Expression levels of PEPT1 and ABCG2 play key roles in 5-aminolevulinic acid (ALA)-induced tumor-specific protoporphyrin IX (PpIX) accumulation in bladder cancer

Photodiagnosis Photodyn Ther. 2013 Sep;10(3):288-95. doi: 10.1016/j.pdpdt.2013.02.001. Epub 2013 Mar 15.

Abstract

Background: A detection method widely used of late in cancer surgery is 5-aminolevulinic acid-based photodynamic diagnosis (ALA-PDD), which relies on the tumor-specific accumulation of photosensitizing protoporphyrin IX (PpIX) after the administration of ALA. In this regard, we recently reported that peptide transporter PEPT1 and human ATP-binding cassette transporter ABCG2 are key players in regulating intracellular PpIX levels. In the present study, we re-evaluated in vivo the expression of genes involved in the porphyrin biosynthesis pathway.

Methods: Using quantitative real-time (qRT)-PCR, we measured the mRNA levels in a clinical specimen of bladder cancer from a patient who had been subjected to ALA-PDD.

Results: We confirmed that PEPT1 and ABCG2 are major contributors to the regulation of tumor-specific PpIX accumulation. qRT-PCR analysis revealed a predominantly high level of PEPT1 mRNA and a very low level of ABCG2 mRNA in the bladder cancer, corresponding to the roles of these genes in vitro. These findings were further confirmed by immunohistochemical studies with PEPT1- and ABCG2-specific antibodies.

Conclusion: The induction of PEPT1 gene and the suppression of ABCG2 gene expression are among the key molecular mechanisms underlying tumor-specific PpIX accumulation after the administration of ALA in bladder cancer.

Keywords: 5-Aminolevulinic acid; ABCG2; Bladder cancer; PEPT1; Photodynamic diagnosis; Protoporphyrin IX.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • ATP Binding Cassette Transporter, Subfamily G, Member 2
  • ATP-Binding Cassette Transporters / metabolism*
  • Aminolevulinic Acid / administration & dosage*
  • Drug Therapy, Combination / methods
  • Gene Expression Regulation, Neoplastic / drug effects*
  • Gene Expression Regulation, Neoplastic / radiation effects
  • Humans
  • Metabolic Clearance Rate / drug effects
  • Metabolic Clearance Rate / radiation effects
  • Neoplasm Proteins / metabolism*
  • Peptide Transporter 1
  • Photochemotherapy / methods
  • Photosensitizing Agents / administration & dosage
  • Protoporphyrins / pharmacokinetics*
  • Signal Transduction / drug effects
  • Signal Transduction / radiation effects
  • Symporters / metabolism*
  • Tumor Cells, Cultured
  • Urinary Bladder Neoplasms / drug therapy*
  • Urinary Bladder Neoplasms / metabolism*

Substances

  • ABCG2 protein, human
  • ATP Binding Cassette Transporter, Subfamily G, Member 2
  • ATP-Binding Cassette Transporters
  • Neoplasm Proteins
  • Peptide Transporter 1
  • Photosensitizing Agents
  • Protoporphyrins
  • SLC15A1 protein, human
  • Symporters
  • Aminolevulinic Acid
  • protoporphyrin IX