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Kwon, Young-Do,Chung, Hea-Jong,Lee, Sun Joo,Lee, Sun-Hwa,Jeong, Byung-Hoon,Kim, Hee-Kwon Elsevier 2018 Bioorganic & medicinal chemistry letters Vol.28 No.4
<P><B>Abstract</B></P> <P>Prostate-specific membrane antigen (PSMA) is an important biological target for therapy and diagnosis of prostate cancer. In this study, novel multivalent PSMA inhibitors with glutamate-urea-lysine structures were designed to improve inhibition characteristics. Precursors of the novel inhibitors were prepared from glutamic acid with di-<I>tert</I>-butyl ester. A near-infrared molecular dye, sulfo-Cy5.5, was introduced into the precursors to generate the final PSMA fluorescent inhibitors, compounds <B>12</B>–<B>14</B>, to visualize prostate cancer. Biological behaviors of the inhibitors were evaluated using <I>in vitro</I> inhibition assays, <I>in vivo</I> fluorescent imaging, and <I>ex vivo</I> biodistribution assays. <I>K</I> <SUB>i</SUB> values from inhibition studies indicated that dimeric inhibitor <B>13</B> with a glutamine linker showed approximately 3-fold more inhibitory activity than monomeric inhibitor <B>12</B>. According to other biological studies using a mouse model of prostate cancer, dimeric inhibitor compounds <B>13</B> and <B>14</B> had higher tumor accumulation than the monomer. However, glutamine-based dimeric inhibitor <B>13</B> showed lower liver uptake than dimeric inhibitor <B>14</B>, which had a benzene structure. Thus, these studies suggest that glutamine-based dimeric inhibitor <B>13</B> can be a promising optical inhibitor of prostate cancer.</P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Kwon, Young-Do,Oh, Jung-Mi,La, Minh Thanh,Chung, Hea-Jong,Lee, Sun Joo,Chun, Sungkun,Lee, Sun-Hwa,Jeong, Byung-Hoon,Kim, Hee-Kwon American Chemical Society 2019 Bioconjugate chemistry Vol.30 No.1
<P>Prostate cancer is one of the most common cancers in the world. It is widely known that prostate-specific membrane antigen (PSMA) is highly expressed in prostate cancer, and hypoxia is a common characteristic of many solid tumors, including prostate cancer. In this study, we designed multifunctional fluorescent inhibitors to target PSMA and tumor hypoxia in order to increase the tumor uptake of inhibitors. Novel PSMA inhibitors were prepared using lysine as the backbone to connect three different functional groups: the glutamate-urea-lysine (GUL) structure for inhibiting PSMA, 2-nitroimidazole for the hypoxia-sensitive moiety, and a near-infrared fluorophore (sulfo-Cyanine 5.5). According to the <I>in vitro</I> PSMA binding assay, novel fluorescent inhibitors were demonstrated to have nanomolar binding affinities. Multifunctional inhibitor <B>2</B> with one 2-nitroimidazole had a similar inhibitory activity to inhibitor <B>1</B> that did not contain the hypoxia targeting moiety, but multifunctional inhibitor <B>3</B> with two 2-nitroimidazoles showed lower inhibitory activity than inhibitor <B>1</B> due to the bulky structure of the hypoxia-sensitive group. However, <I>in vivo</I> optical imaging and <I>ex vivo</I> biodistribution studies indicated that both multifunctional inhibitors <B>2</B> and <B>3</B> had higher accumulation in tumors than inhibitor <B>1</B> due to a synergistic combination of PSMA and hypoxia targeting moieties. These observations suggest that this novel multifunctional strategy might be a promising approach to improve the diagnosis and therapy of prostate cancer.</P> [FIG OMISSION]</BR>
Enhanced Cytotoxicity of 5-FU by bFGF through Up-Regulation of Uridine Phosphorylase 1
Young-Sam Im,Hea Kyeong Shin,Hye-Ryun Kim,So-Hee Jeong,김승렬,Yong-Min Kim,Do Hyung Lee,Seong-Ho Jeon,이현우,최중국 한국분자세포생물학회 2009 Molecules and cells Vol.28 No.2
Anti cancer agent 5-FU (Fluoro Uracil) is a prodrug that can be metabolized and then activated to interfere with RNA and DNA homeostasis. However, the majority of administered 5-FU is known to be catabolized áå=îáîç in the liver where Dihydropyrimidine dehydrogenase (DPD) is abundantly expressed to degrade 5-FU. The biological factors that correlate with the response to 5-FU-based chemotherapy have been proposed to include uridine phosphorylase (UPP), thymidine phosphorylase (TPP), p53 and microsatellite instability. Among these, the expression of UPP is known to be controlled by cytokines such as TNF-α, IL1 and IFN-γ. Our preliminary study using a DNA microarray technique showed that basic fibroblast growth factor (bFGF) markedly induced the expression of UPP1 at the transcription level. In the present study, we investigated whether bFGF could modulate the expression of UPP1 in osteo-lineage cells and examined the sensitivity of these cells to 5-FU mediated apoptosis.
