ZK756326

ZK756326 is a full agonist of CCR8Chemokine receptor 8 with an IC50 of 1.8 M, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1.ZK 756326 stimulated extracellular acidification in cells expressing human CCR8. The ability of ZK 756326 to induce a response was receptor-specific and mediated through Gi, because it could be blocked by treatment with pertussis toxin. Like CCL1, ZK 756326 inhibited human immunodeficiency virus (HIV) fusion of cells expressing CD4 and CCR8. But unlike mCCL1, ZK 756326 bound to and activated a form of mCCR8 that was mutated to eliminate O-linked sulfation at tyrosines 14 and 15. Therefore, ZK 756326 is most probably not binding in the same manner as CCL1 but can activate the switch mechanism involved in transducing signaling events