7O2I

METTL3-METTL14 heterodimer bound to the SAM competitive small molecule inhibitor STM2457

Summary for 7O2I

• Entry DOI: 10.2210/pdb7o2i/pdb
• Descriptor: N6-adenosine-methyltransferase catalytic subunit, N6-adenosine-methyltransferase non-catalytic subunit, ~{N}-[[6-[(cyclohexylmethylamino)methyl]imidazo[1,2-a]pyridin-2-yl]methyl]-4-oxidanylidene-1~{H}-pyrido[1,2-a]pyrimidine-2-carboxamide, ... (5 entities in total)
• Functional Keywords: methyltransferase, sam, inhibitor, m6a, rna binding protein
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 2
• Total formula weight: 60175.70

Authors

Pilka, E.S.,Blackaby, W.,Hardick, D.,Harper, C.,Hewstone, D.,Ridgill, M.,Rotty, B.,Rausch, O. (deposition date: 2021-03-30, release date: 2021-04-14, Last modification date: 2024-01-31)

• Primary citation: 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.; Small-molecule inhibition of METTL3 as a strategy against myeloid leukaemia.; Nature, 593:597-601, 2021; PubMed: 33902106; DOI: 10.1038/s41586-021-03536-w

Experimental method

X-RAY DIFFRACTION (3 Å)