Pteroic acid
Application Notes
Pteroic acid is an endogenous degradation product of folic acid (pteroyl glutamic acid). Pteroic acid is able to mediate the selective delivery of ligands to tumors overexpressing the folate receptor despite having minimal affinity, further stimulating research into the antitumor activity of pteroic acid conjugates. Investigation into the SAR of the ability of folate and pteroic acid conjugates of the hydroxamide histone deacetylase inhibitors to target folate receptor overexpressing cancer cells, showed that pteroic acid hydroxamates but not folate hydroxamates displayed anticancer activities against the folate receptor positive (FRþ) tumors KB and HeLa.
References
- Preparation of pteroic acid from folic acid. Houlihan C.M. et al. Analyt Biochem. 1972, 46, 1.
- Bacterial degradation of folic acid. Rappold H.& Bacher A. J Gen Microbiol. 1974, 85, 283.
- Inhibition of growth of leukemia cells by enzymic folate depletion. Bertino J.R. et al. Science 1971, 172, 161.
- Targeting the tumor-associated folate receptor with an 111In−DTPA conjugate of pteroic acid. Ke C-Y. et al. J Am Chem Soc. 2005, 127, 7421.
- Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids. Sodji Q.V. et al. Eur J Med Chem. 2015, 96, 340.