{"id":214179,"date":"2025-05-17T05:19:43","date_gmt":"2025-05-17T10:19:43","guid":{"rendered":"https:\/\/lifeboat.com\/blog\/2025\/05\/scientists-map-activation-of-prostaglandin-e%e2%82%82-receptor-ep1-at-atomic-level"},"modified":"2025-05-17T05:19:43","modified_gmt":"2025-05-17T10:19:43","slug":"scientists-map-activation-of-prostaglandin-e%e2%82%82-receptor-ep1-at-atomic-level","status":"publish","type":"post","link":"https:\/\/lifeboat.com\/blog\/2025\/05\/scientists-map-activation-of-prostaglandin-e%e2%82%82-receptor-ep1-at-atomic-level","title":{"rendered":"Scientists map activation of prostaglandin E\u2082 receptor EP1 at atomic level"},"content":{"rendered":"<p><a class=\"aligncenter blog-photo\" href=\"https:\/\/lifeboat.com\/blog.images\/scientists-map-activation-of-prostaglandin-ee28282-receptor-ep1-at-atomic-level2.jpg\"><\/a><\/p>\n<p>Prostaglandin E<sub>2<\/sub> (PGE<sub>2<\/sub>), a bioactive lipid derived from arachidonic acid, mediates a broad range of physiological processes through four G protein-coupled receptor (GPCR) subtypes: EP1\u2013EP4. While the high-resolution structures of EP2, EP3 and EP4 have been resolved, EP1 remained structurally uncharacterized due to its intrinsic instability, hindering detailed understanding of its Gq-mediated signaling.<\/p>\n<p>In a study <a href=\"https:\/\/doi.org\/10.1073\/pnas.2423840122\" target=\"_blank\">published<\/a> in <i>Proceedings of the National Academy of Sciences<\/i>, a research team led by Eric H. Xu (Xu Huaqiang) and Xu Youwei from the Shanghai Institute of Materia Medica of the Chinese Academy of Sciences reported the cryo\u2013<a href=\"https:\/\/phys.org\/tags\/electron+microscopy\/\" rel=\"tag\" class=\"\">electron microscopy<\/a> (cryo-EM) structure of the human EP1 receptor in complexes with PGE<sub>2<\/sub> and the heterotrimeric Gq protein, completed structural atlas of EP receptor family, and revealed EP1-specific mechanisms of ligand recognition and signal transduction.<\/p>\n<p>To overcome the instability of EP1, the researchers employed a multi-pronged engineering strategy, including BRIL fusion, truncation of flexible loops, incorporation of a mini-Gq chimera, and NanoBiT-assisted complex stabilization. They resolved the structure of the EP1\u2013PGE<sub>2<\/sub>\u2013Gq complex at 2.55 \u00c5 resolution using single-particle cryo-EM, enabling detailed analysis of both ligand binding and G protein coupling interfaces.<\/p>\n","protected":false},"excerpt":{"rendered":"<p>Prostaglandin E2 (PGE2), a bioactive lipid derived from arachidonic acid, mediates a broad range of physiological processes through four G protein-coupled receptor (GPCR) subtypes: EP1\u2013EP4. While the high-resolution structures of EP2, EP3 and EP4 have been resolved, EP1 remained structurally uncharacterized due to its intrinsic instability, hindering detailed understanding of its Gq-mediated signaling. In a [\u2026]<\/p>\n","protected":false},"author":427,"featured_media":0,"comment_status":"open","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[38,48],"tags":[],"class_list":["post-214179","post","type-post","status-publish","format-standard","hentry","category-engineering","category-particle-physics"],"_links":{"self":[{"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/posts\/214179","targetHints":{"allow":["GET"]}}],"collection":[{"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/users\/427"}],"replies":[{"embeddable":true,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/comments?post=214179"}],"version-history":[{"count":0,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/posts\/214179\/revisions"}],"wp:attachment":[{"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/media?parent=214179"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/categories?post=214179"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/lifeboat.com\/blog\/wp-json\/wp\/v2\/tags?post=214179"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}