Author/Authors :
Andrew G. Cole، نويسنده , , Ilana L. Stroke، نويسنده , , Marc-Raleigh Brescia، نويسنده , , Srilatha Simhadri، نويسنده , , Joan J. Zhang، نويسنده , , Zahid Hussain، نويسنده , , Michael Snider، نويسنده , , Christopher Haskell، نويسنده , , Sofia Ribeiro، نويسنده , , Kenneth C. Appell، نويسنده , , Ian Henderson، نويسنده , , Maria L. Webb، نويسنده ,
Abstract :
The identification and evaluation of aryl-[1,4]diazepane ureas as functional antagonists of the chemokine receptor CXCR3 are described. Specific examples exhibit IC50 values of 60 nM in a calcium mobilization functional assay, and dose-dependently inhibit CXCR3 functional response to CXCL11 (interferon-inducible T-cell α chemoattractant/I-TAC) as measured by T-cell chemotaxis, with a potency of approximately 100 nM.
Keywords :
CXCR3 , chemokine , GPCR , Antagonist , Diazepane , urea
