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( Hiyoung Kim ),( Jungwook Chin ),( Hyukjae Choi ),( Kyungryul Baek ),( Tae Gu Lee ),( Seong Eon Park ),( Weihong Wang ),( Dongyup Hahn ),( Inho Yang ),( Jihye Lee ),( Bora Mun ),( Merrick Ekins ),( S 영남대학교 약품개발연구소 2013 영남대학교 약품개발연구소 연구업적집 Vol.23 No.0
Two unprecedented phosphorus-containing iodinated polyacetylenes, phosphoiodyns A and B (1-2), were isolated from a Korean marine sponge Placospongia sp. Their structures were elucidated by spectroscopic data analysis. Phosphoiodyn A exhibited potent agonistic activity on human peroxisome proliferator-activated receptor delta (hPPARδ) with an EC(50) of 23.7 nM.
Kim, Hiyoung,Chin, Jungwook,Choi, Hyukjae,Baek, Kyungryul,Lee, Tae-Gu,Park, Seong Eon,Wang, Weihong,Hahn, Dongyup,Yang, Inho,Lee, Jihye,Mun, Bora,Ekins, Merrick,Nam, Sang-Jip,Kang, Heonjoong American Chemical Society 2013 Organic letters Vol.15 No.1
<P>Two unprecedented phosphorus-containing iodinated polyacetylenes, phosphoiodyns A and B (<B>1</B>–<B>2</B>), were isolated from a Korean marine sponge <I>Placospongia</I> sp. Their structures were elucidated by spectroscopic data analysis. Phosphoiodyn A exhibited potent agonistic activity on human peroxisome proliferator-activated receptor delta (hPPARδ) with an EC<SUB>50</SUB> of 23.7 nM.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/orlef7/2013/orlef7.2013.15.issue-1/ol3031318/production/images/medium/ol-2012-031318_0005.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/ol3031318'>ACS Electronic Supporting Info</A></P>
Lee, Aeju,Chin, Jungwook,Park, Ok Kyu,Chung, Hyunjin,Kim, Jin Won,Yoon, Soo-Young,Park, Kyeongsoon The Royal Society of Chemistry 2013 Chemical communications Vol.49 No.53
<P>A novel near-infrared fluorescence (NIRF) copper sensor allows rapid and ultra-sensitive detection of copper ions with excellent selectivity and specificity due to the specificity of click ligation and effective dark-quenching mechanism.</P>
( Dongyup Hahn ),( Hiyoung Kim ),( Inho Yang ),( Jungwook Chin ),( Hoosang Hwang ),( Dong Hwan Won ),( Byoungchan Lee ),( Sang Jip Nam ),( Merrick Ekins ),( Hyukjae Choi ),( Heonjoong Kang ) 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
Three new structurally related depsipeptides, halieylindramides F-H (1-3), and two known halieylindra-mides were isolated from a Petrosia sp. marine sponge collected off the shore of Youngdeok-Gun, East Sea, Republic of Korea. Their planar structures were elucidated by extensive spectroscopic data analyses including ID and 2D NMR data as well as MS data. The absolute configurations of halicylin-drarnides F-H (1-3) were determined by Marfey``s method in combination with Edman degradation. The absolute config-urations at C-4 of the dioxyindolyl alanine (Dioia) residues of halieylindramides G (2) and H (3) were determined as 4S and 4R, respectively, based on ECD spectroscopy. The C-2 configurations of Dioia in 2 and 3 were speculated to both be 2R based on the shared biogenesis of the halicylindramides. Halieylindrarnides F (1), A (4), and C (5) showed human farnesoid X receptor (hFXR) antagonistic activities, but did not bind directly to hFXR.
Marinopyrones A-D, α-pyrones from marine-derived actionmycetes of the family Nocardiopsaceae
( Jihye Lee ),( Chulkyeong Han ),( Tae Gu Lee ),( Jungwook Chin ),( Hyukjae Choi ),( Wonjae Lee ),( Man Jeong Paik ),( Dong Hwan Won ),( Gyusang Jeong ),( Jaeyoung Ko ),( Yeo Joon Yoon ),( Sang Jip Na 영남대학교 약품개발연구소 2016 영남대학교 약품개발연구소 연구업적집 Vol.26 No.-
Two actinomycetes, a member of the rare halophilic genus Streptomonospora and a Nocardiopsis sp. (Nocardiopsaceae), strains CNQ-082 and CNQ-675, respectively. were isolated from marine sediments collected off shore near La Jolla. California. HPLC-UV guided fractionations of the extracts of these strains yielded marinopyrones A-D (1-4), the structures of which were elucidated by interpretation of 10 and 20 NMR and HRMS spectroscopic data. Oxidative ozonation, followed by conversion of the acid product to an α-naphthyl amide, provided the absolute configuration at the chiral center on the side-chain. Marinopyrones A-D were examined for the inhibitory activity on nitric oxide production in LPS-activated mouse macrophage cells (RAW 264.7); marinopyrone D (4) was inhibitory with an IC<sub>50</sub> value of 13 I``M. To our knowledge, marinopyrones A-C are only the second reported natural products from the rare halophi-lic genus Streptomonospora.
