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Chemical Compound Review

Pyrofolic acid     4-[(2-amino-4-oxo-1H- pteridin-6...

Synonyms: Pteroic acid, Peroic Acid, P1781_ALDRICH, CHEMBL341824, SureCN245980, ...
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Disease relevance of Pteroic acid

  • Fingerling catfish raised under controlled conditions on feed containing 130 mg/kg of pteroic acid failed to gain weight and developed anemia with the characteristic red cell morphologic features that are seen in the naturally occurring disease [1].
  • A culture, to be retained, must be active against Enterococcus faecium grown in a medium which contains a limited amount of pteroic acid but lacks activity against the microorganism grown in a medium supplemented with thymidine [2].

High impact information on Pteroic acid

  • The IC(50) of the aptamer for RTA in an in vitro translation assay is 100 nM, roughly 3 orders of magnitude lower than a small molecule inhibitor of ricin, pteroic acid, and 2 orders of magnitude lower than the best known RNA inhibitor [3].
  • Targeting the tumor-associated folate receptor with an 111In-DTPA conjugate of pteroic acid [4].
  • We conclude that severe anemia in channel catfish can be caused by abnormal folate metabolism and may be due to ingestion of folic acid-breakdown products, such as pteroic acid [1].
  • Using solid-phase chemistries, we have synthesized dipeptide derivatives of pteroic acid for the purpose of identifying the preferred site onto which a macromolecule can be chemically attached without compromising its endocytosis potential [5].
  • 4. Pteroic acid, PteGlu1 and anionic polysaccharides did not inhibit human or porcine conjugase [6].

Analytical, diagnostic and therapeutic context of Pteroic acid

  • In control studies, tumor targeting with this pteroic acid conjugate appears as effective as that seen using (111)In-DTPA-folate, a radiopharmaceutical that has progressed to clinical trials for detection of folate receptor-expressing gynecological tumors [4].


  1. Abnormal folate metabolism in feed-related anemia of cultured channel catfish. Butterworth, C.E., Plumb, J.A., Grizzle, J.M. Proc. Soc. Exp. Biol. Med. (1986) [Pubmed]
  2. Screening for new antifolates of microbial origin and a new antifolate AM-8402. Omura, S., Murata, M., Kimura, K., Matsukura, S., Nishihara, T., Tanaka, H. J. Antibiot. (1985) [Pubmed]
  3. In vitro selection of RNA molecules that inhibit the activity of ricin A-chain. Hesselberth, J.R., Miller, D., Robertus, J., Ellington, A.D. J. Biol. Chem. (2000) [Pubmed]
  4. Targeting the tumor-associated folate receptor with an 111In-DTPA conjugate of pteroic acid. Ke, C.Y., Mathias, C.J., Green, M.A. J. Am. Chem. Soc. (2005) [Pubmed]
  5. Folate-mediated drug delivery: effect of alternative conjugation chemistry. Leamon, C.P., DePrince, R.B., Hendren, R.W. Journal of drug targeting. (1999) [Pubmed]
  6. Comparison of pteroylpolyglutamate hydrolase (folate conjugase) from porcine and human intestinal brush border membrane. Gregory, J.F., Ink, S.L., Cerda, J.J. Comp. Biochem. Physiol., B (1987) [Pubmed]
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