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

ABSTRACT: 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.

SUBMITTER: Gasparik V 

PROVIDER: S-EPMC4025865 | biostudies-other | 2012 Jan

REPOSITORIES: biostudies-other

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

Gasparik Vincent V   Daubeuf François F   Hachet-Haas Muriel M   Rohmer François F   Gizzi Patrick P   Haiech Jacques J   Galzi Jean-Luc JL   Hibert Marcel M   Bonnet Dominique D   Frossard Nelly N  

ACS medicinal chemistry letters 20111209 1

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. ...[more]