Targeting L-type amino acid transporter 1 for anticancer therapy: clinical impact from diagnostics to therapeutics

Expert Opin Ther Targets. 2015;19(10):1319-37. doi: 10.1517/14728222.2015.1044975. Epub 2015 May 12.

Abstract

Introduction: L-type amino acid transporter 1 (LAT1) is one of the amino acid transporters. It is overexpressed in various types of cancer cells, while it is produced restrictedly in normal tissues.

Areas covered: We discuss its characteristics in cancer cells compared with normal cells. We also mention the current applications to target LAT1 for anticancer therapy focusing on prognostic biomarkers, radio-labeled tumor imaging reagents, amino acid-stapled prodrugs, LAT1-mediated enhanced transport of anticancer drugs and LAT1 inhibitors.

Expert opinion: LAT1 can be a versatile target to promisingly develop transporter-based drugs with enhanced drug delivery potential for anticancer therapy.

Keywords: L-type amino acid transporter 1; anticancer drug; cancer; inhibitor; prodrug; prognostic biomarker; tumor imaging.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology*
  • Biomarkers, Tumor / metabolism
  • Drug Delivery Systems
  • Drug Design
  • Humans
  • Large Neutral Amino Acid-Transporter 1 / metabolism*
  • Neoplasms / diagnosis
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Prognosis

Substances

  • Antineoplastic Agents
  • Biomarkers, Tumor
  • Large Neutral Amino Acid-Transporter 1