Jang, Jae-Ho,Park, Hea Jung,Park, Jeong Yong,Kim, Hee Un,Hwang, Do-Hoon Elsevier 2018 ORGANIC ELECTRONICS Vol.60 No.-
<P><B>Abstract</B></P> <P>Orange phosphorescent iridium(III) complexes, (DMBT)<SUB>2</SUB>Ir(acac) and (TBT)<SUB>2</SUB>Ir(acac), based on either 2-(3,4-dimethylphenyl)benzo[<I>d</I>]thiazole (DMBT) or 2-(4-(trimethylsilyl)phenyl)benzo[<I>d</I>]thiazole (TBT) as the cyclometalated main ligands and acetylacetone (acac) as an ancillary ligand, were synthesized for solution-processed organic light-emitting diodes (OLEDs). The Ir(III) complex, (BT)<SUB>2</SUB>Ir(acac), which consists of 2-phenylbenzo[<I>d</I>]thiazole (BT) as the main ligand and acac as the ancillary ligand, was also synthesized as a reference. The photophysical, electrochemical, and electroluminescent properties of these Ir(III) complexes were investigated. The OLED fabricated using (TBT)<SUB>2</SUB>Ir(acac) exhibited significantly improved luminance and external quantum efficiency (EQE) as self-quenching at high doping concentrations was successfully prevented by introducing bulky trimethylsilyl groups. The EL spectrum of (TBT)<SUB>2</SUB>Ir(acac) exhibited an emission maximum at 578 nm with a full-width-at-half-maximum of 74 nm and Commission Internationale de L'Eclairage coordinates of (0.55, 0.44) at 1000 cd/m<SUP>2</SUP>. The device with 7 wt% (TBT)<SUB>2</SUB>Ir(acac) dopant exhibited a maximum luminance of 6837 cd/m<SUP>2</SUP>, maximum luminous efficiency of 25.26 cd/A, power efficiency of 12.37 l m/W, and EQE of 9.94%.</P> <P><B>Highlights</B></P> <P> <UL> <LI> New orange phosphorescent (DMBT)<SUB>2</SUB>Ir(acac) and (TBT)<SUB>2</SUB>Ir(acac) were synthesized. </LI> <LI> (DMBT)<SUB>2</SUB>Ir(acac) and (TBT)<SUB>2</SUB>Ir(acac) effectively suppress concentration self-quenching in the fabricated devices. </LI> <LI> The device using (TBT)<SUB>2</SUB>Ir(acac) exhibited a <I>L</I> <SUB>max</SUB> of 6837 cd/m<SUP>2</SUP> and <I>CE</I> <SUB> <I>max</I> </SUB> of 25.26 cd/A. </LI> </UL> </P> <P><B>Graphical abstract</B></P> <P>[DISPLAY OMISSION]</P>
Jadhav Amol Maruti,Park Hea Jung,Jang Jae‐Ho,Park Jeong Yong,Kwak Seon Lee,Hwang Do‐Hoon 대한화학회 2022 Bulletin of the Korean Chemical Society Vol.43 No.1
We developed a new green phosphorescent iridium (III) complex, bis[2-(9-ethyl- 9H-carbazol-3-yl)-1-methyl-1H-benzo[d]imidazole]iridium(III) acetylacetonate [(Bic)2 Ir(acac)], which functions as a solution-processable dopant for organic lightemitting diodes (OLEDs). 2-(9-Ethyl-9H-carbazol-3-yl)-1-methyl-1H-benzo[d]imidazole was incorporated as the main ligand, while acetylacetone was introduced as an ancillary ligand in the heteroleptic iridium (III) complex. The molecular structure of the synthesized (Bic)2Ir(acac) was characterized by 1H- and 13C-NMR. In addition, it was well soluble in common organic solvents, suitable for solution processible dopant material. The Ir (III) complex exhibited a green emission in solution state (dichloromethane) with an emission maximum at 503 nm. The solutionprocessed OLED device using (Bic)2Ir(acac) as a green dopant achieved an external quantum efficiency of 6.85%, with a power efficiency of 14.96 lm/W, a maximum luminous efficiency of 23.00 cd/A, and Commission Internationale de Eclairage coordinates of (0.30, 0.61) at 7 wt% doping concentration.
