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Discovery of β-Arrestin Biased Ligands of 5-HT<sub>7</sub>R
Kim, Youngjae,Kim, Hyunguk,Lee, Jieon,Lee, Jae Kyun,Min, Sun-Joon,Seong, Jihye,Rhim, Hyewhon,Tae, Jinsung,Lee, Hyunjoo Jenny,Choo, Hyunah American Chemical Society 2018 Journal of medicinal chemistry Vol.61 No.16
<P>Though many studies have been published about therapeutic potentials of selective 5-HT<SUB>7</SUB>R ligands, there have been few biased ligands of 5-HT<SUB>7</SUB>R. The development of potent and selective biased ligands of 5-HT<SUB>7</SUB>R would be of great help in understanding the relationship between pharmacological effects and G protein/β-arrestin signaling pathways of 5-HT<SUB>7</SUB>R. In order to identify 5-HT<SUB>7</SUB>R ligands with biased agonism, we designed and synthesized a series of tetrahydroazepine derivatives <B>1</B> and <B>2</B> with arylpyrazolo moiety or arylisoxazolo moiety. Through several biological evaluations such as binding affinity, selectivity profile, and functions in G protein and β-arrestin signaling pathways, 3-(4-chlorophenyl)-1,4,5,6,7,8-hexahydropyrazolo[3,4-<I>d</I>]azepine <B>1g</B> was discovered as the β-arrestin biased ligand of 5-HT<SUB>7</SUB>R. In an electroencephalogram (EEG) test, <B>1g</B> increased total non-rapid eye movement (NREM) sleep time and decreased total rapid eye movement (REM) sleep time.</P> [FIG OMISSION]</BR>
Converting a Host Receptor into Sustained Intranasal Virucides against SARS-CoV-2 Using Nanodiscs
Jaehyeon HWANG,Wonbeom PARK,Soomin KIM,SeungJoo KIM,Suhyun KIM,Nayoon CHOI,Eunkhang PARK,Hwanju KIM,Mina KIM,Hyunjoo CHOO,Soyun CHOI,MinKyeom KIM,YeonJin CHO,Dae-Hyuk KWEON 한국생물공학회 2023 한국생물공학회 학술대회 Vol.2023 No.10