Therapeutic targeting of pancreatic cancer utilizing sigma-2 ligands

Surgery. 2012 Sep;152(3 Suppl 1):S152-6. doi: 10.1016/j.surg.2012.05.014. Epub 2012 Jul 3.

Abstract

One major barrier in the development of pancreas cancer therapeutics is the selective delivery of the drugs to their cellular targets. We have previously developed several sigma-2 ligands and reported the discovery of a component of the receptor for these ligands. Several sigma-2 ligands have been shown to trigger apoptosis in pancreas cancer cells. More importantly, sigma-2 ligands are internalized rapidly by the cancer cells and are capable of delivering other small-molecule therapeutics. Here we review sigma-2 ligands and conjugates as a potential novel therapy suitable for investigation in patients with pancreatic cancer.

Publication types

  • Review

MeSH terms

  • Animals
  • Apoptosis
  • Binding Sites
  • Drug Delivery Systems
  • Humans
  • Ligands
  • Membrane Proteins / metabolism
  • Molecular Targeted Therapy*
  • Pancreatic Neoplasms / drug therapy
  • Pancreatic Neoplasms / metabolism*
  • Pancreatic Neoplasms / pathology
  • Receptors, Progesterone / metabolism
  • Receptors, sigma / administration & dosage
  • Receptors, sigma / metabolism*

Substances

  • Ligands
  • Membrane Proteins
  • PGRMC1 protein, human
  • Receptors, Progesterone
  • Receptors, sigma
  • sigma-2 receptor