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-Structure paper
タイトル | Structural basis for ligand recognition and signaling of the lysophosphatidylserine receptors GPR34 and GPR174. |
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ジャーナル・号・ページ | PLoS Biol, Vol. 21, Issue 12, Page e3002387, Year 2023 |
掲載日 | 2023年12月4日 |
著者 | Guibing Liu / Xiu Li / Yujing Wang / Xuan Zhang / Weimin Gong / |
PubMed 要旨 | Lysophosphatidylserine (LysoPS) is a naturally occurring lipid mediator involved in various physiological and pathological processes especially those related to the immune system. GPR34, GPR174, and ...Lysophosphatidylserine (LysoPS) is a naturally occurring lipid mediator involved in various physiological and pathological processes especially those related to the immune system. GPR34, GPR174, and P2Y10 have been identified as the receptors for LysoPS, and its analogues have been developed as agonists or antagonists for these receptors. However, the lack of structural information hinders the drug development with novel characteristics, such as nonlipid ligands and allosteric modulators. Here, we determined the structures of human GPR34 and GPR174 in complex with LysoPS and G protein by cryo-EM. Combined with structural analysis and functional studies, we elucidated the lipid-binding modes of these receptors. By structural comparison, we identified the structural features of GPR34 and GPR174 in active state. Taken together, our findings provide insights into ligand recognition and signaling of LysoPS receptors and will facilitate the development of novel therapeutics for related inflammatory diseases and autoimmune diseases. |
リンク | PLoS Biol / PubMed:38048360 / PubMed Central |
手法 | EM (単粒子) |
解像度 | 2.91 - 3.06 Å |
構造データ | EMDB-35838, PDB-8izb: EMDB-37771, PDB-8wrb: |
化合物 | ChemComp-UBL: ChemComp-SER: ChemComp-CLR: |
由来 |
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キーワード | SIGNALING PROTEIN / Complex |