Rzuczek, Suzanne G. published the artcileFeatures of Modularly Assembled Compounds That Impart Bioactivity Against an RNA Target, Related Products of chlorides-buliding-blocks, the publication is ACS Chemical Biology (2013), 8(10), 2312-2321, database is CAplus and MEDLINE.
Transcriptomes provide a myriad of potential RNAs that could be the targets of therapeutics or chem. genetic probes of function. Cell-permeable small mols., however, generally do not exploit these targets, owing to the difficulty in the design of high affinity, specific small mols. targeting RNA. As part of a general program to study RNA function using small mols., we designed bioactive, modularly assembled small mols. that target the noncoding expanded RNA repeat that causes myotonic dystrophy type 1 (DM1), r-(CUG)exp. Herein, we present a rigorous study to elucidate features in modularly assembled compounds that afford bioactivity. Different modular assembly scaffolds were investigated, including polyamines, α-peptides, β-peptides, and peptide tertiary amides (PTAs). On the basis of activity as assessed by improvement of DM1-associated defects, stability against proteases, cellular permeability, and toxicity, we discovered that constrained backbones, namely, PTAs, are optimal. Notably, we determined that r-(CUG)exp is the target of the optimal PTA in cellular models and that the optimal PTA improves DM1-associated defects in a mouse model. Biophys. analyses were employed to investigate potential sources of bioactivity. These investigations show that modularly assembled compounds have increased residence times on their targets and faster on rates than the RNA-binding modules from which they were derived. Moreover, they have faster on rates than the protein that binds r-(CUG)exp, the inactivation of which gives rise to DM1-associated defects. These studies provide information about features of small mols. that are programmable for targeting RNA, allowing for the facile optimization of therapeutics or chem. probes against other cellular RNA targets.
ACS Chemical Biology published new progress about 42074-68-0. 42074-68-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 2-Chlorotrityl chloride, and the molecular formula is C19H14Cl2, Related Products of chlorides-buliding-blocks.
Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics