Pub. Date : 1994 Feb
PMID : 8114682
6 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Previous attempts to design inhibitors of mammalian folylpolyglutamate synthetase (FPGS) have resulted in three classes of active compounds, all of which have charged moieties in the side chain, but structural alteration of the rest of the folate molecule has not seemed to be an avenue for drug discovery. | Folic Acid | folylpolyglutamate synthase | Homo sapiens |
| 2 | Previous attempts to design inhibitors of mammalian folylpolyglutamate synthetase (FPGS) have resulted in three classes of active compounds, all of which have charged moieties in the side chain, but structural alteration of the rest of the folate molecule has not seemed to be an avenue for drug discovery. | Folic Acid | folylpolyglutamate synthase | Homo sapiens |
| 3 | We now report that substituents at the 7-, 2"-, or 3"-position of 2-desamino-2-methyl-4-hydroxyquinazoline antifolates decrease or prevent the catalysis of diglutamate formation by FPGS but are compatible with efficient binding to the reduced folate carrier system. | Folic Acid | folylpolyglutamate synthase | Homo sapiens |
| 4 | We conclude that the region of the folate molecule bounded by the 7-, 6-, 9-, 10-, 3"-, and 2"-positions, the "bay region," is of major importance both for the binding of folates and folate analogs to FPGS and for the assumption of a conformation of the enzyme-substrate complex compatible with catalysis. | Folic Acid | folylpolyglutamate synthase | Homo sapiens |
| 5 | We conclude that the region of the folate molecule bounded by the 7-, 6-, 9-, 10-, 3"-, and 2"-positions, the "bay region," is of major importance both for the binding of folates and folate analogs to FPGS and for the assumption of a conformation of the enzyme-substrate complex compatible with catalysis. | Folic Acid | folylpolyglutamate synthase | Homo sapiens |
| 6 | We conclude that the region of the folate molecule bounded by the 7-, 6-, 9-, 10-, 3"-, and 2"-positions, the "bay region," is of major importance both for the binding of folates and folate analogs to FPGS and for the assumption of a conformation of the enzyme-substrate complex compatible with catalysis. | Folic Acid | folylpolyglutamate synthase | Homo sapiens |