Folate targeting
Folate targeting is a method utilized in biotechnology for drug delivery purposes. This Trojan Horse process, which was created by Drs. Christopher P. Leamon and Philip S. Low, involves the attachment of the vitamin, folate (folic acid), to a molecule/drug to form a "folate conjugate". Based on the natural high affinity of folate for the folate receptor protein (FR), which is commonly expressed on the surface of many human cancers, folate-drug conjugates also bind tightly to the FR and trigger cellular uptake via endocytosis. Molecules as diverse as small radiodiagnostic imaging agents to large DNA plasmid formulations have successfully been delivered inside FR-positive cells and tissues.
Folic acid (FA, folate or vitamin B9), is a vital nutrient required by all living cells for nucleotide biosynthesis and for the proper metabolic maintenance of 1-carbon pathways. Aside from its cofactor role for intracellular enzymes, FA also displays high affinity for the folate receptor (FR), a glycosylphosphatidyinositol-linked protein that captures its ligands from the extracellular milieu and transports them inside the cell via a non-destructive, recycling endosomal pathway. The FR is also a recognized tumor antigen/biomarker. Because of this, diagnostic and therapeutic methods which exploit the FR’s function are being developed for cancer.
The FR is an emerging therapeutic target for diagnosis and treatment of cancer and chronic inflammatory diseases. Expression of the FR is selectively upregulated on certain malignant cells and activated macrophages. Overexpression of the FR on these types of cells is clinically significant because they designate areas where the physiological symptoms of disease are most extensive. The malignant cells indicate the presence of tumors associated with ovarian, lung, breast, kidney, brain, endometrial, and colon cancer. Macrophages become activated in chronic diseases such as rheumatoid arthritis, Crohn’s disease, ulcerative colitis, psoriasis, atherosclerosis, diabetes, and most other inflammatory diseases.
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