Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L.

Basavapathruni A, Jin L, Daigle SR, Majer CR, Therkelsen CA, Wigle TJ, Kuntz KW, Chesworth R, Pollock RM, Scott MP, Moyer MP, Richon VM, Copeland RA, Olhava EJ. Conformational adaptation drives potent, selective and durable inhibition of the human protein methyltransferase DOT1L. Chem Biol Drug Des. 2012 Dec; 80(6):971-80.

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subject areas

Binding Sites
Cell Line, Tumor
Crystallography, X-Ray
Drug Design
Enzyme Inhibitors
Histone-Lysine N-Methyltransferase
Histones
Humans
Kinetics
Methylation
Methyltransferases
Nucleosides
Protein Binding
Protein Structure, Tertiary
Structure-Activity Relationship

authors with profiles

Robert L. Copeland

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