Kainyl-bovine serum albumin: a novel ligand of the kainate sub-type of glutamate receptor with a very high binding affinity.
Bovine serum albumin has been conjugated with kainylaminooxyacetylglycine to afford a multivalent kainylated protein called kainyl-bovine serum albumin (KA-BSA). This derivative, radiolabelled with 125I to more than 5000 Ci/mmol, was found to interact in the chick, goldfish and rat brain to specific membranous sites displaying the pharmacological properties attributed to the kainate sub-type of glutamate receptor. Measurements of the kinetics of association and dissociation of KA-BSA showed a quasi-irreversible binding with dissociation constants in the subpicomolar and nanomolar range. The chemical properties and the binding characteristics of KA-BSA suggest that it interacts mainly with kainate binding sites present in clusters in the membrane. Localization of the KA-BSA binding sites, by autoradiography in the chick cerebellum and by immunoperoxidase staining in the goldfish cerebellum, revealed an exclusive association with the molecular layer.
Eshhar
N
N
Department of Neurobiology, Weizmann Institute of Science, Rehovot, Israel.
Lederkremer
G
G
Beaujean
M
M
Goldberg
O
O
Gregor
P
P
Ortega
A
A
Triller
A
A
Teichberg
V I
VI
D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism*; D002531:Cerebellum / Q000378:metabolism; D002645:Chickens; D005998:Glycine / Q000031:analogs & derivatives* / Q000378:metabolism; D006054:Goldfish; D007608:Kainic Acid / Q000031:analogs & derivatives* / Q000378:metabolism; D007700:Kinetics; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D017470:Receptors, Glutamate; D017981:Receptors, Neurotransmitter / Q000378:metabolism*; D013347:Subcellular Fractions / Q000378:metabolism
D017470:Receptors, Glutamate; D017981:Receptors, Neurotransmitter; C058524:kainylaminooxyacetylglycine; D007608:Kainic Acid; D005998:Glycine