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TitleSmall-molecule inhibition of METTL3 as a strategy against myeloid leukaemia.
Journal, issue, pagesNature, Vol. 593, Page 597-601, Year 2021
Publish dateMar 30, 2021 (structure data deposition date)
AuthorsYankova, E. / Blackaby, W. / Albertella, M. / Rak, J. / De Braekeleer, E. / Tsagkogeorga, G. / Pilka, E.S. / Aspris, D. / Leggate, D. / Hendrick, A.G. ...Yankova, E. / Blackaby, W. / Albertella, M. / Rak, J. / De Braekeleer, E. / Tsagkogeorga, G. / Pilka, E.S. / Aspris, D. / Leggate, D. / Hendrick, A.G. / Webster, N.A. / Andrews, B. / Fosbeary, R. / Guest, P. / Irigoyen, N. / Eleftheriou, M. / Gozdecka, M. / Dias, J.M.L. / Bannister, A.J. / Vick, B. / Jeremias, I. / Vassiliou, G.S. / Rausch, O. / Tzelepis, K. / Kouzarides, T.
External linksNature / PubMed:33902106
MethodsX-ray diffraction
Resolution3 Å
Structure data

PDB-7o2i:
METTL3-METTL14 heterodimer bound to the SAM competitive small molecule inhibitor STM2457
Method: X-RAY DIFFRACTION / Resolution: 3 Å

Chemicals

ChemComp-V22:
~{N}-[[6-[(cyclohexylmethylamino)methyl]imidazo[1,2-a]pyridin-2-yl]methyl]-4-oxidanylidene-1~{H}-pyrido[1,2-a]pyrimidine-2-carboxamide

ChemComp-DMS:
DIMETHYL SULFOXIDE / DMSO, precipitant*YM

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsRNA BINDING PROTEIN / methyltransferase / SAM / inhibitor / m6A

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