292045-49-9Relevant academic research and scientific papers
A step-wise synthetic approach is necessary to access γ-conjugates of folate: Folate-conjugated prodigiosenes
Figliola, Carlotta,Marchal, Estelle,Groves, Brandon R.,Thompson, Alison
, p. 14078 - 14092 (2019/05/21)
Despite the vast literature that describes reacting folic acid with a pharmacophore, this route is ineffective in providing the correct regioisomer of the resulting conjugate. We herein present a step-wise route to the preparation of nine folate conjugate
Cryptophane-Folate Biosensor for 129Xe NMR
Khan, Najat S.,Riggle, Brittany A.,Seward, Garry K.,Bai, Yubin,Dmochowski, Ivan J.
, p. 101 - 109 (2015/01/30)
Folate-conjugated cryptophane was developed for targeting cryptophane to membrane-bound folate receptors that are overexpressed in many human cancers. The cryptophane biosensor was synthesized in 20 nonlinear steps, which included functionalization with folate recognition moiety, solubilizing peptide, and Cy3 fluorophore. Hyperpolarized 129Xe NMR studies confirmed xenon binding to the folate-conjugated cryptophane. Cellular internalization of biosensor was monitored by confocal laser scanning microscopy and quantified by flow cytometry. Competitive blocking studies confirmed cryptophane endocytosis through a folate receptor-mediated pathway. Flow cytometry revealed 10-fold higher cellular internalization in KB cancer cells overexpressing folate receptors compared to HT-1080 cells with normal folate receptor expression. The biosensor was determined to be nontoxic in HT-1080 and KB cells by MTT assay at low micromolar concentrations typically used for hyperpolarized 129Xe NMR experiments.
