Abstract
Since the discovery of the overexpression of alpha folate receptors (α-FR) in different types of epithelial origin cancers, the arising implications in diagnosis, prognosis and therapy have been thoroughly studied. The α-FR is a glycosylphosphatidylinositol-anchored protein with high affinity for 5-methyltetrahydrofolate, the predominant plasma folate. The expression of FRα in healthy cells is found to be only on the apical surface, but the expression in numerous carcinomas of epithelial origin is 100-300 times higher than on healthy cells and it is in the order of 1-10 million receptor copies per cell. Due to the increased expression of α-FR in epithelial tumor cells, it has been emphasized that this receptor could represent a useful target for the development of new and selective anticancer drugs. For targeted delivery to FR expressing cells, it is involved the covalent linkage of folate to a variety of molecules, including chemotherapy or imaging agents. Exploiting the overexpression of α-FR in cervical dysplasia and cervical cancer, a new, cost effective and high sensitivity screening test has been developed. Keywords: folate receptor, gynecologic oncology, folate receptor-mediated staining procedures, cervical cancer screening
Highlights
Since the discovery of the overexpression of alpha folate receptors (α-FR) in different types of epithelial origin cancers, the arising implications in diagnosis, prognosis and therapy have been thoroughly studied
In vitro and in vivo studies have stated that the expression of alpha folate receptor (α-FR) allows epithelial tumor cells to proliferate even under conditions of limited folate supply, leading to α-FR expression, which can be considered as an acquired marker of tumor cell proliferation, tumor biology and patient prognosis [2,4]
Recent studies have reported a variable expression of alpha FRs in carcinomas of the ovary and endometrium, non-small cell lung adenocarcinoma, clear cell renal carcinoma, colorectal carcinoma, breast carcinoma, high grade cervical dysplasia, cervical cancer [5,6]
Summary
Since the discovery of the overexpression of alpha folate receptors (α-FR) in different types of epithelial origin cancers, the arising implications in diagnosis, prognosis and therapy have been thoroughly studied. 12 ♦ 2019 the folate and the expression and distribution of α-FRs in non-cancerous tissue is largely confined to cells crucial for embryonic development. The high systemic toxicity of cytostatic drugs led the way in developing the targeted delivery into the tumor cells as a desired goal in modern cancer chemotherapy [13,14,15,16].
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