alpha-Conotoxins are small peptides present in the venom of different species of marine snails of the Conus genus that target nicotinic acetylcholine receptors (nAChRs), with a marked specificity for muscle-type nAChRs. alpha-Conotoxin Imperialis I (alpha-Ctx-Iml), from Conus imperialis, has been recently described as a potent antagonist of mammalian neuronal alpha-bungarotoxin (alpha-Bgtx)-sensitive nAChRs. Human small cell lung carcinoma (SCLC) is a very aggressive tumor composed of neuroendocrine secretory cells. We demonstrated that human SCLC cells express neuronal-type alpha-Bgtx-sensitive nAChRs, and that their activation causes secretion of mitogenic hormones and stimulates cell proliferation, alpha-Ctx ImI inhibits both these nicotinic effects, and could therefore be considered a new important tool for investigating human neuronal-type alpha-Bgtx-sensitive nAChRs.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/0304-3940(96)12423-x | DOI Listing |
J Neurochem
July 2004
Department of Pharmacology, Oxford University, Oxford, UK.
The alpha7 nicotinic acetylcholine receptor (nAChR) plays a key role in neural development and neurodegeneration. Here, we identify a novel, modulatory receptor ligand, a 14-amino acid peptide (AEFHRWSSYMVHWK) derived from the C-terminus of acetylcholinesterase (AChE). In three different in vitro preparations, this 'AChE-peptide' is bioactive in a ligand-specific and concentration-dependent manner.
View Article and Find Full Text PDFJ Physiol
June 1998
Department of Anatomy and Cell Biology in the Center for Neurobiology and Behavior, College of Physicians and Surgeons, Columbia University, New York, NY 10032, USA.
1. Heterologous expression studies of the alpha5 subunit of the neuronal acetylcholine receptor (nAChR) gene family have demonstrated that it can participate in the function of ACh-gated channels if co-expressed with another alpha- and a beta-subunit. Previous studies also indicate prominent expression of alpha5 in both central and peripheral nervous systems.
View Article and Find Full Text PDFJ Physiol
June 1998
Department of Anatomy and Cell Biology in the Center for Neurobiology and Behavior, College of Physicians and Surgeons, Columbia University, New York, NY 10032, USA.
1. Many studies of the alpha7 subunit of the neuronal nicotinic acetylcholine receptor (nAChR) family have demonstrated that this alpha-bungarotoxin (alpha-BgTx)-binding neuronal receptor can participate in ACh-gated channels. Heterologous expression studies reveal that alpha7 subunits form homomeric channels of unusually high Ca2+ permeability.
View Article and Find Full Text PDFJ Pharmacol Exp Ther
March 1998
Department of Pharmacology and Toxicology, Medical College of Virginia, Virginia Commonwealth University, Richmond, USA.
The objective of this study was to determine which nicotinic receptor subtypes are involved in antinociception and their site of action. For that, the antinociceptive effects of several nicotinic receptor ligands were evaluated in the tail-flick test both after s.c.
View Article and Find Full Text PDFNeurosci Lett
March 1996
CNR Center of Cellular and Molecular Pharmacology, University of Milan, Italy.
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!