Ontology highlight
ABSTRACT:
SUBMITTER: Chen D
PROVIDER: S-EPMC7429357 | biostudies-literature | 2020 Aug
REPOSITORIES: biostudies-literature
Chen Dongxing D Dong Cheng C Dong Guangping G Srinivasan Karthik K Min Jinrong J Noinaj Nicholas N Huang Rong R
Journal of medicinal chemistry 20200716 15
The bisubstrate analogue strategy is a promising approach to develop potent and selective inhibitors for protein methyltransferases. Herein, the interactions of a series of bisubstrate analogues with protein N-terminal methyltransferase 1 (NTMT1) were examined to probe the molecular properties of the active site of NTMT1. Our results indicate that a 2-C to 4-C atom linker enables its respective bisubstrate analogue to occupy both substrate- and cofactor-binding sites of NTMT1, but the bisubstrat ...[more]