Drug intelligence / Profile preview

(10R)-10-formyl-5,8,10-trideazafolic acid

Development stage
Unknown
Modality
Small Molecules
01

Overview

(10R)-10-formyl-5,8,10-trideazafolic acid is a synthetic antifolate small molecule designed to inhibit glycinamide ribonucleotide formyltransferase (GARFT), an enzyme essential for de novo purine biosynthesis. By blocking GARFT activity, the drug disrupts nucleotide synthesis and thus inhibits cell proliferation. It is structurally related to folic acid analogs and has been studied primarily as an experimental anticancer agent targeting rapidly dividing cells[1][3][5].

Other names
2-{4-[2-(2-amino-4-hydroxyquinazolin-6-yl)-1-carboxyethyl]-benzoylamino}-pentanedioic acid(2S)-2-{4-[(1R)-2-(2-amino-4-hydroxyquinazolin-6-yl)-1-carboxyethyl]phenyl}formamido)pentanedioic acid
02

Targets

GART (GAR transformylase)ATIC (Aminoimidazole carboxamide ribonucleotide transformylase)

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