› 4wua

X-ray diffraction
2Å resolution

Crystal structure of human SRPK1 complexed to an inhibitor SRPIN340

Released:
DOI: 10.2210/pdb4wua/pdb
PDB entry 4wua coloured by chain, front view.
PDB entry 4wua coloured by chain, side view.
PDB entry 4wua coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Identification of a Dual Inhibitor of SRPK1 and CK2 That Attenuates Pathological Angiogenesis of Macular Degeneration in Mice.
Morooka S, Hoshina M, Kii I, Okabe T, Kojima H, Inoue N, Okuno Y, Denawa M, Yoshida S, Fukuhara J, Ninomiya K, Ikura T, Furuya T, Nagano T, Noda K, Ishida S, Hosoya T, Ito N, Yoshimura N, Hagiwara M
Mol Pharmacol 88 316-25 (2015)
PMID: 25993998

Function and Biology Details

Reaction catalysed: 
ATP + a protein = ADP + a phosphoprotein
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-188751 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
SRSF protein kinase 1 Chain: A
Molecule details ›
Chain: A
Length: 401 amino acids
Theoretical weight: 45.64 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: Q96SB4 (Residues: 42-255, 474-655; Coverage: 61%)
Gene name: SRPK1
Sequence domains: Protein kinase domain
Structure domains:

Ligands and Environments

2 bound ligands:
Ligand 3UL 1 x 3UL
Ligand CIT 1 x CIT
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SPRING-8 BEAMLINE BL38B1
Spacegroup: P6522
Unit cell:
a: 75.132Å b: 75.132Å c: 310.623Å
α: 90° β: 90° γ: 120°
R-values:
R R work R free
0.199 0.197 0.236
Expression system: Escherichia coli

Quick links

Citations

8 review citations

Protein kinase CK2: a potential therapeutic target for diverse human diseases.
Borgo et al. (2021)
7 more

3 mentions without citation

Identification of a novel and potent small molecule inhibitor of SRPK1: mechanism of dual inhibition of SRPK1 for the inhibition of cancer progression.
Chandra et al. (2020)
2 more