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Updated: Aug 23, 2025

A Flow Cytometry-based Assay to Identify Compounds That Disrupt Binding of Fluorescently-labeled CXC Chemokine Ligand 12 to CXC Chemokine Receptor 4
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Atypical chemokine receptors: emerging therapeutic targets in cancer

Robert J Torphy1, Elliott J Yee1, Richard D Schulick1

  • 1Department of Surgery, University of Colorado Anschutz Medical Campus, Aurora, CO 80045, USA.

Trends in Pharmacological Sciences
|October 28, 2022
PubMed

Insights

Atypical chemokine receptors (ACKRs) scavenge chemokines and influence the tumor microenvironment. Targeting these receptors offers new cancer treatment strategies.

Area of Science:

  • Oncology
  • Immunology
  • Molecular Biology

Background:

  • Atypical chemokine receptors (ACKRs) regulate chemokine availability through scavenging and can signal via β-arrestin.
  • Unlike conventional receptors, ACKRs do not primarily mediate immune cell migration via G protein signaling.
  • The role of ACKRs in cancer biology and the tumor microenvironment (TME) is increasingly recognized.

Purpose of the Study:

  • To review recent advancements in understanding the function of ACKRs in cancer.
  • To discuss related receptors like GPR182, CCRL2, GPR1, PITPNM3, and C5aR2.
  • To explore the therapeutic potential and challenges of targeting ACKRs in oncology.

Main Methods:

  • Literature review of recent findings on ACKR function in cancer.
  • Analysis of studies on related chemokine receptor families.
  • Discussion of pharmacological targeting strategies.

Main Results:

  • ACKRs play multifaceted roles in tumorigenesis and immune modulation within the TME.
  • Several receptors (GPR182, CCRL2, GPR1, PITPNM3, C5aR2) show ACKR-like functions.
  • Targeting ACKRs presents both opportunities and challenges for cancer therapy.

Conclusions:

  • ACKRs are significant players in cancer development and immune response.
  • Further research into ACKR-like receptors can uncover new therapeutic avenues.
  • Pharmacological targeting of ACKRs holds promise for novel cancer treatments.
Keywords:
G protein-coupled receptorarrestin-coupled receptoratypical chemokine receptorcancerchemokineimmunotherapy

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