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Bioconjug Chem. 2019 Mar 20;30(3):487-502. doi: 10.1021/acs.bioconjchem.8b00919. Epub 2019 Jan 23.

Bench to Bedside: Albumin Binders for Improved Cancer Radioligand Therapies.

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Laboratory of Molecular Imaging and Nanomedicine (LOMIN), National Institute of Biomedical Imaging and Bioengineering (NIBIB) , National Institutes of Health (NIH) , Bethesda , Maryland 20892 , United States.
Department of Molecular Oncology , BC Cancer , Vancouver , British Columbia V5Z 1L3 , Canada.


Radioligand therapy (RLT) relies on the use of pharmacophores to selectively deliver ionization energy to cancers to exert its tumoricidal effects. Cancer cells that are not directly targeted by a radioconjugate remain susceptible to RLT because of the crossfire effect. This is significant given the inter- and intra-heterogeneity of tumors. In recent years, reversible albumin binders have been used as simple "add-ons" for radiopharmaceuticals to modify pharmacokinetics and to enhance therapeutic efficacy. In this Review, we discuss recent advances in albumin binder platforms used in RLT, with an emphasis on 4-( p-iodophenyl)butyric acid and Evans blue derivatives. We focus on four biological systems pertinent to oncology that utilize this class of compounds: folate receptor, integrin αvβ3, somatostatin receptor, and prostate-specific membrane antigen. Finally, we offer our perspectives on albumin binders for RLT, highlighting future areas of research that will help propel the technology further for clinical use.

[Indexed for MEDLINE]

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