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  • Title: Structure-activity relationship of pyrimidine base analogs as ligands of orotate phosphoribosyltransferase.
    Author: Niedzwicki JG, Iltzsch MH, el Kouni MH, Cha S.
    Journal: Biochem Pharmacol; 1984 Aug 01; 33(15):2383-95. PubMed ID: 6466360.
    Abstract:
    Eighty pyrimidine base analogs were evaluated as inhibitors of mouse liver orotate phosphoribosyltransferase (OPRTase, EC 2.4.2.10). Based on these findings and an extensive literature review, a structure-activity relationship has been formulated for the binding of pyrimidine base analogs to OPRTase. This study provides a basis for the rational design of new inhibitors of this enzyme, and several such compounds are proposed. Additionally, 4,6-dihydroxypyrimidine has been found to be a potent OPRTase inhibitor. Eleven OPRTase inhibitors were also evaluated as inhibitors of orotidine 5'-monophosphate decarboxylase (ODCase, EC 4.1.2.23). 5-Azauracil, 5-azaorotate, and barbituric acid inhibited ODCase significantly only after preincubation with PRPP and MgCl2 in the presence of cytosol.
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