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Structure paper

TitleStructure of the active G-coupled human lysophosphatidic acid receptor 1 complexed with a potent agonist.
Journal, issue, pagesNat Commun, Vol. 13, Issue 1, Page 5417, Year 2022
Publish dateSep 15, 2022
AuthorsHiroaki Akasaka / Tatsuki Tanaka / Fumiya K Sano / Yuma Matsuzaki / Wataru Shihoya / Osamu Nureki /
PubMed AbstractLysophosphatidic acid receptor 1 (LPA) is one of the six G protein-coupled receptors activated by the bioactive lipid, lysophosphatidic acid (LPA). LPA is a drug target for various diseases, ...Lysophosphatidic acid receptor 1 (LPA) is one of the six G protein-coupled receptors activated by the bioactive lipid, lysophosphatidic acid (LPA). LPA is a drug target for various diseases, including cancer, inflammation, and neuropathic pain. Notably, LPA agonists have potential therapeutic value for obesity and urinary incontinence. Here, we report a cryo-electron microscopy structure of the active human LPA-G complex bound to ONO-0740556, an LPA analog with more potent activity against LPA. Our structure elucidated the details of the agonist binding mode and receptor activation mechanism mediated by rearrangements of transmembrane segment 7 and the central hydrophobic core. A structural comparison of LPA and other phylogenetically-related lipid-sensing GPCRs identified the structural determinants for lipid preference of LPA. Moreover, we characterized the structural polymorphisms at the receptor-G-protein interface, which potentially reflect the G-protein dissociation process. Our study provides insights into the detailed mechanism of LPA binding to agonists and paves the way toward the design of drug-like agonists targeting LPA.
External linksNat Commun / PubMed:36109516 / PubMed Central
MethodsEM (single particle)
Resolution3.5 - 5.6 Å
Structure data

34097

7yu3

EMDB-34097, PDB-7yu3:
Human Lysophosphatidic Acid Receptor 1-Gi complex bound to ONO-0740556
Method: EM (single particle) / Resolution: 3.5 Å

34098

7yu4

EMDB-34098, PDB-7yu4:
Human Lysophosphatidic Acid Receptor 1-Gi complex bound to ONO-0740556, focused on receptor
Method: EM (single particle) / Resolution: 3.7 Å

34099

7yu5

EMDB-34099, PDB-7yu5:
Human Lysophosphatidic Acid Receptor 1-Gi complex bound to ONO-0740556, state1
Method: EM (single particle) / Resolution: 3.7 Å

34100

7yu6

EMDB-34100, PDB-7yu6:
Human Lysophosphatidic Acid Receptor 1-Gi complex bound to ONO-0740556, state2
Method: EM (single particle) / Resolution: 3.9 Å

34101

7yu7

EMDB-34101, PDB-7yu7:
Human Lysophosphatidic Acid Receptor 1-Gi complex bound to ONO-0740556, state3
Method: EM (single particle) / Resolution: 4.5 Å

34102

7yu8

EMDB-34102, PDB-7yu8:
Human Lysophosphatidic Acid Receptor 1-Gi complex bound to ONO-0740556, state4
Method: EM (single particle) / Resolution: 5.6 Å

Chemicals

ChemComp-K6L:
[(2~{R})-2-[5-(2-hexylphenyl)pentanoylamino]-3-oxidanyl-propyl] dihydrogen phosphate

Source
  • rattus norvegicus (Norway rat)
  • homo sapiens (human)
  • bos taurus (cattle)
  • mus musculus (house mouse)
KeywordsMEMBRANE PROTEIN / GPCR

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