Folate Receptor-Targeted Diagnostics and Therapeutics for Inflammatory Diseases

• Published in: Immune network Vol. 16; no. 6; pp. 337 - 343
• Main Author: Yi, Young-Su
• Format: Journal Article
• Language: English
• Published: Korea (South) 대한면역학회 01.12.2016; The Korean Association of Immunologists
• Subjects: Review; 면역학; Folate receptor; Diagnostics; Inflammatory diseases; Therapeutics; Macrophage
• ISSN: 1598-2629; 2092-6685
• DOI: 10.4110/in.2016.16.6.337

Inflammation, an innate immune response mediated by macrophages, forms the first line of defence to protect our body from the invasion of various pathogens. Although inflammation is a defensive response, chronic inflammation has been regarded as the major cause of many types of human diseases such as inflammatory/autoimmune diseases, cancers, neurological diseases, and cardiovascular diseases. Folate receptor (FR) is a cell surface glycosylphosphatidylinositol (GPI)-anchored glycoprotein, and its three isoforms, FR-α, FR-β, and FR-γ, are found in humans. Interestingly, FRs are highly expressed on a variety of cells, including cancer cells and activated macrophages, whereas their expression on normal cells is undetectable, indicating that FR-targeting could be a good selective strategy for the diagnosis and therapeutic treatment of cancers and activated macrophage-mediated inflammatory diseases. Previous studies successfully showed FR-targeted imaging of many types of cancers in animal models as well as human patients. Recently, a number of emerging studies have found that activated macrophages, which are critical players for a variety of inflammatory diseases, highly express FRs, and selective targeting of these FR-positive activated macrophages is a good approach to diagnose and treat inflammatory diseases. In this review, we describe the characteristics and structure of FRs, and further discuss FR-targeted diagnostics and therapeutics of human diseases, in particular, activated macrophage-mediated inflammatory diseases.