Modification of the GABA/benzodiazepine receptor with the arginine reagent, 2,3-butanedione.

Abstract:

:Treatment of either crude or purified preparations of the gamma-aminobutyrate (GABA)/benzodiazepine receptor complex with arginine-specific reagents resulted in a time- and concentration-dependent loss of [3H]muscimol binding activity. Following exposure to either 2,3-butanedione or phenylglyoxal (less than or equal to 20 mM), [3H]muscimol binding was inhibited by up to 80%. [3H]Flunitrazepam binding was much less sensitive to the effects of the reagents. Scatchard analysis of the binding data indicated that treatment with butanedione resulted in a loss of [3H]muscimol binding sites with little effect on binding affinity. Considerable protection against inactivation was provided by arginine and by the endogenous receptor ligand, GABA. These results indicate that arginine residues play a critical role in maintaining the GABA receptor in a conformation capable of ligand binding, possibly by participating in the binding site through interaction with the carboxylate moiety of GABA.

journal_name

FEBS Lett

journal_title

FEBS letters

authors

Widdows KB,Kirkness EF,Turner AJ

doi

10.1016/0014-5793(87)80204-1

subject

Has Abstract

pub_date

1987-09-28 00:00:00

pages

125-8

issue

1

eissn

0014-5793

issn

1873-3468

pii

0014-5793(87)80204-1

journal_volume

222

pub_type

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