Structure−Activity Studies and Analgesic Efficacy ofN-(3-Pyridinyl)-Bridged Bicyclic Diamines, Exceptionally Potent Agonists at Nicotinic Acetylcholine Receptors

2007 ◽  
Vol 50 (15) ◽  
pp. 3627-3644 ◽  
Author(s):  
William H. Bunnelle ◽  
Jerome F. Daanen ◽  
Keith B. Ryther ◽  
Michael R. Schrimpf ◽  
Michael J. Dart ◽  
...  
Keyword(s):  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Analgesic Efficacy ◽  
Nicotinic Acetylcholine ◽  
Structure Activity ◽  
Bicyclic Diamines

scholarly journals Mutagenesis of α-Conotoxins for Enhancing Activity and Selectivity for Nicotinic Acetylcholine Receptors

Toxins ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 113 ◽  
Author(s):  
Matthew W. Turner ◽  
Leanna A. Marquart ◽  
Paul D. Phillips ◽  
Owen M. McDougal
Keyword(s):  
Nicotinic Acetylcholine Receptors ◽  
Acetylcholine Receptors ◽  
Physiological Role ◽  
Molecular Probes ◽  
Nicotinic Acetylcholine ◽  
The Past ◽  
Structure Activity ◽  
Marine Snails ◽  
Composition And Structure

Nicotinic acetylcholine receptors (nAChRs) are found throughout the mammalian body and have been studied extensively because of their implication in a myriad of diseases. α-Conotoxins (α-CTxs) are peptide neurotoxins found in the venom of marine snails of genus Conus. α-CTxs are potent and selective antagonists for a variety of nAChR isoforms. Over the past 40 years, α-CTxs have proven to be valuable molecular probes capable of differentiating between closely related nAChR subtypes and have contributed greatly to understanding the physiological role of nAChRs in the mammalian nervous system. Here, we review the amino acid composition and structure of several α-CTxs that selectively target nAChR isoforms and explore strategies and outcomes for introducing mutations in native α-CTxs to direct selectivity and enhance binding affinity for specific nAChRs. This review will focus on structure-activity relationship studies involving native α-CTxs that have been rationally mutated and molecular interactions that underlie binding between ligand and nAChR isoform.

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