Al-Hamashi, Ayad A. et al. published their research in Acta Pharmaceutica Sinica B in 2021 |CAS: 574-98-1

The Article related to amino acids role: bsu (biological study, unclassified), biol (biological study), computational biology, drug design, homo sapiens, human, methylation, molecular docking, molecular modeling, tripeptides role: bsu (biological study, unclassified), biol (biological study) (rgk), tripeptides role: bsu (biological study, unclassified), biol (biological study) (rgr) and other aspects.Application of 574-98-1

On September 30, 2021, Al-Hamashi, Ayad A.; Chen, Dongxing; Deng, Youchao; Dong, Guangping; Huang, Rong published an article.Application of 574-98-1 The title of the article was Discovery of a potent and dual-selective bisubstrate inhibitor for protein arginine methyltransferase 4/5. And the article contained the following:

Protein arginine methyltransferases (PRMTs) have been implicated in the progression of many diseases. Understanding substrate recognition and specificity of individual PRMT would facilitate the discovery of selective inhibitors towards future drug discovery. Herein, we reported the design and synthesis of bisubstrate analogs for PRMTs that incorporate a S-adenosylmethionine (SAM) analog moiety and a tripeptide through an alkyl substituted guanidino group. Compound AH237 is a potent and selective inhibitor for PRMT4 and PRMT5 with a half-maximal inhibition concentration (IC50) of 2.8 and 0.42 nmol/L, resp. Computational studies provided a plausible explanation for the high potency and selectivity of AH237 for PRMT4/5 over other 40 methyltransferases. This proof-of-principle study outlines an applicable strategy to develop potent and selective bisubstrate inhibitors for PRMTs, providing valuable probes for future structural studies. The experimental process involved the reaction of 2-(2-Bromoethyl)isoindoline-1,3-dione(cas: 574-98-1).Application of 574-98-1

The Article related to amino acids role: bsu (biological study, unclassified), biol (biological study), computational biology, drug design, homo sapiens, human, methylation, molecular docking, molecular modeling, tripeptides role: bsu (biological study, unclassified), biol (biological study) (rgk), tripeptides role: bsu (biological study, unclassified), biol (biological study) (rgr) and other aspects.Application of 574-98-1

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary