Transferrin receptors and the targeted delivery of therapeutic agents against cancer
By Tracy R. Daniels, E. Bernabeu, José A. Rodríguez, Shabnum Patel, Maggie Kozman, D. Chiappetta, E. Holler, J. Ljubimova, G. Helguera, M. Penichet. Biochimica et Biophysica Acta, 2011
729 citations recorded by the source corpus.
Background Traditional cancer therapy can be successful in destroying tumors, but can also cause dangerous side effects. Therefore, many targeted therapies are in development. The transferrin receptor (TfR) functions in cellular iron uptake through its interaction with transferrin. This receptor is an attractive molecule for the targeted therapy of cancer since it is upregulated on the surface of many cancer types and is efficiently internalized. This receptor can be targeted in two ways: 1) for the delivery of therapeutic molecules into malignant cells or 2) to block the natural function of the receptor leading directly to cancer cell death. Scope of review In the present article we discuss the strategies used to target the TfR for the delivery of therapeutic agents into cancer cells. We provide a summary of the vast types of anti-cancer drugs that have been delivered into cancer cells employing a variety of receptor binding molecules including Tf, anti-TfR antibodies, or TfR-binding peptides alone or in combination with carrier molecules including nanoparticles and viruses. Major conclusions Targeting the TfR has been shown to be effective in delivering many different therapeutic agents and causing cytotoxic effects in cancer cells in vitro and in vivo. General significance The extensive use of TfR for targeted therapy attests to the versatility of targeting this receptor for therapeutic purposes against malignant cells. More advances in this area are expected to further improve the therapeutic potential of targeting the TfR for cancer therapy leading to an increase in the number of clinical trials of molecules targeting this receptor.
Subfields: Hematology, Nutrition and Dietetics, Oncology
View Paper: https://www.semanticscholar.org/paper/4afcd545c7ec59677a6047070a12242e6d632e08
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Citations in the corpus
- Cancer active targeting by nanoparticles: a comprehensive review of literature (2014, background): “Transferrin receptor is of particular interest in development of nanotherapeuticals because it is expressed at levels several fold higher on malignant cells than on normal cells (Daniels et al. 2012).”
- Nanomedicine in cancer therapy (2023, background): “The liposome is decorated with an anti-TfR scFv to target the transferrin receptor, which is ubiquitously overexpressed on the cell surface of multiple solid tumors.(201,202) Preclinical studies have shown that SGT-53 can specifically and effectively deliver the p53 cDNA to tumor cells, leading to s”
- Innovative approaches for cancer treatment: current perspectives and new challenges (2019, background): “Ulbrich K, Hekmatara T, Herbert E, et al. Transferrin- and transferrin-receptor-antibody-modified nanoparticles enable drug delivery across the blood-brain barrier (BBB).”
- Transferrin Receptor Is a Specific Ferroptosis Marker (2020, neutral): “TfR1 is abundantly expressed and involved in the progression of several cancers, including brain cancers, breast cancers, colon cancers, and liver cancers, suggesting that TfR1 may be a potential therapeutic target (Daniels et al., 2012).”
- Nanomedicine therapeutic approaches to overcome cancer drug resistance (2013, background): “These therapeutic antibodies, as well as targeting antibodies such as 2C5 [2] and anti-transferrin receptor mAbs [99-101], can be conjugated to various nanoparticles to improve efficacy and increase binding affinity to the cancer cells.”