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Organophosphate analogs of biologically active compounds. XIV. Halophosphonate analogs of ATP as acetyl CoA carboxylase inhibitors

Biriukov, A.I.; Tarusova, N.B.; Amontov, S.G.; Osipova, T.I.; Goriachenkova, E.V.

Bioorganicheskaia Khimiia 11(5): 598-604

1985

ISSN/ISBN: 0132-3423
PMID: 2864043
Document Number: 249338
Halophosphonate ATP analogues pp[CHBr]pA and p[CHBr]ppA synthesised from bromomethylenebisphosphonate and adenosine derivatives, proved to be effective competitive inhibitors of Ac-CoA-carboxylase (CE 6.4.1.2) from rat liver (Ki = 0,2 mM). The inhibitory effects of both analogues were reversible and higher than those of some other ATP analogues. Another enzyme, Ac-CoA-synthetase (CE 6.2.1.1), with a different mode of ATP-cleavage showed wider specificity to ATP-analogues than Ac-CoA-carboxylase.

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