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ACS Med Chem Lett. 2011 Dec 9;3(1):10-4. doi: 10.1021/ml200017d. eCollection 2012 Jan 12.

Prodrugs of a CXC Chemokine-12 (CXCL12) Neutraligand Prevent Inflammatory Reactions in an Asthma Model in Vivo.

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Laboratoire d'Innovation Thérapeutique, UMR 7200 CNRS/Université de Strasbourg , Faculté de Pharmacie, 74 route du Rhin, 67401 Illkirch, France.
Biotechnologie et signalisation cellulaire, UMR 7242 CNRS/Université de Strasbourg , ESBS, Bld Sébastien Brant, 67412 Illkirch, France.


Chalcone 4 (compound 1) is a small molecule that neutralizes the CXC chemokine CXCL12 and prevents it from acting on the CXCR4 and CXCR7 receptors. To overcome its poor solubility in aqueous buffers, we designed highly soluble analogues of compound 1, phosphate, l-seryl, and sulfate, all inactive by themselves on CXCL12 but when cleaved in vivo into 1, highly active locally at a low dose in a mouse airway hypereosinophilia model.


CXCL12 chemokine; CXCR4 receptor; GPCR; asthma; prodrug; solubility

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