PHARMACOLOGICAL STUDIES ON 4 (OR 5)-AMINOIMIDAZOLE-5 (OR 4)-CARBOXAMIDE (AICA) DERIVATIVES

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Pharmacological studies on 4 (or 5)-aminoimidazole-5 (or 4)-carboxamide (AICA) derivatives.

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Role of 4-aminoimidazole-5-carboxamide in purine synthesis by Escherichia coli.

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Inhibition of 5-aminoimidazole-4-carboxamide ribotide transformylase, adenosine deaminase and 5'-adenylate deaminase by polyglutamates of methotrexate and oxidized folates and by 5-aminoimidazole-4-carboxamide riboside and ribotide.

With the use of a continuous spectrophotometric assay and initial rates determined by the method of Waley [Biochem. J. (1981) 193, 1009-1012] methotrexate was found to be a non-competitive inhibitor, with Ki(intercept) = 72 microM and Ki(slope) = 41 microM, of 5-aminoimidazole-4-carboxamide ribotide transformylase, whereas a polyglutamate of methotrexate containing three gamma-linked glutamate ...

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ژورنال

عنوان ژورنال: The Japanese Journal of Pharmacology

سال: 1967

ISSN: 0021-5198,1347-3506

DOI: 10.1254/jjp.17.668