WRW4 is a selective and potent antagonist of the Formylpeptide receptors (FPR2 and FPR3), which was identified by screening hexapeptide libraries that inhibit the binding of the FPR2 agonist WKYMVm to its specific receptor, in RBL-2H3 cells. In human umbilical vein endothelial cells, WRW4 (10 mM), inhibited CCL2 production, which was stimulated by serum amyloid A.
产品描述
A Potent Antagonist of FPR2 and FPR3 G-Protein Coupled Receptors
产品形式
Chemotactic factors from both Gram-positive and Gram-negative bacteria are short peptides with N-formyl methionine at the N-terminus (extensively reviewed in reference 1). These peptides are released from bacteria during infection and activate formyl peptide receptor (FPR), a member of G-protein coupled receptors (GPCRs). In human, the FPR family consists mainly of three receptors, FPR1, FPR2/ALX (formerly FPRL1), and FPR3 (formerly FPRL2) which all couple to the Gi subtype of G-proteins and ultimately lead to the activation of phospholipase C and intracellular Ca2+ increase.