CXCR4 antagonist

A CXCR4 antagonist is a substance which blocks the CXCR4 receptor and prevent its activation. Blocking the receptor stops the receptor's ligand, CXCL12, from binding which prevents downstream effects. CXCR4 antagonists are especially in important for hindering cancer progression because one of the downstream effects initiated by CXCR4 receptor activation is cell movement which helps the spread of cancer, known as metastasis. The CXCR4 receptor has been targeted by antagonistic substances since being identified as a co-receptor in HIV and assisting the development of cancer.[1] Macrocyclic ligands have been utilised as CXCR4 antagonists.[2]

References

  1. ↑ Knight, James C (2012). "Nuclear (PET/SPECT) and optical imaging probes targeting the CXCR4 chemokine receptor". MedChemComm 3: 1039. doi:10.1039/c2md20117h.
  2. ↑ Burke, Benjamin P. (2013). "Macrocyclic coordination chemistry". Annu. Rep. Prog. Chem., Sect A: Inorg. Chem. 109: 232. doi:10.1039/c3ic90032k.