Margaret S Lee
• Journal: Progress in medicinal chemistry (Prog Med Chem) Vol. 53 Pg. 147-86 ( 2014) ISSN: 0079-6468 [Print] Netherlands
• PMID: 24418610 (Publication Type: Journal Article, Review)
• Copyright: © 2014 Elsevier B.V. All rights reserved.

Chemical References

• Calcium Channels, N-Type
• Indoles
• Peptides
• Piperazines
• Piperidines

Topics

• Amino Acid Sequence
• Animals
• Calcium Channels, N-Type (drug effects, physiology)
• Drug Discovery
• Humans
• Indoles (therapeutic use)
• Molecular Sequence Data
• Pain (drug therapy, physiopathology)
• Peptides (therapeutic use)
• Piperazines (therapeutic use)
• Piperidines (therapeutic use)