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Updated: Sep 7, 2025

Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents
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Amide Coupling Reaction for the Synthesis of Bispyridine-based Ligands and Their Complexation to Platinum as Dinuclear Anticancer Agents

Published on: May 28, 2014

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BCL2 G quadruplex-binding small molecules: Current status and prospects for the development of next-generation

Mamta Singh1, Rajat Gupta1, Lucia Comez2

  • 1Amity Institute of Molecular Medicine and Stem Cell Research, Amity University, Noida, UP, 201303, India.

Drug Discovery Today
|June 16, 2022
PubMed

Insights

Small molecules targeting BCL2 gene G-quadruplex structures show promise for cancer therapy. Stabilizing these structures inhibits BCL2 expression, offering a new strategy against chemotherapy resistance and poor prognosis in various human tumors.

Area of Science:

  • Oncology
  • Molecular Biology
  • Medicinal Chemistry

Background:

  • Overexpression of BCL2 (B cell lymphoma 2) is linked to chemotherapy resistance and poor prognosis in human cancers.
  • GC-rich regions in the BCL2 gene promoter can form G-quadruplex (G4) structures.

Purpose of the Study:

  • To review BCL2 G4 binding ligands as potential anticancer therapeutics.
  • To discuss structural features, binding characteristics, and biological activity of these ligands.

Main Methods:

  • Literature review of studies on BCL2 G4 structures and their ligands.
  • Analysis of in vitro and in vivo data on ligand efficacy and selectivity.

Main Results:

  • G4 structures in the BCL2 promoter can be targeted by small molecules.
  • Selective binding of ligands to BCL2 G4 structures inhibits gene expression.
  • Demonstrated in vitro and in vivo activity of characterized BCL2 G4 binding ligands.

Conclusions:

  • Targeting BCL2 G4 structures represents a promising anticancer therapeutic strategy.
  • Further research into G4-based therapeutics could lead to novel treatments for BCL2-overexpressing cancers.
Keywords:
Anticancer therapeuticsBLC2Drug discoveryG quadruplexSmall moleculesTargeted cancer therapy

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