Recent advances in peptidomimetics antagonists targeting estrogen receptor α-coactivator interaction in cancer therapy

Bioorg Med Chem Lett. 2018 Sep 15;28(17):2827-2836. doi: 10.1016/j.bmcl.2018.05.062. Epub 2018 May 31.

Abstract

Estrogen receptor α (ERα) is a crucial target for ERα positive breast cancer treatment. Previous drug discovery efforts were focused on developing inhibitors that targeted the canonical ligand binding pockets of the ligand binding domain (LBD) of ERα. However, significant percentage of patients developed cancer relapse with drug-resistance. ERα peptidomimetic modulators have been considered as promising treatments for drug resistant breast cancers as they are targeting ERα-coactivator interacting interface instead of the ligand binding pocket of ERα. Herein, we reviewed the recent development of ERα peptidomimetics antagonists.

Keywords: Breast cancer; Estrogen receptor; Inhibitor; Peptidomimetics; Protein-protein interaction.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / therapeutic use*
  • Breast Neoplasms / drug therapy*
  • Breast Neoplasms / metabolism
  • Breast Neoplasms / pathology
  • Cell Proliferation / drug effects
  • Estrogen Receptor alpha / antagonists & inhibitors*
  • Estrogen Receptor alpha / metabolism
  • Female
  • Humans
  • Mammary Neoplasms, Experimental / drug therapy
  • Mammary Neoplasms, Experimental / metabolism
  • Mammary Neoplasms, Experimental / pathology
  • Peptidomimetics / antagonists & inhibitors*
  • Peptidomimetics / metabolism
  • Vinca Alkaloids / chemistry
  • Vinca Alkaloids / therapeutic use*

Substances

  • Antineoplastic Agents
  • Estrogen Receptor alpha
  • Peptidomimetics
  • Vinca Alkaloids