A Light-Controllable Chemical Modulation of m6 A RNA Methylation.
Angew Chem Int Ed Engl
; 60(33): 18116-18121, 2021 08 09.
Article
em En
| MEDLINE
| ID: mdl-34107156
ABSTRACT
Bioactive small molecules with photo-removable protecting groups have provided spatial and temporal control of corresponding biological effects. We present the design, synthesis, computational and experimental evaluation of the first photo-activatable small-molecule methyltransferase agonist. By blocking the functional N-H group on MPCH with a photo-removable ortho-nitrobenzyl moiety, we have developed a promising photo-caged compound that had completely concealed its biological activity. Short UV light exposure of cells treated with that caged molecule in a few minutes resulted in a considerable hypermethylation of m6 A modification in transcriptome RNAs, implicating a rapid release of the parent active compound. This study validates for the first time the photo-activatable small organic molecular concept in the field of RNA epigenetic research, which represents a novel tool in spatiotemporal and cellular modulation approaches.
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Base de dados:
MEDLINE
Assunto principal:
Raios Ultravioleta
/
RNA Mensageiro
Idioma:
En
Ano de publicação:
2021
Tipo de documento:
Article