CXCR2 chemokine receptor antagonism enhances DOP opioid receptor function via allosteric regulation of the CXCR2–DOP receptor heterodimer

CXCR2 chemokine receptor antagonism enhances DOP opioid receptor function via allosteric regulation of the CXCR2–DOP receptor heterodimer

Opioid agonists have a broad range of effects on cells of the immune system, including modulation of the inflammatory response, and opioid and chemokine receptors are co-expressed by many white cells. Hetero-oligomerization of the human DOP opioid and chemokine CXCR2 receptors could be detected following their co-expression by each of co-immunoprecipitation, three different resonance energy tra...

Nonpeptidergic allosteric antagonists differentially bind to the CXCR2 chemokine receptor.

The chemokine receptor CXCR2 is involved in different inflammatory diseases, like chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis; therefore, it is considered an attractive drug target. Different classes of small CXCR2 antagonists have been developed. In this study, we selected seven CXCR2 antagonists from the diarylurea, imidazolylpyrimide, and th...

Chemokine Signaling via the CXCR2 Receptor Reinforces Senescence

Cells enter senescence, a state of stable proliferative arrest, in response to a variety of cellular stresses, including telomere erosion, DNA damage, and oncogenic signaling, which acts as a barrier against malignant transformation in vivo. To identify genes controlling senescence, we conducted an unbiased screen for small hairpin RNAs that extend the life span of primary human fibroblasts. He...

Regulation of -Opioid Receptor Trafficking via -Opioid Receptor Stimulation: Evidence from -Opioid Receptor Knock-Out Mice

Anne Morinville,1,2 Catherine M. Cahill,2 M. James Esdaile,2 Haneen Aibak,2 Brian Collier,1 Brigitte L. Kieffer,3 and Alain Beaudet2 1Department of Pharmacology and Therapeutics, McGill University, Montréal, Québec, Canada H3G 1Y6, 2Montréal Neurological Institute, McGill University, Montréal, Québec, Canada H3A 2B4, and 3Institute of Genetics and of Molecular and Cellular Biology, National Cen...

ELR-CXC Chemokine Receptor Antagonism