Folate-mediated targeting of antineoplastic drugs, imaging agents, and nucleic acids to cancer cells

Susan Wang, Philip S. Low

Research output: Contribution to journalArticlepeer-review

252 Scopus citations

Abstract

The receptor for the vitamin, folic acid, is overexpressed on a number of human tumors, including cancers of the ovary, kidney, uterus, testis, brain, colon, lung, and myelocytic blood cells. Conjugates of folic acid linked via its γ-carboxyl to either a single drug molecule or assembly of molecules can bind to and enter receptor-expressing cancer cells via folate receptor-mediated endocytosis. Because the affinity of folate conjugates for cell surface folate receptors is high (K(D)~10-10 M), folic acid derivatization allows the selective delivery of diagnostic and therapeutic agents to cancer cells in the presence of normal cells. This review will summarize studies aimed at folate-mediated targeting of protein toxins, imaging agents, antisense oligodeoxynucleotides, genes, and liposomes specifically to cancer cells in vitro and in vivo.

Original languageEnglish (US)
Pages (from-to)39-48
Number of pages10
JournalJournal of Controlled Release
Volume53
Issue number1-3
DOIs
StatePublished - Apr 30 1998

Keywords

  • Cancer cell targeting
  • Cancer chemotherapy
  • Folate receptor-mediated endocytosis
  • Targeted imaging agents

ASJC Scopus subject areas

  • Pharmaceutical Science

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