Protease activated receptor-2 (PAR2): possible target of phytochemicals

J Biomol Struct Dyn. 2015 Sep;33(9):2003-22. doi: 10.1080/07391102.2014.986197. Epub 2014 Dec 13.

Abstract

The use of phytochemicals either singly or in combination with other anticancer drugs comes with an advantage of less toxicity and minimal side effects. Signaling pathways play central role in cell cycle, cell growth, metabolism, etc. Thus, the identification of phytochemicals with promising antagonistic effect on the receptor/s playing key role in single transduction may have better therapeutic application. With this background, phytochemicals were screened against protease-activated receptor 2 (PAR2). PAR2 belongs to the superfamily of GPCRs and is an important target for breast cancer. Using in silico methods, this study was able to identify the phytochemicals with promising binding affinity suggesting their therapeutic potential in the treatment of breast cancer. The findings from this study acquires importance as the information on the possible agonists and antagonists of PAR2 is limited due its unique mechanism of activation.

Keywords: Protease activated receptors; breast cancer; docking; phytochemicals; signal transduction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding Sites
  • Breast Neoplasms / chemistry*
  • Breast Neoplasms / drug therapy
  • Breast Neoplasms / genetics
  • Cell Cycle / drug effects
  • Cell Proliferation / drug effects*
  • Computer Simulation
  • Female
  • Humans
  • Phytochemicals / chemistry*
  • Phytochemicals / pharmacology
  • Protein Binding
  • Receptor, PAR-2 / chemistry*
  • Receptor, PAR-2 / genetics
  • Signal Transduction / drug effects

Substances

  • Phytochemicals
  • Receptor, PAR-2