Biological ActivityCXCR4 allosteric agonist (EC50 = 194 nM). Induces chemotaxis in CXCR4-expressing cells in vitro. Mobilizes polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) from bone marrow niche in vivo. Exhibits biased signaling towards Gi proteins over G13 and β-arrestin.
(Modifications: Met-1 = N-terminal Palmitoyl)
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Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cells.
Tchernychev et al.
Studying the binding interactions of allosteric agonists and antagonists of the CXCR4 receptor.
Planesas et al.
J.Mol.Graph Model., 2015;60:1
Pepducin targeting the C-X-C chemokine receptor type 4 acts as a biased agonist favoring activation of the inhibitory G protein.
Quoyer et al.
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