› 3q4t

X-ray diffraction
1.96Å resolution

Crystal structure of Activin receptor type-IIA (ACVR2A) kinase domain in complex with dorsomorphin

Released:
DOI: 10.2210/pdb3q4t/pdb
PDB entry 3q4t coloured by chain, front view.
PDB entry 3q4t coloured by chain, side view.
PDB entry 3q4t coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Small molecules dorsomorphin and LDN-193189 inhibit myostatin/GDF8 signaling and promote functional myoblast differentiation.
Horbelt D, Boergermann JH, Chaikuad A, Alfano I, Williams E, Lukonin I, Timmel T, Bullock AN, Knaus P
J Biol Chem 290 3390-404 (2015)
PMID: 25368322

Function and Biology Details

Reaction catalysed: 
ATP + [receptor-protein] = ADP + [receptor-protein] phosphate
Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-150920 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Activin receptor type-2A Chains: A, B
Molecule details ›
Chains: A, B
Length: 322 amino acids
Theoretical weight: 36.55 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P27037 (Residues: 191-488; Coverage: 60%)
Gene names: ACVR2, ACVR2A
Sequence domains: Protein kinase domain
Structure domains:

Ligands and Environments

4 bound ligands:
Ligand TAK 2 x TAK
Ligand SO4 4 x SO4
Ligand EDO 21 x EDO
Ligand PG4 1 x PG4
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: DIAMOND BEAMLINE I03
Spacegroup: P6522
Unit cell:
a: 110.1Å b: 110.1Å c: 206.911Å
α: 90° β: 90° γ: 120°
R-values:
R R work R free
0.171 0.168 0.223
Expression system: Spodoptera frugiperda

Quick links

Citations

8 review citations

The role of exercise-induced myokines in regulating metabolism.
Huh JY. (2018)
7 more

7 mentions without citation

Small molecules dorsomorphin and LDN-193189 inhibit myostatin/GDF8 signaling and promote functional myoblast differentiation.
Horbelt et al. (2015)
6 more