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Modulators of CXCR4 and CXCR7/ACKR3 Function.

Ilze Adlere1, Birgit Caspar1, Marta Arimont1

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This review details modulators for C-X-C chemokine receptor type 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3), crucial drug targets for HIV, cancer, and inflammation. It covers structural insights, ligand selectivity, and small-molecule developments for receptor characterization.

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Area of Science:

  • Pharmacology and Drug Discovery
  • Molecular Biology
  • Structural Biology

Background:

  • C-X-C chemokine receptor type 4 (CXCR4) and atypical chemokine receptor 3 (ACKR3) are Class A G protein-coupled receptors (GPCRs).
  • These receptors are implicated as drug targets in human immunodeficiency virus (HIV) infection, cancer, and inflammatory diseases.
  • CXCR4 is one of the few chemokine receptors with an FDA-approved therapeutic agent, AMD3100.

Purpose of the Study:

  • To review known modulators of CXCR4 and ACKR3.
  • To discuss the structural relationships between these receptors and their ligands.
  • To explore the development and application of small-molecule modulators and imaging tools for receptor characterization.

Main Methods:

  • Review of existing literature on CXCR4 and ACKR3 modulators.
  • Analysis of structural data and common motifs for receptor-ligand interactions.
  • Discussion of selectivity, receptor activation, and signaling outputs of various ligand classes.

Main Results:

  • Ligand design for ACKR3 is challenging due to a lack of crystallized structures.
  • Pepducins, derived from GPCR internal loops, bind to CXCR4.
  • Small-molecule modulators have enabled the development of labeled tool compounds for in vitro and in vivo imaging.

Conclusions:

  • Significant efforts are focused on discovering and developing diverse ligands, including small molecules and peptides, for CXCR4 and ACKR3.
  • Imaging tools like fluorescent probes are vital for drug discovery in this area.
  • This review provides an overview of modulators that aid in studying CXCR4 and ACKR3 pharmacology.