[2] Park Jong G,Tischfield Max A,Nugent Alicia A et al. Loss of MAFB Function in Humans and Mice Causes Duane Syndrome, Aberrant Extraocular Muscle Innervation, and Inner-Ear Defects.[J] .Am J Hum Genet, 2016, 98: 1220-1227. [3] Whitman Mary C...
The aim of our study was to investigate the formation of ACKR3/CXCR4 heterodimers in platelets and the subsequent consequences for platelet function. Methods and Results Using a proximity ligation assay (PLA, Duolink) to screen for CXCR4/ACKR3 heterodimerization inducing compounds, we found that ...
ACKR7 is a seven-transmembrane domain receptor phylogenetically related to the rhodopsin-like family of G protein-coupled receptors (GPCRs) which binds the chemokines CXCL12/SDF-1 (Kd~ 0.4 nM) and CXCL11/I-TAC (Kd~ 4 nM) and the peptide hormone adrenomedullin (Kd~ 0.2 nM), but appears ...
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prevents ACKR3’s negative regulatory function on opioid peptides in an ex vivo rat brain model and potentiates their activity towards classical opioid receptors. These results, together with a previous report showing that a small-molecule ACKR3 agonist CCX771 exhibits anxiolytic-like behavior in mic...
Recent evidence suggests that chemokine CXCL12, the cognate agonist of chemokine receptors CXCR4 and ACKR3, reduces thrombin-mediated impairment of endothelial barrier function. A detailed characterization of the effects of CXCL12 on thrombin-mediated human lung endothelial hyperpermeability is lacking and...
(VLA-4) and lymphocyte function-associated antigen-1 (LFA-1)-driven adhesion of human lymphocytes onto inflamed endothelium [26]. Moreover, ACKR3 knockdown resulted in suppression of adhesion along with VCAM-1 expression in TNF-α-stimulated human brain microvascular endothelial cells [35]. We ...
To decipher the function and impact of ACKR3 on the opioid system, we tested the ability of opioid peptides to trigger downstream signaling through ACKR3 in U87 cells that have no endogenous expression of CXCR431. We first applied a whole-cell optical biosensing approach based on dynamic mass...
While only synonymous variants were found in COPS8, one of the missense variants in ACKR3:c.892C>T, observed in 4/479 individuals screened (0.8%), was predicted likely to damage ACKR3 function. Identification of causal genes for RCC has potential clinical utility, where risk assessment and ...
ACKR3 is not modulated by prescription opioids, but we show that an ACKR3-selective subnanomolar competitor peptide, LIH383, can restrain ACKR3's negative regulatory function on opioid peptides in rat brain and potentiate their activity towards classical receptors, which may open alternative ...