› 5dsg

X-ray diffraction
2.6Å resolution

Structure of the M4 muscarinic acetylcholine receptor (M4-mT4L) bound to tiotropium

Released:
DOI: 10.2210/pdb5dsg/pdb
PDB entry 5dsg coloured by chain, front view.
PDB entry 5dsg coloured by chain, side view.
PDB entry 5dsg coloured by chain, top view.
Source organisms:
Primary publication:
Crystal structures of the M1 and M4 muscarinic acetylcholine receptors.
Thal DM, Sun B, Feng D, Nawaratne V, Leach K, Felder CC, Bures MG, Evans DA, Weis WI, Bachhawat P, Kobilka TS, Sexton PM, Kobilka BK, Christopoulos A
Nature 531 335-40 (2016)
PMID: 26958838

Function and Biology Details

Reaction catalysed: 
Hydrolysis of (1->4)-beta-linkages between N-acetylmuramic acid and N-acetyl-D-glucosamine residues in a peptidoglycan and between N-acetyl-D-glucosamine residues in chitodextrins
Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assemblies composition:
monomeric
homo dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-132956 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Endolysin; Muscarinic acetylcholine receptor M4 Chains: A, B
Molecule details ›
Chains: A, B
Length: 422 amino acids
Theoretical weight: 47.8 KDa
Source organisms: Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P08173 (Residues: 22-238, 390-478; Coverage: 64%)
  • Canonical: P00720 (Residues: 61-161; Coverage: 62%)
Gene names: CHRM4, E
Sequence domains:

Ligands and Environments

6 bound ligands:
Ligand 0HK 2 x 0HK
Ligand OLA 5 x OLA
Ligand EDT 1 x EDT
Ligand P6G 2 x P6G
Ligand OLC 5 x OLC
Ligand PG6 1 x PG6
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 23-ID-D
Spacegroup: P21
Unit cell:
a: 48.49Å b: 172.04Å c: 60.66Å
α: 90° β: 94.37° γ: 90°
R-values:
R R work R free
0.228 0.226 0.24
Expression system: Spodoptera frugiperda

Quick links

Citations

41 review citations

Allosteric Modulation of GPCRs: New Insights and Potential Utility for Treatment of Schizophrenia and Other CNS Disorders.
Foster et al. (2017)
40 more

43 mentions without citation

G protein-coupled receptors: structure- and function-based drug discovery.
Yang et al. (2021)
42 more