title: Synthesis of an acetylcholine receptor-specific toxin derivative regioselectively labeled with an undecagold cluster.
abstract: The regioselective modification of a snake curaremimetic toxin is described. Toxin-alpha from Naja nigricollis was derivatized with an electron-dense maleimido undecagold cluster 5. The cluster-bound obtained toxin 8 has a very high affinity for the cholinergic binding site (Ki = 70 pM) of Torpedo marmorata nicotinic receptor. It is harboring a compact heavy atom core of about 8 A which makes it very useful for electron microscopy experiments.
authors.affiliation: Départment d'Ingéniérie et d'Etudes des Protéines (DIEP), CEA, C.E. Saclay, Gif-sur-Yvette, France.
authors.forename: P
authors.initials: P
authors.lastname: Kessler
authors.forename: F
authors.initials: F
authors.lastname: Kotzyba-Hibert
authors.forename: M
authors.initials: M
authors.lastname: Leonetti
authors.forename: F
authors.initials: F
authors.lastname: Bouet
authors.forename: P
authors.initials: P
authors.lastname: Ringler
authors.forename: A
authors.initials: A
authors.lastname: Brisson
authors.forename: A
authors.initials: A
authors.lastname: Ménez
authors.forename: M P
authors.initials: MP
authors.lastname: Goeldner
authors.forename: C
authors.initials: C
authors.lastname: Hirth
mesh_terms: D000818:Animals; D001665:Binding Sites; D003039:Cobra Neurotoxin Proteins / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism; D066298:In Vitro Techniques; D015394:Molecular Structure; D018733:Nicotinic Antagonists; D050607:Organogold Compounds; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000378:metabolism; D011978:Receptors, Nicotinic / Q000378:metabolism; D014101:Torpedo / Q000378:metabolism
chemical_list: D003039:Cobra Neurotoxin Proteins; D018733:Nicotinic Antagonists; D050607:Organogold Compounds; D009942:Organometallic Compounds; D011978:Receptors, Nicotinic; C035797:undecagold; C025154:alpha-cobratoxin