7PPY

CARM1 in complex with EML709

Summary for 7PPY

• Entry DOI: 10.2210/pdb7ppy/pdb
• Descriptor: Histone-arginine methyltransferase CARM1, methyl 6-[4-[[~{N}-[[(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]methyl]carbamimidoyl]amino]butylcarbamoylamino]-4-oxidanyl-naphthalene-2-carboxylate, 1,2-ETHANEDIOL, ... (4 entities in total)
• Functional Keywords: protein arginine n-methyltransferase, prmt4, carm1, inhibitor, transcription
• Biological source: Mus musculus (Mouse)
• Total number of polymer chains: 4
• Total formula weight: 166637.17

Authors

Marechal, N.,Cura, V.,Bonnefond, L.,Troffer-Charlier, N.,Cavarelli, J. (deposition date: 2021-09-15, release date: 2022-04-06, Last modification date: 2024-01-31)

• Primary citation: Iannelli, G.,Milite, C.,Marechal, N.,Cura, V.,Bonnefond, L.,Troffer-Charlier, N.,Feoli, A.,Rescigno, D.,Wang, Y.,Cipriano, A.,Viviano, M.,Bedford, M.T.,Cavarelli, J.,Castellano, S.,Sbardella, G.; Turning Nonselective Inhibitors of Type I Protein Arginine Methyltransferases into Potent and Selective Inhibitors of Protein Arginine Methyltransferase 4 through a Deconstruction-Reconstruction and Fragment-Growing Approach.; J.Med.Chem., 65:11574-11606, 2022; PubMed: 35482954; DOI: 10.1021/acs.jmedchem.2c00252

Experimental method

X-RAY DIFFRACTION (2.42 Å)