Synthesis of an acetylcholine receptor-specific toxin derivative regioselectively labeled with an undecagold cluster.
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.
Kessler
P
P
Départment d'Ingéniérie et d'Etudes des Protéines (DIEP), CEA, C.E. Saclay, Gif-sur-Yvette, France.
Kotzyba-Hibert
F
F
Leonetti
M
M
Bouet
F
F
Ringler
P
P
Brisson
A
A
Ménez
A
A
Goeldner
M P
MP
Hirth
C
C
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
D003039:Cobra Neurotoxin Proteins; D018733:Nicotinic Antagonists; D050607:Organogold Compounds; D009942:Organometallic Compounds; D011978:Receptors, Nicotinic; C035797:undecagold; C025154:alpha-cobratoxin