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Updated: Dec 1, 2025

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Chemokine receptor CXCR4: An important player affecting the molecular-targeted drugs commonly used in hematological

Liangliang Li1,2, Ye Chai2, ChongYang Wu2

  • 1The First Clinical Medical College of Lanzhou University , Lanzhou, Gansu, China.

Expert Review of Hematology
|November 10, 2020
PubMed
Abstract

Insights

C-X-C chemokine receptor 4 (CXCR4) significantly impacts molecular-targeted drug resistance in hematological malignancies. Combining CXCR4 antagonists with targeted drugs shows synergistic effects, improving treatment outcomes.

Area of Science:

  • Hematology
  • Oncology
  • Molecular Biology

Background:

  • Molecular-targeted drugs have advanced hematological malignancy treatment.
  • Drug resistance and relapse are significant clinical challenges.
  • C-X-C chemokine receptor 4 (CXCR4) plays a role in treatment resistance.

Purpose of the Study:

  • To review the role of CXCR4 in molecular-targeted drug resistance in hematological malignancies.
  • To evaluate the clinical efficacy of combining CXCR4 antagonists with molecular-targeted drugs.

Main Methods:

  • Literature search of PubMed/Medline for studies published between 2006 and 2020.
  • Review of existing research on CXCR4 expression, mutations, and drug resistance.
  • Analysis of studies investigating the combination of molecular-targeted drugs and CXCR4 antagonists.

Main Results:

  • CXCR4 expression and mutations generally inhibit molecular-targeted drug efficacy.
  • Exceptions exist, such as bortezomib resistance in multiple myeloma associated with low CXCR4 expression.
  • Combination therapy with CXCR4 antagonists synergistically enhances anti-proliferative and pro-apoptotic effects.

Conclusions:

  • CXCR4 is a critical mediator of molecular-targeted drug resistance in hematological cancers.
  • Targeting CXCR4 in combination with molecular-targeted drugs offers a promising strategy to overcome resistance and improve patient outcomes.
Keywords:
CXCR4 antagonistsChemokine receptor CXCR4hematological malignanciesmolecular-targeted drugsresistance

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