Inhibition of brain choline acetyltransferase by tetraplatin

Tetraplatin inhibited choline acetyltransferase (CAT) from rat and bovine brain with I50 values of 13.5 and 40 microM, respectively. At 0.5 mM concentration, tetraplatin exhibited inhibition of the rat brain enzyme by 89%, whereas cisplatin yielded only 18% inhibition. With bovine CAT, tetraplatin s...

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Bibliographic Details
Published inBrain research bulletin Vol. 19; no. 2; p. 283
Main Authors Ho, B T, Feiffer, R, Tansey, L W, Newman, R A, Fields, W S, Krakoff, I H
Format Journal Article
LanguageEnglish
Published United States 01.08.1987
Subjects
Animals
Brain - enzymology
Cattle
Choline O-Acetyltransferase - antagonists & inhibitors
Cisplatin - pharmacology
Organoplatinum Compounds - pharmacology
Osmolar Concentration
Rats
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Summary:Tetraplatin inhibited choline acetyltransferase (CAT) from rat and bovine brain with I50 values of 13.5 and 40 microM, respectively. At 0.5 mM concentration, tetraplatin exhibited inhibition of the rat brain enzyme by 89%, whereas cisplatin yielded only 18% inhibition. With bovine CAT, tetraplatin showed noncompetitive inhibition with the substrate choline, Km 337 microM, Ki 29 microM, Vmax 2.83 nmoles acetylcholine formed/min/mg protein, and competitive inhibition with the substrate acetyl-CoA, Km 21 microM, Ki 16 microM, Vmax 3.85 nmoles acetylcholine formed/min/mg protein.
ISSN:0361-9230
DOI:10.1016/0361-9230(87)90094-3