Dual Epithelial and Stromal Targeting in Breast Cancer Using the Phase II ROCK2 Inhibitor KD025 Guided by Intravital Imaging Technology

Abstract

A key factor that limits the efficacy of drug treatment for breast cancer is extensive deposition of extracellular matrix (ECM) or fibrosis, which (i) hinders drug delivery and (ii) provides positive biomechanical feedback signaling to tumors to enhance tumor progression and treatment resistance. We have access to the clinically relevant ROCK2 inhibitor KD025 and have confirmed here that pharmacological ROCK2 inhibition can significantly reduce fibrosis in our breast cancer models. Using cell-derived matrix assays and collagen contraction assays, we have shown that ROCK2 inhibition significantly reduces ECM production and remodeling resulting in a softer ECM. Organotypic invasion assays showed that this inhibition of ECM remodeling (stromal targeting) in combination with ROCK2inhibition during breast cancer cell invasion (epithelial targeting) significantly reduces breast cancer cell invasiveness.

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Document Details

Document Type
Technical Report
Publication Date
Mar 01, 2023
Accession Number
AD1197737

Entities

People

  • David Herrmann
  • Paul Timpson

Organizations

  • Garvan Institute of Medical Research

Tags

DTIC Thesaurus Topics

  • Abstracts
  • Animals
  • Biomedical Research
  • Breast Cancer
  • Cancer
  • Cell Physiological Processes
  • Cells
  • Combination Therapy
  • Department Of Defense
  • Governments
  • Health Services
  • Humanities
  • Inhibition
  • Inhibitors
  • Institutional Review Board
  • Laboratory Animals
  • Medical Personnel
  • Neoplasms
  • Professional Development
  • Standards
  • Therapy
  • Three Dimensional

Fields of Study

  • Biology
  • Medicine

Readers

  • Molecular Biology and Genetics
  • Oncology (Cancer Research).