Abstract
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 pairs using a "bump-and-hole" strategy.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Chlorella / physiology
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Chlorella / virology
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Coenzymes / chemical synthesis*
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Coenzymes / pharmacology
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Histone-Lysine N-Methyltransferase / metabolism*
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Histones / metabolism
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Lysine / metabolism
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Methylation
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Models, Molecular
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Mutation
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Paramecium / physiology
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Protein Conformation
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S-Adenosylhomocysteine / analogs & derivatives*
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S-Adenosylhomocysteine / chemical synthesis*
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S-Adenosylhomocysteine / pharmacology
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Stereoisomerism
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Structure-Activity Relationship
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Viral Proteins / genetics
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Viral Proteins / metabolism*
Substances
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Coenzymes
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Histones
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Viral Proteins
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S-Adenosylhomocysteine
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Histone-Lysine N-Methyltransferase
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Lysine