A5068375416- Chemokine receptors and signaling
- Coagulation, Bradykinin, Polyphosphates, and Angioedema
- Receptor Mechanisms and Signaling
- T-cell and B-cell Immunology
- Food Allergy and Anaphylaxis Research
- Neuropeptides and Animal Physiology
- Heparin-Induced Thrombocytopenia and Thrombosis
- Peptidase Inhibition and Analysis
- Blood Coagulation and Thrombosis Mechanisms
- Adenosine and Purinergic Signaling
- Platelet Disorders and Treatments
- Urticaria and Related Conditions
- Advanced Proteomics Techniques and Applications
- Monoclonal and Polyclonal Antibodies Research
- Mast cells and histamine
- Immunotherapy and Immune Responses
- Drug-Induced Adverse Reactions
Université de Montréal
2009-2017
Centre Hospitalier Universitaire Sainte-Justine
2017
Chemokines orchestrate cell migration for development, immune surveillance, and disease by binding to surface heterotrimeric guanine nucleotide-binding protein (G protein)-coupled receptors (GPCRs). The array of interactions between the nearly 50 chemokines their 20 GPCR targets generates an extensive signaling network which promiscuity biased agonism add further complexity. receptor CXCR4 recognizes both monomeric dimeric forms chemokine CXCL12, is a distinct example ligand bias in family....
The CXC chemokine receptor 7 (CXCR7)/ACKR3 is a that recognizes stromal cell-derived factor 1 (SDF-1)/CXCL12 and interferon-inducible T-cell α chemoattractant (I-TAC)/CXCL11. Here, we report the development of novel CXCR7-selective ligands with cyclic pentapeptide scaffold through an SAR study 4 (CXCR4) selective antagonist FC131 [cyclo(-d-Tyr-l-Arg-l-Arg-l-Nal-Gly-), Nal = 3-(2-naphthyl)alanine]. Substitution Gly l-Pro switched preference peptides from CXCR4 to CXCR7. led identification...
The chemokine receptor CXCR7 is an atypical CXCL12 that, as opposed to the classical CXCR4, signals preferentially via β-arrestin pathway and does not mediate chemotaxis. We previously reported that cyclic peptide TC14012, a potent CXCR4 antagonist, also engaged CXCR7, albeit with lower potency. Surprisingly, compound activated CXCR7-arrestin pathway. reason underlying opposite effects of TC14012 on mode binding remained unclear. known from cocrystallization its analogue CVX15 CXCR4. here...