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Soft structure formation and cancer cell transport mechanisms of a folic acid–dipeptide conjugate

Folic acid (FA) is a low‐molecular‐weight micronutrient, which plays a critical role in the prevention of birth defects and cancers. It is also essential for biochemical pathways responsible for DNA synthesis and maintenance and for the generation of new red blood cells. Cellular trafficking of FA and folate is based on its high‐affinity binding to cognate folate receptor, a protein commonly expressed in several human cancers. Thus, folate conjugates of drugs, plasmids, biosensors, contrast, and radiodiagnostic imaging agents have been used for assisted delivery in folate receptor‐positive cancer cells, via endocytosis pathways. This report describes morphologies of soft structures from a fully characterized FA–dipeptide conjugate and detailed mechanistic studies of its cancer cell uptake, as tracked by the inherent fluorescence of the conjugate. Copyright © 2015 European Peptide Society and John Wiley & Sons, Ltd.