› 2rgn

X-ray diffraction
3.5Å resolution

Crystal Structure of p63RhoGEF complex with Galpha-q and RhoA

Released:
DOI: 10.2210/pdb2rgn/pdb
PDB entry 2rgn coloured by chain, front view.
PDB entry 2rgn coloured by chain, side view.
PDB entry 2rgn coloured by chain, top view.
Source organisms:
Primary publication:
Structure of Galphaq-p63RhoGEF-RhoA complex reveals a pathway for the activation of RhoA by GPCRs.
Lutz S, Shankaranarayanan A, Coco C, Ridilla M, Nance MR, Vettel C, Baltus D, Evelyn CR, Neubig RR, Wieland T, Tesmer JJ
Science 318 1923-7 (2007)
PMID: 18096806

Function and Biology Details

Reaction catalysed: 
GTP + H(2)O = GDP + phosphate
Biochemical function:
Biological process:
Cellular component:
Sequence domains:
Structure domains:

Structure analysis Details

Assembly composition:
hetero trimer (preferred)
PDBe Complex ID:
PDB-CPX-145466 (preferred)
Entry contents:
3 distinct polypeptide molecules
Macromolecules (3 distinct):
Guanine nucleotide-binding protein G(i) subunit alpha-1; Guanine nucleotide-binding protein G(q) subunit alpha Chains: A, D
Molecule details ›
Chains: A, D
Length: 353 amino acids
Theoretical weight: 41.3 KDa
Source organisms: Expression system: Trichoplusia ni
UniProt:
  • Canonical: P10824 (Residues: 1-28; Coverage: 8%)
  • Canonical: P21279 (Residues: 37-359; Coverage: 90%)
Gene names: Gnai-1, Gnai1, Gnaq
Sequence domains: G-protein alpha subunit
Structure domains:
Rho guanine nucleotide exchange factor 25 Chains: B, E
Molecule details ›
Chains: B, E
Length: 354 amino acids
Theoretical weight: 40.61 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: Q86VW2 (Residues: 149-502; Coverage: 61%)
Gene names: ARHGEF25, GEFT
Sequence domains: RhoGEF domain
Structure domains:
Transforming protein RhoA Chains: C, F
Molecule details ›
Chains: C, F
Length: 196 amino acids
Theoretical weight: 22.13 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: P61586 (Residues: 1-193; Coverage: 100%)
Gene names: ARH12, ARHA, RHO12, RHOA
Sequence domains: Ras family
Structure domains: P-loop containing nucleotide triphosphate hydrolases

Ligands and Environments

3 bound ligands:
Ligand ALF 2 x ALF
Ligand MG 2 x MG
Ligand GDP 2 x GDP
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 21-ID-D
Spacegroup: P1
Unit cell:
a: 67.187Å b: 68.056Å c: 138.018Å
α: 80.87° β: 85.16° γ: 87.09°
R-values:
R R work R free
0.243 0.243 0.299
Expression systems:
  • Trichoplusia ni
  • Escherichia coli

Quick links

Citations

32 review citations

Regulation of small GTPases by GEFs, GAPs, and GDIs.
Cherfils et al. (2013)
31 more

24 mentions without citation

Regulators of G-protein signaling and their Gα substrates: promises and challenges in their use as drug discovery targets.
Kimple et al. (2011)
23 more