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

Overview

Journal ACS Med Chem Lett

Publisher American Chemical Society

Specialty Chemistry

Date 2014 Jun 6

PMID 24900366

Citations 11

Authors

Vincent Gasparik

Francois Daubeuf

Muriel Hachet-Haas

Francois Rohmer

Patrick Gizzi

Jacques Haiech

Jean-Luc Galzi

Marcel Hibert

Dominique Bonnet

Nelly Frossard

Affiliations

Soon will be listed here.

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.

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