정은경,조남수,이춘우,최민호,허진영,강성도,고정수,성은경,성기호,이관형,류도곤,이호섭,Jeong, Weun-Kyung,Cho, Nam-Su,Lee, Chun-Woo,Choi, Min-Ho,Hea, Jin-Young,Kang, Sung-Do,Go, Jeong-Soo,Sung, Yeun-Kyung,Sung, Ki-Ho,Lee, Kwang-Hyung,Ryu, D 대한동의생리학회 1999 동의생리학회지 Vol.14 No.2
The aim of the present experiments was to investigate the effect of Palmijihwangtang water extracts on the plasma renin activity and plasma levels of atrial natriuretic peptide and aldosterone in rats. The results of this study were as follows 1. Plasma renin activity was not different after the administration of Palmijihwangtang water extracts 2. Plasma levels of aldosterone decreased significantly after the administration of Palmijihwangtang water extract 3.0 ml/kg. 3. Plasma levels of atrial natriuretic peptide (ANP) decreased significantly after the administration of Palmijihwangtang water extracts.
연미영(Mi Yong Yon),이윤나(Yoon Na Lee),김도희(Do Hee Kim),이지연(Jee Yeon Lee),고은미(Eun Mi Koh),남은정(Eun Jeong Nam),신혜형(Hye Hyung Shin),강백원(Baeg Won Kang),김종욱(Jong Wook Kim),허석(Seok Heo),조해영(Hea Young Cho),김초일(C) 대한지역사회영양학회 2011 대한지역사회영양학회지 Vol.16 No.4
We attempted to define the sources of sodium intake for the Korean population at prepared dish level to provide a basis for developing sustainable nutrition policies and feasible programs for sodium intake reduction. Dietary intake data from 2008 and 2009 Korea National Health and Nutrition Examination Survey was used in the analysis for sodium intake sources. Sodium intake from individual dish consumed by each subject was calculated and used in delineating major sodium sources at dish and dish group level for sub-populations of different sex and age. Also, sodium intake was compared between eaters and non-eaters of some specific dish groups with considerable contribution to total sodium intake. The number of subjects included in the analysis was 18,022 and mean sodium intake was 4,600 mg/capita/day. Major sources of sodium intake at dish group level were in the following order: kimchi (1125 mg, 24.5%), noodles (572 mg, 12.4%), soups (488 mg, 10.6%), stews (399 mg, 8.7%), and cooked rice (284 mg, 6.2%). The magnitude of contribution to total sodium intake by soups and stews was different by age group. Sodium intake difference between eaters and non-eaters was much larger for kimchi group (2,343 mg for male, 1,452 mg for female) than for soups or stews. Interaction between consumption of aforementioned specific dish groups and age was highly significant (p < 0.0005) for both sexes. This study revealed an importance of having not only the control over sodium content of foods/dishes, but also the customized approach for different groups of population to accomplish an appreciable reduction in sodium intake. (Korean J Community Nutr 16(4) : 473~487, 2011)