Tumor-penetrating therapy for β5 integrin-rich pancreas cancer

Nat Commun. 2021 Mar 9;12(1):1541. doi: 10.1038/s41467-021-21858-1.

Abstract

Pancreatic ductal adenocarcinoma (PDAC) is characterized by marked desmoplasia and drug resistance due, in part, to poor drug delivery to extravascular tumor tissue. Here, we report that carcinoma-associated fibroblasts (CAFs) induce β5 integrin expression in tumor cells in a TGF-β dependent manner, making them an efficient drug delivery target for the tumor-penetrating peptide iRGD. The capacity of iRGD to deliver conjugated and co-injected payloads is markedly suppressed when β5 integrins are knocked out in the tumor cells. Of note, β5 integrin knock-out in tumor cells leads to reduced disease burden and prolonged survival of the mice, demonstrating its contribution to PDAC progression. iRGD significantly potentiates co-injected chemotherapy in KPC mice with high β5 integrin expression and may be a powerful strategy to target an aggressive PDAC subpopulation.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cancer-Associated Fibroblasts
  • Carcinoma, Pancreatic Ductal / drug therapy
  • Carcinoma, Pancreatic Ductal / genetics
  • Carcinoma, Pancreatic Ductal / metabolism
  • Carcinoma, Pancreatic Ductal / pathology
  • Cell Line, Tumor
  • Disease Progression
  • Drug Delivery Systems
  • Drug Therapy
  • Gene Expression Regulation, Neoplastic
  • Humans
  • Integrin beta Chains / genetics*
  • Integrin beta Chains / metabolism*
  • Mice
  • Mice, Inbred C57BL
  • Oligopeptides
  • Pancreatic Neoplasms / drug therapy
  • Pancreatic Neoplasms / genetics
  • Pancreatic Neoplasms / metabolism*
  • Pancreatic Neoplasms / pathology
  • Tumor Microenvironment
  • Xenograft Model Antitumor Assays

Substances

  • Integrin beta Chains
  • N-end cysteine peptide tumor-homing peptide
  • Oligopeptides
  • integrin beta5