› 8dph

Electron Microscopy
3.2Å resolution

Cryo-EM structure of the 5HT2C receptor (VGV isoform) bound to lorcaserin

Released:
DOI: 10.2210/pdb8dph/pdb
PDB entry 8dph coloured by chain, front view.
PDB entry 8dph coloured by chain, side view.
PDB entry 8dph coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Molecular insights into the regulation of constitutive activity by RNA editing of 5HT2C serotonin receptors.
Gumpper RH, Fay JF, Roth BL
Cell Rep 40 111211 (2022)
PMID: 35977511
Related structures: EMD-27635

Function and Biology Details

Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
hetero pentamer (preferred)
PDBe Complex ID:
PDB-CPX-225562 (preferred)
Entry contents:
5 distinct polypeptide molecules
Macromolecules (5 distinct):
5-hydroxytryptamine receptor 2C Chain: A
Molecule details ›
Chain: A
Length: 458 amino acids
Theoretical weight: 51.82 KDa
Source organism: Homo sapiens
Expression system: Baculovirus expression vector pFastBac1-HM
UniProt:
  • Canonical: P28335 (Residues: 1-458; Coverage: 100%)
Gene names: HTR1C, HTR2C
Sequence domains: 7 transmembrane receptor (rhodopsin family)
G-alpha subunit q (Gi2-mini-Gq chimeric) Chain: B
Molecule details ›
Chain: B
Length: 246 amino acids
Theoretical weight: 28.08 KDa
Source organism: Homo sapiens
Expression system: Baculovirus expression vector pFastBac1-HM
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 Chain: C
Molecule details ›
Chain: C
Length: 358 amino acids
Theoretical weight: 39.42 KDa
Source organism: Homo sapiens
Expression system: Baculovirus expression vector pFastBac1-HM
UniProt:
  • Canonical: P62873 (Residues: 2-340; Coverage: 100%)
Gene name: GNB1
Sequence domains: WD domain, G-beta repeat
Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 Chain: D
Molecule details ›
Chain: D
Length: 71 amino acids
Theoretical weight: 7.86 KDa
Source organism: Homo sapiens
Expression system: Baculovirus expression vector pFastBac1-HM
UniProt:
  • Canonical: P59768 (Residues: 1-71; Coverage: 100%)
Gene name: GNG2
Sequence domains: GGL domain
Antibody fragment scFv16 Chain: E
Molecule details ›
Chain: E
Length: 267 amino acids
Theoretical weight: 28.67 KDa
Source organism: Homo sapiens
Expression system: Baculovirus expression vector pFastBac1-HM

Ligands and Environments

2 bound ligands:
Ligand T4U 1 x T4U
Ligand CLR 2 x CLR
No modified residues

Experiments and Validation Details

Entry percentile scores
Resolution: 3.2Å
Relevant EMDB volumes: EMD-27635
Expression system: Baculovirus expression vector pFastBac1-HM

Quick links

Citations

6 review citations

A Novel "Activation Switch" Motif Common to All Aminergic Receptors.
Lee et al. (2023)
5 more

1 mention without citation

Molecular insights into the regulation of constitutive activity by RNA editing of 5HT2C serotonin receptors.
Gumpper et al. (2022)