Structure-guided design of a methyl donor cofactor that controls a viral histone H3 lysine 27 methyltransferase activity.
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ABSTRACT:
SUBMITTER: Li J
PROVIDER: S-EPMC3326379 | biostudies-literature | 2011 Nov
REPOSITORIES: biostudies-literature
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Structure-guided design of a methyl donor cofactor that controls a viral histone H3 lysine 27 methyltransferase activity.
Li Jiaojie J Wei Hua H Zhou Ming-Ming MM
Journal of medicinal chemistry 20111012 21
vSET (a viral SET domain protein) is an attractive polycomb repressive complex 2 (PRC2) surrogate to study the effect of histone H3 lysine 27 (H3K27) methylation on gene transcription, as both catalyze histone H3K27 trimethylation. To control the enzymatic activity of vSET in vivo with an engineered S-adenosyl-l-methionine (SAM) analogue as methyl donor cofactor, we have carried out structure-guided design, synthesis, and characterization of orthogonal vSET methyltransferase mutant/SAM analogue ...[more]
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