Pub. Date : 1998 Jul 1
PMID : 9647673
4 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | We have synthesized and characterized the prototype of a new class of mechanism-based FPGS inhibitor in which a phosphonate moiety mimics the tetrahedral intermediate formed during the ligation reaction. | Organophosphonates | folylpolyglutamate synthase | Homo sapiens |
| 2 | Inhibition is not time-dependent and preincubation of FPGS with this phosphonate does not increase the degree of inhibition, suggesting that it is not a slow, tight-binding inhibitor involving a time-dependent isomerization, EI --> EI*. | Organophosphonates | folylpolyglutamate synthase | Homo sapiens |
| 3 | Substructures containing the phosphonate moiety but lacking the pterin are much less inhibitory to FPGS, indicating that a significant portion of the inhibitor binding energy is derived from the pterin moiety, a feature also observed in substrate binding. | Organophosphonates | folylpolyglutamate synthase | Homo sapiens |
| 4 | Thus, the phosphonate moiety in this analog represents an important new lead in the development of FPGS inhibitors. | Organophosphonates | folylpolyglutamate synthase | Homo sapiens |