Folate receptor 1

More importantly, folate plays a major role in DNA replication and cell division, which are common characteristics of rapid growth.

[6] FRα, due to its high expression in some tumors, is an attractive therapeutic target for the development of novel anti-cancer agents in order to limit toxic side-effects on off-target tissues.

[8] FRa can be overexpressed by a number of epithelial-derived tumors including ovarian, breast, renal, lung, colorectal, and brain.

[9] Therefore, antibodies to FRa are being developed for use in targeted therapies, with one example being farletuzumab, in a phase III trial for ovarian cancer.

Autoantibodies to the FRA have been linked to neurodevelopmental diseases,[10] particularly cerebral folate deficiency[11] schizophrenia[11] and autism spectrum disorder.

Schematic model of FRα used as a target in cancer therapy. [ 8 ]
Crystallographic structure of FRα protein. The folate is in green, the folate binding site is colored in orange. A Cys66Tyr substitution position induced by a pathogenic variant is represented in red while the disulfide bond between Cys66 and Cys109 is in dark blue. Figure from Mafi et al., 2020 [ 14 ]
Identification of ovarian cancer metastases located on the intestine and mesentery using fluorescence imaging of the folate receptor alpha-binding marker EC17. From Tummers et al., 2016. [ 15 ]