Recent Advances in Chemical Tools for the Regulation and Study of Protein Lysine Methyltransferases.
Chem Rec
; 18(12): 1745-1759, 2018 Dec.
Article
en En
| MEDLINE
| ID: mdl-30079624
ABSTRACT
Protein lysine methyltransferases (PKMTs) are epigenetic regulators that modulate gene transcription and physiological functions by catalyzing the post-translational methylation of specific lysine residues of substrate proteins, such as histones. They are considered to be candidate drugs for the treatment of various diseases, including acute myeloid leukemia, and in the past decade, potent and selective inhibitors of individual PKMTs have been developed. Some are currently under clinical trial. In this review, we will focus on some breakthrough PKMT inhibitors, and discuss chemistry-based methods available for elucidation of the physiological functions of PKMTs and methylated proteins.
Palabras clave
Texto completo:
1
Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Histonas
/
N-Metiltransferasa de Histona-Lisina
/
Epigenómica
Límite:
Humans
Idioma:
En
Revista:
Chem Rec
Asunto de la revista:
QUIMICA
Año:
2018
Tipo del documento:
Article
País de afiliación:
Japón