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Structure paper

TitleStructure and RAF family kinase isoform selectivity of type II RAF inhibitors tovorafenib and naporafenib.
Journal, issue, pagesJ. Biol. Chem., Vol. 299, Page 104634-104634, Year 2023
Publish dateNov 20, 2022 (structure data deposition date)
AuthorsTkacik, E. / Li, K. / Gonzalez-Del Pino, G. / Ha, B.H. / Vinals, J. / Park, E. / Beyett, T.S. / Eck, M.J.
External linksJ. Biol. Chem. / PubMed:36963492
MethodsX-ray diffraction
Resolution2.74 - 3.54 Å
Structure data

PDB-8f7o:
BRAF kinase in complex with TAK580 (tovorafenib)
Method: X-RAY DIFFRACTION / Resolution: 3.54 Å

PDB-8f7p:
BRAF kinase in complex with LXH254 (naporafenib)
Method: X-RAY DIFFRACTION / Resolution: 2.74 Å

Chemicals

ChemComp-QOP:
6-amino-5-chloro-N-[(1R)-1-(5-{[5-chloro-4-(trifluoromethyl)pyridin-2-yl]carbamoyl}-1,3-thiazol-2-yl)ethyl]pyrimidine-4-carboxamide / medication, inhibitor*YM

ChemComp-K81:
N-{3-[2-(2-hydroxyethoxy)-6-(morpholin-4-yl)pyridin-4-yl]-4-methylphenyl}-2-(trifluoromethyl)pyridine-4-carboxamide

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/INHIBITOR / BRAF / TAK580 / tovorafenib / TRANSFERASE / TRANSFERASE-INHIBITOR complex / LXH254 / naporafenib

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