Targeting ligand-receptor interactions for development of cancer therapeutics

Curr Opin Chem Biol. 2017 Jun:38:62-69. doi: 10.1016/j.cbpa.2017.03.010. Epub 2017 Mar 31.

Abstract

The biological importance and druggable properties of receptors and their cognate ligands have designated them as especially useful clinical targets. This significance continues to expand as new molecular insights underlying disease pathophysiology are uncovered. While both ligands and receptors have been exploited as drug targets, their differing biochemical properties require nuanced considerations for drug development, including where in the body they are located and how they are regulated on a cellular and molecular level. In this review we will discuss ligands and receptors as therapeutics targets, including their biodistribution and biological function. We provide examples of monoclonal antibodies (mAbs) used to modulate the activity of these targets, and discuss approaches for using engineered versions of ligands and receptors themselves for therapeutic intervention in cancer.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Discovery / methods*
  • Humans
  • Ligands
  • Molecular Targeted Therapy / methods*
  • Neoplasms / drug therapy*
  • Neoplasms / metabolism
  • Protein Binding / drug effects
  • Protein Transport / drug effects

Substances

  • Ligands