Propylbenzilylcholine mustard labels an acidic residue in transmembrane helix 3 of the muscarinic receptor
- PMID: 2909533
Propylbenzilylcholine mustard labels an acidic residue in transmembrane helix 3 of the muscarinic receptor
Abstract
Muscarinic acetylcholine receptors were purified from rat forebrain and labeled with [3H]N-(2-chloroethyl)N-(2',3'-[3H2]propyl)-2-aminoethylbenzilate. Cleavage of the labeled muscarinic acetylcholine receptors with a lysine-specific protease yielded labeled, glycosylated peptides about 130 and 200 residues in length, which came from different receptor sequences. The probable cleavage sites are in the second intracellular loop and in the second extracellular or third intracellular loop. The N-terminal 130 residues are disulfide-bonded to another part of the receptor structure, supporting the presence of a link between the second and third extracellular loops. The [3H]propylbenzilylcholine mustard-receptor link is cleaved by nucleophiles, acids, and bases under denaturing conditions, suggesting modification of an acidic residue. Cyanogen bromide cleavage points to transmembrane helix 3 as the site of label attachment.
Similar articles
-
Muscarinic acetylcholine receptors. Peptide sequencing identifies residues involved in antagonist binding and disulfide bond formation.J Biol Chem. 1990 Aug 15;265(23):13702-8. J Biol Chem. 1990. PMID: 2380182
-
Location in muscarinic acetylcholine receptors of sites for [3H]propylbenzilylcholine mustard binding and for phosphorylation with protein kinase C.J Neurochem. 1990 Jun;54(6):1870-81. doi: 10.1111/j.1471-4159.1990.tb04885.x. J Neurochem. 1990. PMID: 2338546
-
Distance between the propylbenzilylcholine mustard attachment site and carbohydrates and thiol groups in muscarinic acetylcholine receptor protein from rat cerebral cortex.Biochem J. 1988 May 1;251(3):657-65. doi: 10.1042/bj2510657. Biochem J. 1988. PMID: 3415640 Free PMC article.
-
Muscarinic acetylcholine receptors: structure, function subtypes and therapeutic perspectives.Postgrad Med J. 1987;63 Suppl 1:5-12. Postgrad Med J. 1987. PMID: 3321013 Review.
-
Neuroreceptor autoradiography.Monogr Neural Sci. 1984;10:120-39. doi: 10.1159/000408386. Monogr Neural Sci. 1984. PMID: 6321968 Review. No abstract available.
Cited by
-
Identification of orthosteric and allosteric site mutations in M2 muscarinic acetylcholine receptors that contribute to ligand-selective signaling bias.J Biol Chem. 2010 Mar 5;285(10):7459-74. doi: 10.1074/jbc.M109.094011. Epub 2010 Jan 5. J Biol Chem. 2010. PMID: 20051519 Free PMC article.
-
Functional role of proline and tryptophan residues highly conserved among G protein-coupled receptors studied by mutational analysis of the m3 muscarinic receptor.EMBO J. 1993 Jan;12(1):331-8. doi: 10.1002/j.1460-2075.1993.tb05661.x. EMBO J. 1993. PMID: 7679072 Free PMC article.
-
Surface masking shapes the traffic of the neuropeptide Y Y2 receptor.Peptides. 2012 Sep;37(1):40-8. doi: 10.1016/j.peptides.2012.06.008. Epub 2012 Jun 23. Peptides. 2012. PMID: 22732667 Free PMC article.
-
Site-directed mutagenesis of the m3 muscarinic receptor: identification of a series of threonine and tyrosine residues involved in agonist but not antagonist binding.EMBO J. 1991 Dec;10(12):3729-34. doi: 10.1002/j.1460-2075.1991.tb04941.x. EMBO J. 1991. PMID: 1657592 Free PMC article.
-
In vitro mutagenesis and the search for structure-function relationships among G protein-coupled receptors.Biochem J. 1992 Apr 1;283 ( Pt 1)(Pt 1):1-19. doi: 10.1042/bj2830001. Biochem J. 1992. PMID: 1314560 Free PMC article. Review. No abstract available.
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
