Structure-guided design of a methyl donor cofactor that controls a viral histone H3 lysine 27 methyltransferase activity.
J Med Chem
; 54(21): 7734-8, 2011 Nov 10.
Article
em En
| MEDLINE
| ID: mdl-21958314
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.
Texto completo:
1
Coleções:
01-internacional
Temas:
Geral
Base de dados:
MEDLINE
Assunto principal:
S-Adenosil-Homocisteína
/
Proteínas Virais
/
Histona-Lisina N-Metiltransferase
/
Coenzimas
Idioma:
En
Revista:
J Med Chem
Assunto da revista:
QUIMICA
Ano de publicação:
2011
Tipo de documento:
Article
País de afiliação:
Estados Unidos