G protein-coupled receptors in haematopoietic disruption

Expert Opin Biol Ther. 2006 Feb;6(2):109-20. doi: 10.1517/14712598.6.2.109.


Haematopoiesis is the process by which blood and immune cells are replenished from a finite number of resident bone marrow (BM) haematopoietic stem cells (HSCs). Regulatory molecules within the BM microenvironment contribute developmental signals to an interactive network capable of ensuring ordered biological processes. Many bioactive molecules contribute to the network through G protein-coupled receptors (GPCRs). GPCRs are seven-transmembrane receptors that, following ligand binding, signal by activating coupled heterotrimeric G proteins. This review focuses on those bioactive molecules that regulate haematopoietic development through GPCRs. Chemokines (SDF-1alpha, MIP-1), opioids and tachykinins (SP, NK-A) are important G protein-coupled haematopoietic regulators. Their biology in normal and diseased haematopoiesis is discussed below, as well as their potential as therapeutic targets.

Publication types

  • Review

MeSH terms

  • Animals
  • Bone Marrow Cells / cytology
  • Chemokine CCL4
  • Chemokine CXCL12
  • Chemokines / metabolism
  • Chemokines, CXC / metabolism
  • Hematologic Diseases / metabolism
  • Hematopoietic Stem Cells / metabolism*
  • Histamine / metabolism
  • Humans
  • Ligands
  • Macrophage Inflammatory Proteins / metabolism
  • Models, Biological
  • Narcotics / metabolism
  • Receptors, G-Protein-Coupled / chemistry
  • Receptors, G-Protein-Coupled / physiology*
  • Receptors, Neurokinin-1 / metabolism
  • Serotonin / metabolism
  • Signal Transduction
  • Tachykinins / metabolism


  • CXCL12 protein, human
  • Chemokine CCL4
  • Chemokine CXCL12
  • Chemokines
  • Chemokines, CXC
  • Ligands
  • Macrophage Inflammatory Proteins
  • Narcotics
  • Receptors, G-Protein-Coupled
  • Receptors, Neurokinin-1
  • Tachykinins
  • Serotonin
  • Histamine