› 4k5y

X-ray diffraction
2.98Å resolution

Crystal structure of human corticotropin-releasing factor receptor 1 (CRF1R) in complex with the antagonist CP-376395

Released:
DOI: 10.2210/pdb4k5y/pdb
PDB entry 4k5y coloured by chain, front view.
PDB entry 4k5y coloured by chain, side view.
PDB entry 4k5y coloured by chain, top view.
Source organisms:
Primary publication:
Structure of class B GPCR corticotropin-releasing factor receptor 1.
Hollenstein K, Kean J, Bortolato A, Cheng RK, Doré AS, Jazayeri A, Cooke RM, Weir M, Marshall FH
Nature 499 438-43 (2013)
PMID: 23863939

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

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-132978 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Corticotropin-releasing factor receptor 1; Endolysin Chains: A, B, C
Molecule details ›
Chains: A, B, C
Length: 441 amino acids
Theoretical weight: 50.43 KDa
Source organisms: Expression system: Trichoplusia ni
UniProt:
  • Canonical: P34998 (Residues: 103-249, 253-402; Coverage: 64%)
  • Canonical: P00720 (Residues: 2-161; Coverage: 98%)
Gene names: CRFR, CRFR1, CRHR, CRHR1, E
Sequence domains:
Structure domains:

Ligands and Environments

6 bound ligands:
Ligand 1Q5 3 x 1Q5
Ligand OLA 2 x OLA
Ligand OLC 3 x OLC
Ligand SO4 4 x SO4
Ligand PGW 3 x PGW
Ligand 1PE 1 x 1PE
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: DIAMOND BEAMLINE I24
Unit cell:
a: 86.559Å b: 123.968Å c: 166.834Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.243 0.242 0.265
Expression system: Trichoplusia ni

Quick links

Citations

60 review citations

Biased signalling: from simple switches to allosteric microprocessors.
Smith et al. (2018)
59 more

80 mentions without citation

Towards an Understanding of Synapse Formation.
Südhof TC. (2018)
79 more