Many
lectins have been reported to have antitumor activities; identifying the
glycan ligands in
tumor cells of
lectins is crucial for
lectin clinical application. An edible mushroom
galectin, Agrocybe aegerita
lectin (AAL/AAGL), that has a high antitumor activity has been reported. In this paper, based on the
glycan array data, it is showed that the
Thomsen-Friedenreich antigen (
TF antigen)-related O-
glycans were found to be highly correlated with the antitumor activity of AAL/AAGL. Further
glycosyltransferase quantification suggested that the ratio between
GAL3ST2 and ST3GAL1 (
GAL3ST2/ST3GAL1), which determined the 3'-sulfo-TF expression level, was highly correlated with the antitumor activity of AAL/AAGL. Overexpressing the
enzyme of
GAL3ST2 in HL60 and HeLa cell lines could increase the growth inhibition ratio of AAL/AAGL from 22.7 to 43.9% and 27.8 to 39.1%, respectively. However, ST3GAL1 in Jurkat cells could decrease the growth inhibition ratio from 44.7 to 35.6%. All the data suggested that the 3'-sulfo-TF
antigen is one of the main
glycan ligands that AAL/AAGL recognizes in
tumor cells. AAL/AAGL may potentially serve as a
reagent for
cancer diagnosis and a targeted
therapy for the 3'-sulfo-TF
antigen.