Inhibition of Anti-Apoptotic Bcl-2 Proteins in Preclinical and Clinical Studies: Current Overview in Cancer

Research output: Contribution to journalReview articlepeer-review

Abstract

The dynamic interplay between pro-death and pro-survival Bcl-2 family proteins is responsible for a cell's fate. Due to the recognized relevance of this family in cancer progression and response to therapy, different efforts have made in recent years in order to develop small molecules able to target anti-apoptotic proteins such as Bcl-2, Bcl-xL and Mcl-1. The limitations of the first Bcl-2 family targeted drugs, regarding on-target and off-target toxicities, have been overcome with the development of venetoclax (ABT-199), the first BH3 mimetic inhibitor approved by the FDA. The purpose of this review is to discuss the state-of-the-art in the development of drugs targeting Bcl-2 anti-apoptotic proteins and to highlight the potential of their application as single agents or in combination for improving anti-cancer therapy, focusing in particular on solid tumors.

Original languageEnglish
JournalCells
Volume9
Issue number5
DOIs
Publication statusPublished - May 21 2020

Keywords

  • Bcl-2
  • cancer
  • inhibitors

ASJC Scopus subject areas

  • Medicine(all)

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