Dong, Guangping; Iyamu, Iredia D.; Vilseck, Jonah Z.; Chen, Dongxing; Huang, Rong published the artcile< Improved Cell-Potent and Selective Peptidomimetic Inhibitors of Protein N-Terminal Methyltransferase 1>, Category: bromides-buliding-blocks, the main research area is peptidomimetic inhibitor preparation antitumor mol docking protein terminal methyltransferase; cell-permeable inhibitor; peptidomimetic inhibitor; protein N-terminal methyltransferase; structure-based drug design.
A series of new peptidomimetic inhibitors I (R = 3-bromophenyl, cyclohexylmethyl, 2-(4-phenylphenyl)ethyl, etc.) was designed and synthesized. Through a focused optimization of DC113, a new cell-potent peptidomimetic inhibitor GD562 (IC50 = 0.93 ± 0.04μM) is discovered. GD562 exhibited improved inhibition of the cellular N-terminal methylation levels of both the regulator of chromosome condensation 1 and the oncoprotein SET with an IC50 value of ∼50μM in human colorectal cancer HCT116 cells. Notably, the inhibitory activity of GD562 for the SET protein increased over 6-fold compared with the previously reported cell-potent inhibitor DC541. Furthermore, GD562 also exhibited over 100-fold selectivity for NTMT1 against several other methyltransferases. Thus, this study provided a valuable probe to investigate the biol. functions of NTMT1.
Molecules published new progress about Amines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 3959-07-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H8BrN, Category: bromides-buliding-blocks.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary