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TitleLive-cell target engagement of allosteric MEKi on MEK-RAF/KSR-14-3-3 complexes.
Journal, issue, pagesNat. Chem. Biol., Vol. 20, Page 373-381, Year 2024
Publish dateApr 6, 2022 (structure data deposition date)
AuthorsMarsiglia, W.M. / Chow, A. / Khan, Z.M. / He, L. / Dar, A.C.
External linksNat. Chem. Biol. / PubMed:37919548
MethodsX-ray diffraction
Resolution3.231 Å
Structure data

PDB-7umb:
NanoBRET tracer Tram-bo bound to a KSR2-MEK1 complex
Method: X-RAY DIFFRACTION / Resolution: 3.231 Å

Chemicals

ChemComp-ANP:
PHOSPHOAMINOPHOSPHONIC ACID-ADENYLATE ESTER / AMP-PNP, energy-carrying molecule analogue*YM

ChemComp-U9F:
{3-[(1M,2M)-2-{[(1S,2P)-1H,1'H-[2,2'-bipyrrol]-5-yl-kappaN~1~]methylidene}-2H-pyrrol-5-yl-kappaN]-N-(2-{2-[3-({(3M)-3-[(4aM)-3-cyclopropyl-5-(2-fluoro-4-iodoanilino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}amino)-3-oxopropoxy]ethoxy}ethyl)propanamidato}(difluorido)boron

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / Tracer / kinase / complex / MEK1 / KSR2

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