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Targeting uptake transporters for cancer imaging and treatment

Yuchen Zhang1, Joanne Wang1

  • 1Department of Pharmaceutics, University of Washington, Seattle, WA 98195, USA.

Acta Pharmaceutica Sinica. B
|January 30, 2020
PubMed

Insights

Targeting cancer cell uptake transporters, like sodium/iodine symporter (NIS) and glucose transporter 1 (GLUT1), with radiopharmaceuticals offers promising avenues for improved cancer imaging and therapy.

Area of Science:

  • Molecular Biology
  • Oncology
  • Radiopharmaceutical Chemistry

Background:

  • Cancer cells exhibit unique gene expression patterns, including altered expression of solute carrier (SLC) transporters.
  • These transporters concentrate small molecules, making them attractive targets for delivering imaging and therapeutic agents selectively to cancer cells.

Purpose of the Study:

  • To review solute carrier (SLC) transporters involved in transporting radiopharmaceuticals into cancer cells.
  • To discuss the clinical applications and future potential of targeting these transporters for cancer diagnosis and treatment.

Main Methods:

  • Review of literature focusing on specific SLC transporters: sodium/iodine symporter (NIS), norepinephrine transporter (NET), glucose transporter 1 (GLUT1), and monocarboxylate transporters (MCTs).
  • Analysis of molecular and functional characteristics, cancer-specific expression, and interaction with imaging/theranostic agents (e.g., I-123, I-131, mIBG, 18F-FDG, 13C pyruvate).

Main Results:

  • Detailed examination of NIS, NET, GLUT1, and MCTs in the context of cancer.
  • Discussion of current clinical uses and ongoing research for these transporters in cancer imaging and therapy.

Conclusions:

  • Targeting specific SLC transporters with radiopharmaceuticals presents significant opportunities for advancing cancer theranostics.
  • Further research into these transporters is crucial for developing novel strategies in cancer diagnosis and treatment.
Keywords:
CT, computed tomographyCancer imagingDDI, drug–drug interactionDTC, differentiated thyroid cancerFDA, U.S. Food and Drug AdministrationsFDG, fluorodeoxyglucoseGLUT, glucose transporterIAEA, the International Atomic Energy AgencyLACC, locally advanced cervical cancerLAT, large amino acid transporterMCT, monocarboxylate transporterMRI, magnetic resonance imagingNE, norepinephrineNET, norepinephrine transporterNIS, sodium/iodine symporterNeuroblastomaOCT, organic cation transporterPET, positron emission tomographyPHEO, pheochromocytomaRA, retinoic acidRET, rearranged during transfectionSLC, solute carrierSPECT, single-photon emission computed tomographySUV, standardized uptake valueTFB, tetrafluoroborateTSH, thyroid stimulating hormonesThyroid cancerUptake transporterWarburg effectmIBGmIBG, iobenguane/meta-iodobenzylguanidinevHL, von Hippel-Lindau

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