› 5e8u

X-ray diffraction
2.03Å resolution

TGF-BETA RECEPTOR TYPE 1 KINASE DOMAIN (T204D,I211V,Y249F,S280T, Y282F,S287N,A350C,L352F)

Released:
DOI: 10.2210/pdb5e8u/pdb
PDB entry 5e8u coloured by chain, front view.
PDB entry 5e8u coloured by chain, side view.
PDB entry 5e8u coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Crystal structures of apo and inhibitor-bound TGFβR2 kinase domain: insights into TGFβR isoform selectivity.
Tebben AJ, Ruzanov M, Gao M, Xie D, Kiefer SE, Yan C, Newitt JA, Zhang L, Kim K, Lu H, Kopcho LM, Sheriff S
Acta Crystallogr D Struct Biol 72 658-74 (2016)
PMID: 27139629

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-153250 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
TGF-beta receptor type-1 Chain: A
Molecule details ›
Chain: A
Length: 307 amino acids
Theoretical weight: 35.23 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P36897 (Residues: 200-503; Coverage: 65%)
Gene names: ALK5, SKR4, TGFBR1
Sequence domains: Protein kinase domain
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand GOL 3 x GOL
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: CLSI BEAMLINE 08ID-1
Spacegroup: P212121
Unit cell:
a: 41.6Å b: 77.1Å c: 89.6Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.182 0.179 0.223
Expression system: Spodoptera frugiperda

Quick links

Citations

2 review citations

Structural basis for the potent and selective binding of LDN-212854 to the BMP receptor kinase ALK2.
Williams et al. (2018)
1 more

1 mention without citation

"Let my liver rather heat with wine" - a review of hepatic fibrosis pathophysiology and emerging therapeutics.
Moscoso et al. (2019)