› 8f7p

X-ray diffraction
2.74Å resolution

BRAF kinase in complex with LXH254 (naporafenib)

Released:
DOI: 10.2210/pdb8f7p/pdb
PDB entry 8f7p coloured by chain, front view.
PDB entry 8f7p coloured by chain, side view.
PDB entry 8f7p coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Structure and RAF-family kinase isoform selectivity of Type II RAF inhibitors tovorafenib and naporafenib.
Tkacik E, Li K, Gonzalez-Del Pino G, Ha BH, Vinals J, Park E, Beyett TS, Eck MJ
OpenAccess logo J Biol Chem 104634 (2023)
PMID: 36963492

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:
homo dimer (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-147199 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Serine/threonine-protein kinase B-raf Chains: A, B
Molecule details ›
Chains: A, B
Length: 283 amino acids
Theoretical weight: 32.01 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21
UniProt:
  • Canonical: P15056 (Residues: 441-723; Coverage: 37%)
Gene names: BRAF, BRAF1, RAFB1
Sequence domains: Protein tyrosine and serine/threonine kinase

Ligands and Environments

1 bound ligand:
Ligand K81 2 x K81
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 24-ID-E
Spacegroup: P21
Unit cell:
a: 49.647Å b: 101.746Å c: 58.688Å
α: 90° β: 109.67° γ: 90°
R-values:
R R work R free
0.216 0.214 0.258
Expression system: Escherichia coli BL21

Quick links

Citations

2 review citations

BRAFV600E-mutant metastatic NSCLC: disease overview and treatment landscape.
Planchard et al. (2024)
1 more

1 mention without citation

Structure and RAF family kinase isoform selectivity of type II RAF inhibitors tovorafenib and naporafenib.
Tkacik et al. (2023)