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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 (), to a molecule/drug to form a "folate conjugate". [1]
For example, methotrexate is used as cancer chemotherapy because it can prevent neoplastic cells from dividing. [1] [2] Bacteria also need DHFR to grow and multiply and hence inhibitors selective for bacterial vs. host DHFR have found application as antibacterial agents. [3] Tetrahydrofolate synthesis pathway
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.
Folate-binding protein (FBP) are proteins that bind folate, typically the folate receptors and reduced folate carrier. [1]FBP can be a marker for ovarian cancer. [2]FBP can be measured to help in tumour classification to aid treatment, as it is over-expressed (20-80 fold) in more than 90% of ovarian and endometrial cancers, as well as 20-50% of breast, lung, colorectal, and renal cell carcinomas.
Dextran can be grafted with folic acid to develop doxorubicin-loaded nanoparticles. Dextran-folic acid nanoparticles effectively target tumors, reduce off-site toxicity, and prolong blood circulation. Dextran-spermine nanoparticles loaded with doxorubicin can achieve targeted and sustained drug release in tumors. [1]
It acts by blocking the body's use of folic acid. [4] Methotrexate was first made in 1947 and initially was used to treat cancer, as it was less toxic than the then-current treatments. [9] In 1956 it provided the first cures of a metastatic cancer. [10] It is on the World Health Organization's List of Essential Medicines. [11]
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