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.
journal_name
Biochem Pharmacoljournal_title
Biochemical pharmacologyauthors
Niedzwicki JG,Iltzsch MH,el Kouni MH,Cha Sdoi
10.1016/0006-2952(84)90710-xsubject
Has Abstractpub_date
1984-08-01 00:00:00pages
2383-95issue
15eissn
0006-2952issn
1873-2968pii
0006-2952(84)90710-Xjournal_volume
33pub_type
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更新日期：2004-02-01 00:00:00
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journal_title：Biochemical pharmacology
pub_type： 杂志文章
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更新日期：1982-03-01 00:00:00
