Data on human neutrophil activation induced by pepducins with amino acid sequences derived from β2AR and CXCR4
نویسندگان
چکیده
The data described here is related to the research article titled (Gabl et al., 2016) [1]. Pepducins with peptide sequence derived from one of the intracellular domains of a given G-protein coupled receptor (GPCR) can either activate or inhibit cell functions. Here we include data on human neutrophil function induced by pepducins derived from β2AR (ICL3-8) and CXCR4 (ATI-2341), respectively. ICL3-8 exerts neither direct activating effect on the NADPH-oxidase as measured by superoxide release nor inhibitory effect on FPR signaling. ATI-2341 dose-dependently triggers neutrophil activation and these cells were subsequently desensitized in their response to FPR2 specific agonists F2Pal10 and WKYMVM. Moreover, the ATI-2341 response is inhibited by PBP10 and the peptidomimetic Pam-(Lys-betaNSpe)6-NH2 (both are FPR2 specific inhibitors), but not to the FPR1 specific inhibitor cyclosporine H.
منابع مشابه
Discovery of a CXCR4 agonist pepducin that mobilizes bone marrow hematopoietic cells.
The G protein-coupled receptor (GPCR), chemokine CXC-type receptor 4 (CXCR4), and its ligand, CXCL12, mediate the retention of polymorphonuclear neutrophils (PMNs) and hematopoietic stem and progenitor cells (HSPCs) in the bone marrow. Agents that disrupt CXCL12-mediated chemoattraction of CXCR4-expressing cells mobilize PMNs and HSPCs into the peripheral circulation and are therapeutically use...
متن کاملReversal of murine alcoholic steatohepatitis by pepducin-based functional blockade of interleukin-8 receptors
OBJECTIVE Alcoholic steatohepatitis is a life-threatening condition with short-term mortality up to 40%. It features hepatic neutrophil infiltration and blood neutrophilia, and may evolve from ethanol-induced breakdown of the enteric barrier and consequent bacteraemia. Signalling through CXCR1/2 G-protein-coupled-receptors (GPCRs), the interleukin (IL)-8 receptors, is critical for the recruitme...
متن کاملFormyl peptide derived lipopeptides disclose differences between the receptors in mouse and men and call the pepducin concept in question
A pepducin is a lipopeptide containing a peptide sequence that is identical to one of the intracellular domains of the G-protein coupled receptor (GPCR) assumed to be the target. Neutrophils express two closely related formyl peptide receptors belonging to the family of GPCRs; FPR1 and FPR2 in human and their respective orthologue Fpr1 and Fpr2 in mouse. By applying the pepducin concept, we hav...
متن کاملComparative Analysis of Expression of Chemokoine Receptors CXCR4, CXCR6, CCR1 and CX3CR in Human Adipose-Drived Mesenchymal Stem Cell with Valproic Acid
Introduction: Chemokine receptors are found on the surface of stem cells. There have been 19 distinct chemokine receptors described in mammals. Chemokines are major players in migration and homing. Therefore, changes in their levels or function can help us to increase the migratory potential of these cells. Valproic acid differs in structure from other drugs in common use. The way in which Va...
متن کاملTargeting CXCR4 with cell-penetrating pepducins in lymphoma and lymphocytic leukemia.
The chemokine receptor CXCR4, which normally regulates stromal stem cell interactions in the bone marrow, is highly expressed on a variety of malignant hematologic cells, including lymphoma and lymphocytic leukemias. A new treatment concept has arisen wherein CXCR4 may be an effective therapeutic target as an adjunct to treatment of hematologic neoplasms with chemo- and immunotherapy. In the pr...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
عنوان ژورنال:
دوره 8 شماره
صفحات -
تاریخ انتشار 2016