| http://purl.uniprot.org/citations/35065236 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/35065236 | http://www.w3.org/2000/01/rdf-schema#comment | "Pseudo-allergic reactions frequently occur following clinical drug use and sometimes even cause mortal danger. Mas-related G-protein-coupled receptor member X2 (MRGPRX2) is a novel receptor that mediates pseudo-allergy and is an important target in the treatment of allergies. However, to date, there are no synthetic small-molecule inhibitors that prevent anaphylactoid reactions through this pathway. Our preliminary research suggested that B10-S and mubritinib effectively inhibited LAD2 cells. Therefore, two novel derivatives were synthesized by integrating the active substructures of B10-S and mubritinib, according to the molecular docking results. The antiallergic inhibitory effects of the two compounds were preliminarily evaluated in vitro using β-hexosaminidase release, histamine release, and intracellular Ca2+ mobilization assays, and their binding sites on MRGPRX2 were analyzed by molecular docking. Both substances inhibited β-hexosaminidase and histamine release in LAD2 cells and decreased intracellular Ca2+ by inhibiting MRGPRX2 in MRGPRX2-HEK293 cells treated with C48/80 in a dose-dependent manner. The docking results suggested that the molecules could competitively bind to the active site on MRGPRX2 and Glu141, which were combined by C48/80. Our study indicated that the two compounds have potential anti-allergic properties, which may provide evidence that will facilitate the development of synthetic molecules with anti-pseudo-allergic activity for clinical use in the future."xsd:string |
| http://purl.uniprot.org/citations/35065236 | http://purl.org/dc/terms/identifier | "doi:10.1016/j.bmcl.2022.128575"xsd:string |
| http://purl.uniprot.org/citations/35065236 | http://purl.uniprot.org/core/author | "Hou Y."xsd:string |
| http://purl.uniprot.org/citations/35065236 | http://purl.uniprot.org/core/author | "He H."xsd:string |
| http://purl.uniprot.org/citations/35065236 | http://purl.uniprot.org/core/author | "Lu J."xsd:string |
| http://purl.uniprot.org/citations/35065236 | http://purl.uniprot.org/core/author | "Lv Y."xsd:string |
| http://purl.uniprot.org/citations/35065236 | http://purl.uniprot.org/core/author | "Wang C."xsd:string |
| http://purl.uniprot.org/citations/35065236 | http://purl.uniprot.org/core/author | "Wang X."xsd:string |
| http://purl.uniprot.org/citations/35065236 | http://purl.uniprot.org/core/author | "Ge S."xsd:string |
| http://purl.uniprot.org/citations/35065236 | http://purl.uniprot.org/core/date | "2022"xsd:gYear |
| http://purl.uniprot.org/citations/35065236 | http://purl.uniprot.org/core/name | "Bioorg Med Chem Lett"xsd:string |
| http://purl.uniprot.org/citations/35065236 | http://purl.uniprot.org/core/pages | "128575"xsd:string |
| http://purl.uniprot.org/citations/35065236 | http://purl.uniprot.org/core/title | "Synthesis and evaluation of new potential anti-pseudo-allergic agents."xsd:string |
| http://purl.uniprot.org/citations/35065236 | http://purl.uniprot.org/core/volume | "59"xsd:string |
| http://purl.uniprot.org/citations/35065236 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/35065236 |
| http://purl.uniprot.org/citations/35065236 | http://xmlns.com/foaf/0.1/primaryTopicOf | https://pubmed.ncbi.nlm.nih.gov/35065236 |
| http://purl.uniprot.org/uniprot/#_Q96LB1-mappedCitation-35065236 | http://www.w3.org/1999/02/22-rdf-syntax-ns#object | http://purl.uniprot.org/citations/35065236 |
| http://purl.uniprot.org/uniprot/Q96LB1 | http://purl.uniprot.org/core/mappedCitation | http://purl.uniprot.org/citations/35065236 |