• Biomolecules & Therapeutics
• /
• 제30권1호
• /
• pp.64-71
• /
• 2022

Norovirus (NV) is the most common cause of viral gastroenteritis, with the potential to develop into a fatal disease in those who are immuno-compromised, and effective vaccines and treatments are still non-existent. In this study, we aimed to elucidate the molecular mechanism of the previously identified NV replication inhibitor utilizing a vinyl-stilbene backbone, AC-1858. First, we confirmed the inhibition of the NV RNA replication by a structural analog of AC-1858, AC-2288 with its exclusive cytoplasmic sub-cellular localization. We further validated the induction of one specific host factor, the phosphorylated form of heat shock factor (HSF)-1, and its increased nuclear localization by AC-1858 treatment. Finally, we verified the positive and negative impact of the siRNA-mediated downregulation and lentivirus-mediated overexpression of HSF-1 on NV RNA replication. In conclusion, these data suggest the restrictive role of the host factor HSF-1 in overall viral RNA genome replication during the NV life cycle.

• Journal of Photoscience
• /
• 제8권2호
• /
• pp.79-82
• /
• 2001

2-(p-Diethylaminostyryl)pyrrole (I) and 2-[5-diethylaminothienyl]vinyl]pyrrole (II) derivatives with systematic variation of the acceptors have been synthesized and their first hyperpolarizabilities were measured. The $\beta$ values increased systematically as the aromatic resonance energy decreased. Moreover, the value of $\beta$ for the former increased gradually as the acceptor strength increased. The opposite trend observed in the latter series of compounds has been attributed to the distorted structure caused by the steric hindrance between the N-methyl group and the acceptor moiety.

• 한국독성학회:학술대회논문집
• /
• 한국독성학회 2002년도 Current Trends in Toxicological Sciences
• /
• pp.92-92
• /
• 2002

Recently we have reported that various hydroxystilbenes show strong inhibition of human P450 1 activity. A series of synthetic trans-stilbene derivatives were prepared and their inhibitory potentials were evaluated with the bacterial membrane of recombinant human P450 1A1, 1A2 or 1B1 coexpressed with human P450/NADPH-450 reductase to find new candidates for cancer chemoprevention.(omitted)

• 대한약학회:학술대회논문집
• /
• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
• /
• pp.312.3-313
• /
• 2002

Recently we have reported that various hydroxystilbenes show strong inhibition of human P450 1 activity. A series of synthetic trans-stilbene derivatives were prepared and their inhibitory potentials were evaluated with the bacterial membrane of recombinant human P450 1A1, 1A2 or 1B1 coexpressed with human NADPH-P450 reductase to find new candidates for cancer chemoprevention, Of the compounds tested. SY-021 (3.5-dimethoxyphenyl vinyl thiophene) exhibited a potent inhibition of human P450 181 with an IC$_{50}$ value of 2 nM. SY-021 also showed the inhibitrion of P450 1A1 with IC$_{50}$ value of 61 nM and P450 1A2 with IC$_{50}$ value of 11 nM. SY-021 showed 31-fold selectivity for P450 1B1 over P450 1A1 and 6-fold selectivity for P450 1B1 over 1A2. We have further investigated the inhibition kinetics of P450 1A1. 1A2 and 1B1 by SY-021. The modes of inhibition by SY-021were non-compeitive for all three P450 1 enzymes. Effect of preincubation with NADPH on inhibition of P450 1B1 by SY-021 was determined. These results suggest that SY-021 is one of the mostj potent inhibitor of human P450 1 enzymes and may be considered as a good candidate for a cancer chemopreventive agent in human

• 공업화학
• /
• 제9권5호
• /
• pp.710-714
• /
• 1998

Poly(p-phenylene vinylene), PPV를 발광층으로 하고 전자수송층(electron transport layer, ETL)이 도입된 이중 접합구조 유기 전기발광소자(electroluminescence device, ELD)를 제작하고 전기 발광 특성을 조사하였다. 전자 수송제로는 2-(4-biphenyl)-5-(4-tert-butylphenyl)-1,3,4-oxadiazole(PBD)를 사용하고 이를 분산시킬 기재 고분자(matrix polymer)로는 stilbene계 공단량체를 포함하는 poly(styrene-co-p-vinyl-trans-stilbene (PVTS)), poly(styrene-co-MeO-PVTS) 및 poly(styrene-co-MeO-ST)를 합성하였다. 이들 재료를 이용하여 이종 접합구조 ELD를 제조하였으며 poly(styrene-co-PVTS)를 기재 고분자로 쓴 EL 소자가 최대의 휘도를 나타냄을 확인하였다. Poly(styrene-co-MeO-PVTS) 및 poly(styrene-co-MeO-ST) 등 전자 주게 성질을 가진 methoxy기를 함유하는 기재 고분자를 쓴 EL 소자는 전자 수송층이 없는 ITO/PPV/Mg 단층 소자와 휘도가 유사 혹은 낮게 나타났다. Poly(styrene-co-PVTS)를 ETL에 쓴 EL 소자에 있어서 styrene보다 긴 conjugation 길이의 증가가 EL 발광 스펙트럼에 미치는 영향은 크지 않고 실제 발광은 PPV에 의해 주로 일어남이 관찰되었다.