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An update on small molecules targeting CXCR4 as starting points for the development of anti-cancer therapeutics

Fedora Grande1, Gilda Giancotti2, Giuseppina Ioele1

  • 1Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, Via P. Bucci, 87036 Rende (CS), Italy.

European Journal of Medicinal Chemistry
|August 22, 2017
PubMed

Insights

Small molecule antagonists targeting the CXCR4 receptor and its ligand SDF-1α show promise for treating cancer. Research from 2013-2017 identified optimized compounds for potential anticancer drug development.

Area of Science:

  • Pharmacology
  • Oncology
  • Medicinal Chemistry

Background:

  • The CXCR4 receptor and its ligand SDF-1α play roles in physiological and pathological processes, notably cancer progression.
  • Dysregulation of the CXCR4/SDF-1α axis is implicated in various diseases, including metastatic cancer.
  • Targeting this axis offers a therapeutic strategy for CXCR4-mediated conditions.

Purpose of the Study:

  • To review small molecule CXCR4 antagonists published between 2013 and 2017.
  • To identify compounds with potential for treating cancers and other diseases involving the CXCR4/SDF-1α pathway.
  • To highlight promising candidates for further anticancer drug development.

Main Methods:

  • Literature search for CXCR4 antagonists reported from 2013 to 2017.
  • Focus on small molecules with claimed efficacy against CXCR4.
  • Analysis of compound origins, often stemming from optimization of existing molecules.

Main Results:

  • Numerous small molecule CXCR4 antagonists were identified in the reviewed literature.
  • Many compounds are derivatives of previously discovered molecules, indicating iterative optimization.
  • Several identified antagonists show potential as anticancer agents.

Conclusions:

  • Small molecules targeting the CXCR4/SDF-1α axis represent a significant area of research.
  • Optimized CXCR4 antagonists identified between 2013-2017 hold promise for cancer therapy.
  • Further development of these compounds could lead to novel anticancer drugs.
Keywords:
AntagonistsCXCR4CancerSmall molecules

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