The transferrin receptor and the targeted delivery of therapeutic agents against cancer

Daniels, Tracy R.; Bernabeu, Ezequiel; Rodríguez, José A.; Patel, Shabnum; Kozman, Maggie; Chiappetta, Diego A.; Holler, Eggehard; Ljubimova, Julia Y.; Helguera, Gustavo; Penichet, Manuel L.

doi:10.1016/j.bbagen.2011.07.016

Cited by 807Nanoparticle-Based Drug DeliveryIron Metabolism and DisordersRNA Interference and Gene Delivery

The transferrin receptor and the targeted delivery of therapeutic agents against cancer

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Daniels, Tracy R., Bernabeu, Ezequiel, Rodríguez, José A., Patel, Shabnum, Kozman, Maggie, Chiappetta, Diego A., Holler, Eggehard, Ljubimova, Julia Y. +2 more·2012·Biochimica et Biophysica Acta (BBA) - General Subjects

DOI 10.1016/j.bbagen.2011.07.016PMC PMC3500658

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Abstract

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. This article is part of a Special Issue entitled Transferrins: molecular mechanisms of iron transport and disorders.

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A variety of studies confirmed an improved anti-cancer drug uptake upon conjugation to a TfR monoclonal antibody.
“In fact, a variety of studies confirmed an improved anti-cancer drug uptake upon conjugation to a TfR monoclonal antibody [101,102,103].”
From Iron as a central player and promising target in cancer progression (2019) · cites this paper as [101]

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Authors: Daniels, T. R., Bernabeu, E., Rodríguez, J. A., Patel, S., Kozman, M., Chiappetta, D. A., Holler, E., Ljubimova, J. Y., Helguera, G., & Penichet, M. L.
Affiliations: Consejo Nacional de Investigaciones Científicas y Técnicas (AR)
University of California, Los Angeles (US)
Cedars-Sinai Medical Center (US)
Corresponding author: Helguera, Gustavo
Penichet, Manuel L.
ORCID: Bernabeu, Ezequiel
Rodríguez, José A.
Patel, Shabnum
Chiappetta, Diego A.
Holler, Eggehard
Ljubimova, Julia Y.
Helguera, Gustavo
Penichet, Manuel L.
Venue: Biochimica et Biophysica Acta (BBA) - General Subjects
Publisher: Elsevier BV
Published: 2012-03
Volume: 1820
Issue: 3
Pages: 291-317
ISSN: 0304-4165 (ISSN-L)
DOI: 10.1016/j.bbagen.2011.07.016
PMC: PMC3500658
OpenAlex: W2027437657
Cited by: 807
References: 232
Citations by year: 2026: 37 · 2025: 50 · 2024: 69 · 2023: 55 · 2022: 57 · 2021: 65 · 2020: 69 · 2019: 75 · 2018: 64 · 2017: 52 · 2016: 59 · 2015: 55 · 2014: 39 · 2013: 47 · 2012: 14
FWCI: 1.91
Type: journal article
Language: en
Open access: green
hdl.handle.net
Licence: other-oa
www.elsevier.com/tdm/userlicense/1.0/ (tdm)
Locations: Biochimica et Biophysica Acta (BBA) - General Subjects (publishedVersion)
PubMed (publishedVersion)
Conicet (publishedVersion, other-oa)
Europe PMC (PubMed Central) (acceptedVersion)
PubMed Central (acceptedVersion)
CONICET Digital (CONICET) (submittedVersion, cc-by-nc-nd)
Funders: NIH/NCI (R01CA136841, R01CA107023, R01CA123495, R01CA57152, U01CA151815, K01CA138559)
Howard Hughes Medical Institute Gilliam Fellowship
Whitcome Fellowship of the Molecular Biology Institute at UCLA
National Agency for Promotion of Science and Technology (ANPCyT-FONARSEC PICT-PRH 2008-00315)
Topics: Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
Health Sciences › Medicine › Hematology › Iron Metabolism and Disorders
Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
Keywords: transferrin receptor, targeted cancer therapy, receptor-mediated drug delivery, transferrin, nanoparticles, viral vectors, iron absorption, cancer cell death
MeSH terms: Antibodies, Monoclonal, Antineoplastic Agents, Carrier Proteins, Genetic Vectors, Humans, Iron, Neoplasms, Receptors, Transferrin, Drug Delivery Systems, Apoptosis, Molecular Targeted Therapy

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The transferrin receptor and the targeted delivery of therapeutic agents against cancer

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