Choi, Hyukjae,Oh, Sun Kwan,Yih, Wonho,Chin, Jungwook,Kang, Heonjoong,Rho, Jung-Rae The Pharmaceutical Society of Japan 2008 Chemical & pharmaceutical bulletin Vol.56 No.8
<P>Cyanopeptolin CB071 (1), a trypsin inhibitor, was isolated from the freshwater cyanobacterium <I>Aphanocapsa</I> sp. Its complete structure was determined by detailed NMR spectroscopy and MS analyses, along with chemical reactions. The compound showed inhibition of trypsin at a concentration of IC<SUB>50</SUB>=2.5 μ<SMALL>M</SMALL>.</P>
Singh, Thoudam Debraj,Song, Jaeyoung,Kim, Jina,Chin, Jungwook,Ji, Hyun Dong,Lee, Jae-Eon,Lee, Sang Bong,Yoon, Heeseok,Yu, Ji Hoon,Kim, Sang Kyoon,Yoon, Ghil Suk,Hwang, Hayoung,Lee, Ho Won,Oh, Ji Min,L American Association for Cancer Research 2019 Clinical Cancer Research Vol.25 No.16
<P><B>Purpose:</B></P><P>New strategies to restore sodium iodide symporter (NIS) expression and function in radioiodine therapy–refractive anaplastic thyroid cancers (ATCs) are urgently required. Recently, we reported the regulatory role of estrogen-related receptor gamma (ERRγ) in ATC cell NIS function. Herein, we identified DN200434 as a highly potent (functional IC<SUB>50</SUB> = 0.006 μmol/L), selective, and orally available ERRγ inverse agonist for NIS enhancement in ATC.</P><P><B>Experimental Design:</B></P><P>We sought to identify better ERRγ-targeting ligands and explored the crystal structure of ERRγ in complex with DN200434. After treating ATC cells with DN200434, the change in iodide-handling gene expression, as well as radioiodine avidity was examined. ATC tumor–bearing mice were orally administered with DN200434, followed by <SUP>124</SUP>I-positron emission tomography/CT (PET/CT). For radioiodine therapy, ATC tumor–bearing mice treated with DN200434 were administered <SUP>131</SUP>I (beta ray–emitting therapeutic radioiodine) and then bioluminescent imaging was performed to monitor the therapeutic effects. Histologic analysis was performed to evaluate ERRγ expression status in normal tissue and ATC tissue, respectively.</P><P><B>Results:</B></P><P>DN200434–ERRγ complex crystallographic studies revealed that DN200434 binds to key ERRγ binding pocket residues through four-way interactions. DN200434 effectively upregulated iodide-handling genes and restored radioiodine avidity in ATC tumor lesions, as confirmed by <SUP>124</SUP>I-PET/CT. DN200434 enhanced ATC tumor radioiodine therapy susceptibility, markedly inhibiting tumor growth. Histologic findings of patients with ATC showed higher ERRγ expression in tumors than in normal tissue, supporting ERRγ as a therapeutic target for ATC.</P><P><B>Conclusions:</B></P><P>DN200434 shows potential clinical applicability for diagnosis and treatment of ATC or other poorly differentiated thyroid cancers.</P>
Seongsanamides A-D: Antiallergic Bicyclic Peptides from <i>Bacillus safensis</i> KCTC 12796BP
Kim, Geum Jin,Li, Xian,Kim, Seong-Hwan,Yang, Inho,Hahn, Dongyup,Chin, Jungwook,Nam, Sang-Jip,Nam, Joo-Won,Nam, Doo Hyun,Oh, Dong-Chan,Chang, Hyeun Wook,Choi, Hyukjae American Chemical Society 2018 ORGANIC LETTERS Vol.20 No.23
<P>Six seongsanamides were isolated from the culture broth of <I>Bacillus safensis</I> KCTC 12796BP, and their structures were elucidated by spectroscopic data analysis combined with Marfey’s method, electronic circular dichroism calculations, and biosynthetic gene cluster analysis. Compounds <B>1</B>-<B>4</B> were bicyclic peptides with isodityrosine residues; <B>5</B> and <B>6</B> were monocyclic peptides. Only the bicyclic seongsanamides inhibited degranulation and LTC<SUB>4</SUB>/PGD<SUB>2</SUB> generation in IgE/Ag-stimulated bone marrow-derived mast cells. Oral administration of <B>1</B> suppressed mast cell-dependent passive cutaneous anaphylaxis reaction.</P> [FIG OMISSION]</BR>
Sudeep Kumar,진종화,Hyeon Young Park,Mi-Jin Kim,Jungwook Chin,Sungwoo Lee,Jina Kim,Jung-Guk Kim,Yeon-Kyung Choi,박근규 대한내분비학회 2022 Endocrinology and metabolism Vol.37 No.5
Background: Excessive proliferation and migration of vascular smooth muscle cells (VSMCs), which contributes to the development of occlusive vascular diseases, requires elevated mitochondrial oxidative phosphorylation to meet the increased requirements for energy and anabolic precursors. Therefore, therapeutic strategies based on blockade of mitochondrial oxidative phosphorylation are considered promising for treatment of occlusive vascular diseases. Here, we investigated whether DN200434, an orally available estrogen receptor-related gamma inverse agonist, inhibits proliferation and migration of VSMCs and neointima formation by suppressing mitochondrial oxidative phosphorylation. Methods: VSMCs were isolated from the thoracic aortas of 4-week-old Sprague-Dawley rats. Oxidative phosphorylation and the cell cycle were analyzed in fetal bovine serum (FBS)- or platelet-derived growth factor (PDGF)-stimulated VSMCs using a Seahorse XF-24 analyzer and flow cytometry, respectively. A model of neointimal hyperplasia was generated by ligating the left common carotid artery in male C57BL/6J mice. Results: DN200434 inhibited mitochondrial respiration and mammalian target of rapamycin complex 1 activity and consequently suppressed FBS- or PDGF-stimulated proliferation and migration of VSMCs and cell cycle progression. Furthermore, DN200434 reduced carotid artery ligation-induced neointima formation in mice. Conclusion: Our data suggest that DN200434 is a therapeutic option to prevent the progression of atherosclerosis.