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Chemical Compound Review

CHEMBL11139     2-[[4-[(4-amino-2-oxo-3,5,7...

Synonyms: NSC-344279, AC1Q5SFW, NSC344279, AR-1J8797, NSC 344279, ...
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Disease relevance of NSC344279

  • In bacterial studies on the 2-amino-4-oxo analogues, 5-deazafolic acid proved to be a potent inhibitor of Lactobacillus casei DHFR and also the growth of both L. casei ATCC 7469 and Streptococcus faecium ATCC 8043 [1].
  • Folate behaved as a classical, steady-state inhibitor of both enzymes, whereas 5-deazafolate exhibited slow-binding inhibition (Mechanism B) with the enzyme from E. coli and classical, steady-state inhibition with the enzyme from chicken liver [2].

High impact information on NSC344279

  • The 5-deazafolate analogues were inhibitors of mouse liver FPGS, and the DATHF analogues inhibited both mouse FPGS and mouse leukemic cell GARFT [3].
  • The 2.3-A crystal structure of recombinant human dihydrofolate reductase (EC, DHFR) has been solved as a binary complex with folate (a poor substrate at neutral pH) and also as a binary complex with an inhibitor, 5-deazafolate [4].
  • By contrast, 5-deazafolate was bound about 4000 times more tightly than folate to the enzyme from E. coli and about 30 times more tightly than folate to the chicken-liver enzyme [2].

Associations of NSC344279 with other chemical compounds


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