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TitleMolecular mechanism of setron-mediated inhibition of full-length 5-HT receptor.
Journal, issue, pagesNat Commun, Vol. 10, Issue 1, Page 3225, Year 2019
Publish dateJul 19, 2019
AuthorsSandip Basak / Yvonne Gicheru / Abhijeet Kapoor / Megan L Mayer / Marta Filizola / Sudha Chakrapani /
PubMed AbstractSerotonin receptor (5-HTR) is the most common therapeutic target to manage the nausea and vomiting during cancer therapies and in the treatment of irritable bowel syndrome. Setrons, a class of ...Serotonin receptor (5-HTR) is the most common therapeutic target to manage the nausea and vomiting during cancer therapies and in the treatment of irritable bowel syndrome. Setrons, a class of competitive antagonists, cause functional inhibition of 5-HTR in the gastrointestinal tract and brainstem, acting as effective anti-emetic agents. Despite their prevalent use, the molecular mechanisms underlying setron binding and inhibition of 5-HTR are not fully understood. Here, we present the structure of granisetron-bound full-length 5-HTR solved by single-particle cryo-electron microscopy to 2.92 Å resolution. The reconstruction reveals the orientation of granisetron in the orthosteric site with unambiguous density for interacting sidechains. Molecular dynamics simulations and electrophysiology confirm the granisetron binding orientation and the residues central for ligand recognition. Comparison of granisetron-bound 5-HTR with the apo and serotonin-bound structures, reveals key insights into the mechanism underlying 5-HTR inhibition.
External linksNat Commun / PubMed:31324772 / PubMed Central
MethodsEM (single particle)
Resolution2.92 Å
Structure data

0469

6np0

EMDB-0469, PDB-6np0:
Cryo-EM structure of 5HT3A receptor in presence of granisetron
Method: EM (single particle) / Resolution: 2.92 Å

Chemicals

ChemComp-NAG:
2-acetamido-2-deoxy-beta-D-glucopyranose

ChemComp-CWB:
1-methyl-N-[(1R,5S)-9-methyl-9-azabicyclo[3.3.1]nonan-3-yl]indazole-3-carboxamide / chemotherapy, antagonist*YM

ChemComp-CL:
Unknown entry

Source
  • mus musculus (house mouse)
KeywordsMEMBRANE PROTEIN

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