title: 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.
authors.affiliation: Laboratoire d'Innovation Thérapeutique, UMR 7200 CNRS/Université de Strasbourg , Faculté de Pharmacie, 74 route du Rhin, 67401 Illkirch, France.
authors.forename: Vincent
authors.initials: V
authors.lastname: Gasparik
authors.affiliation: Laboratoire d'Innovation Thérapeutique, UMR 7200 CNRS/Université de Strasbourg , Faculté de Pharmacie, 74 route du Rhin, 67401 Illkirch, France.
authors.forename: François
authors.initials: F
authors.lastname: Daubeuf
authors.affiliation: Biotechnologie et signalisation cellulaire, UMR 7242 CNRS/Université de Strasbourg , ESBS, Bld Sébastien Brant, 67412 Illkirch, France.
authors.forename: Muriel
authors.initials: M
authors.lastname: Hachet-Haas
authors.affiliation: Laboratoire d'Innovation Thérapeutique, UMR 7200 CNRS/Université de Strasbourg , Faculté de Pharmacie, 74 route du Rhin, 67401 Illkirch, France.
authors.forename: François
authors.initials: F
authors.lastname: Rohmer
authors.affiliation: Biotechnologie et signalisation cellulaire, UMR 7242 CNRS/Université de Strasbourg , ESBS, Bld Sébastien Brant, 67412 Illkirch, France.
authors.forename: Patrick
authors.initials: P
authors.lastname: Gizzi
authors.affiliation: Laboratoire d'Innovation Thérapeutique, UMR 7200 CNRS/Université de Strasbourg , Faculté de Pharmacie, 74 route du Rhin, 67401 Illkirch, France.
authors.forename: Jacques
authors.initials: J
authors.lastname: Haiech
authors.affiliation: Biotechnologie et signalisation cellulaire, UMR 7242 CNRS/Université de Strasbourg , ESBS, Bld Sébastien Brant, 67412 Illkirch, France.
authors.forename: Jean-Luc
authors.initials: JL
authors.lastname: Galzi
authors.affiliation: Laboratoire d'Innovation Thérapeutique, UMR 7200 CNRS/Université de Strasbourg , Faculté de Pharmacie, 74 route du Rhin, 67401 Illkirch, France.
authors.forename: Marcel
authors.initials: M
authors.lastname: Hibert
authors.affiliation: Laboratoire d'Innovation Thérapeutique, UMR 7200 CNRS/Université de Strasbourg , Faculté de Pharmacie, 74 route du Rhin, 67401 Illkirch, France.
authors.forename: Dominique
authors.initials: D
authors.lastname: Bonnet
authors.affiliation: Laboratoire d'Innovation Thérapeutique, UMR 7200 CNRS/Université de Strasbourg , Faculté de Pharmacie, 74 route du Rhin, 67401 Illkirch, France.
authors.forename: Nelly
authors.initials: N
authors.lastname: Frossard
keywords: CXCL12 chemokine; CXCR4 receptor; GPCR; asthma; prodrug; solubility