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Advances in targeting the folate receptor in the treatment/imaging of cancers

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Abstract

The folate receptor (FR) is a recognised biomarker for tumour cells due to its overexpression on a large number of tumours. Consequently, the FR has been exploited by many diagnostic and therapeutic tools to allow targeted delivery to, and imaging of, cancer cells. Herein, we describe the many different approaches by which this has been achieved, including the attachment of folate to potent chemotherapeutic drugs to form FR-targeting small molecule–drug conjugates (SMDCs), FR-targeting antibodies (as antibody alone and as an antibody–drug conjugate), and in the form of complementary nanotechnology–folate platforms; as well as imaging variants thereof. The potential of exploiting the FR for targeted therapy/imaging has the potential to revolutionise the way several cancers are treated. These FR-targeted technologies can also pave the way for inspiring further sophisticated drug conjugates, especially as this receptor is being targeted by use of several complementary technologies: small molecule, nanoparticle and protein-based – thus providing broad and distinct knowledge in the area.

Graphical abstract: Advances in targeting the folate receptor in the treatment/imaging of cancers

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Publication details

The article was received on 12 Sep 2017, accepted on 15 Dec 2017 and first published on 18 Dec 2017


Article type: Minireview
DOI: 10.1039/C7SC04004K
Citation: Chem. Sci., 2018, Advance Article
  • Open access: Creative Commons BY license
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    Advances in targeting the folate receptor in the treatment/imaging of cancers

    M. Fernández, F. Javaid and V. Chudasama, Chem. Sci., 2018, Advance Article , DOI: 10.1039/C7SC04004K

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