3 years ago

Cover Feature: Development of Novel Inhibitors for Histone Methyltransferase SET7/9 based on Cyproheptadine (ChemMedChem 15/2018)

Cover Feature: Development of Novel Inhibitors for Histone Methyltransferase SET7/9 based on Cyproheptadine (ChemMedChem 15/2018)
Yusuke Okazaki, Hiroyuki Kagechika, Kasumi Ohira, Akihiro Ito, Takashi Fujiwara, Shin Sato, Michitake Hirano, Minoru Yoshida, Tomoya Hirano, Hideaki Niwa, Takashi Umehara, Yuki Maemoto

Abstract

The Cover Feature shows the inhibitor of histone methyltransferase SET7/9 based on a novel scaffold, cyproheptadine, which is used clinically as a serotonin receptor antagonist or histamine receptor antagonist. Among its derivatives, a compound bearing a 2‐hydroxy group showed the most potent activity, while a 3‐hydroxy group or other hydrophilic functional groups such as acetamide decreased the activity. Structural analysis clarified a rationale for the improved potency only by tightly restricted location and type of hydrophilic group. These results are helpful for further structure‐based development of SET7/9 inhibitors. More information can be found in the Full Paper by Tomoya Hirano et al. on page 1530 in Issue 15, 2018 (DOI: 10.1002/cmdc.201800233).

Publisher URL: https://onlinelibrary.wiley.com/doi/abs/10.1002/cmdc.201800495

DOI: 10.1002/cmdc.201800495

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