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First total syntheses of (−)-macrosphelides J and K and elucidation of their absolute configuration
Yun, Hwayoung,Paek, Seung-Mann,Jung, Jong-Wha,Kim, Nam-Jung,Kim, Seok-Ho,Suh, Young-Ger Royal Society of Chemistry 2009 Chemical communications Vol.2009 No.18
<P>First total syntheses of (–)-macrosphelides J and K and their structural elucidation are described.</P> <P>Graphic Abstract</P><P>First total syntheses of (–)-macrosphelides J and K <I>via</I> stereoselective nitrile oxide–olefin cycloaddition and their structural elucidation are described. <IMG SRC='http://pubs.rsc.org/services/images/RSCpubs.ePlatform.Service.FreeContent.ImageService.svc/ImageService/image/GA?id=b817693k'> </P>
Enantioselective Total Synthesis of a Natural Iridoid
Lee, Sujin,Paek, Seung-Mann,Yun, Hwayoung,Kim, Nam-Jung,Suh, Young-Ger American Chemical Society 2011 Organic letters Vol.13 No.13
<P>The first total synthesis of 6-hydroxy-7-(hydroxymethyl)-4-methylenehexahydrocyclopenta[<I>c</I>]pyran-1(3<I>H</I>)-one has been accomplished. A key feature of the synthesis includes facile construction of the bicyclic lactone intermediate via intramolecular Pd(0)-catalyzed allylic alkylation and the efficient transformation of this intermediate into the iridoid skeleton employing silicon tethered radical cyclization.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/orlef7/2011/orlef7.2011.13.issue-13/ol201089f/production/images/medium/ol-2011-01089f_0009.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/ol201089f'>ACS Electronic Supporting Info</A></P>
FMS-like tyrosine kinase 3 inhibitors: a patent review
Lee, Jongkook,Paek, Seung-Mann,Han, Sun-Young Informa UK, Ltd. 2011 Expert opinion on therapeutic patents Vol.21 No.4
<P><B><I>Introduction:</I></B> Flt3 (FMS-like tyrosine kinase 3) has been presented as a target for novel anti-leukemic drugs because Flt3 mutations have been observed in acute myeloid leukemia (AML) cells. Due to both the poor efficacy and high toxicity of current standard AML therapies, there is an unmet need for new, improved therapies. Flt3 inhibitors have great potential to address this with mutated Flt3.</P><P><B><I>Areas covered:</I></B> This paper provides a comprehensive review of the Flt3 inhibitor patents currently available. Information from original research articles in peer-reviewed journals and current clinical developments from several resources is also described.</P><P><B><I>Expert opinion:</I></B> Our understanding of Flt3 inhibitors has been increased by findings from recent preclinical and clinical trials. Some Flt3 inhibitors show good efficacy in AML patients, but relapse and resistance to these inhibitors are still unavoidable. To address these problems, structurally diverse inhibitors, which exhibit inhibitory activities against both wild type and mutated Flt3, should be explored.</P>
Simultaneous quantitative monitoring of drug-induced caspase cascade pathways in carcinoma cells
Naoghare, Pravin K.,Ki, Hyeon A.,Paek, Seung-Mann,Tak, Yu Kyung,Suh, Young-Ger,Kim, Sang Geon,Lee, Kyeong-Hee,Song, Joon Myong Royal Society of Chemistry 2010 Integrative biology Vol.2 No.1
<P>Caspases are the key mediators of apoptosis. The caspase cascade includes a series of events leading to the activation of initiator and downstream caspases in a cell. Analysis of the caspase cascade in intact cells, however, has generally been limited as the simultaneous monitoring of upstream and downstream caspases is not well executed. In an effort to monitor the activation of caspase cascades in an intact cell, high-content cellular imaging that allows simultaneous quantitative monitoring of caspase activation has been developed. This has great significance for the exploration of various cellular caspases involved in apoptotic pathways as possible therapeutic targets in the process of drug discovery. To explore the potential of simultaneous monitoring of caspase-mediated apoptotic pathways, human myeloid leukemia HL-60 cells were treated with SH-03 {(7S,7<I>aR</I>,13<I>aS</I>)-9,10-dimethoxy-3,3-dimethyl-7,7<I>a</I>,13,13<I>a</I>-tetrahydro-3<I>H</I>-chromeno [3,4-<I>b</I>]pyrano[2,3-<I>h</I>]chromen-7-ol} (a newly synthesized candidate), camptothecin or naringenin (agents known to induce apoptosis) with or without caspase inhibitors. SH-03 or naringenin treatment initiated the caspase cascade through an intrinsic apoptotic pathway, whereas camptothecin treatment triggered both intrinsic and extrinsic caspase cascades. We now report a new approach based on uniform threshold intensity distribution that facilitates rapid, quantitative monitoring of drug-induced caspase cascades through multi-spectral and multicolor imaging cytometry.</P> <P>Graphic Abstract</P><P>Simultaneous monitoring of caspase cascades. The developed concept may have fundamental significance in establishing image-based assays for elucidating simultaneous cellular events. <IMG SRC='http://pubs.rsc.org/services/images/RSCpubs.ePlatform.Service.FreeContent.ImageService.svc/ImageService/image/GA?id=b916481b'> </P>
Caspase Cleavage of Receptor Tyrosine Kinases in the Dependence Receptor Family
Park Gyu Hwan,Kang Yoo Kyung,Paek Seung-Mann,Shin Chan Young,Han Sun-Young 한국응용약물학회 2023 Biomolecules & Therapeutics(구 응용약물학회지) Vol.31 No.4
Dependence receptors are a group of receptor proteins with shared characteristics of transducing two different signals within cells. They can transduce a positive signal of survival and differentiation in the presence of ligands. On the other hand, dependence receptors can transduce an apoptosis signal in the absence of ligands. The function of these receptors depends on the availability of their ligands. Several receptor tyrosine kinases (RTKs) have been reported as dependence receptors. When cells undergo apoptosis by dependence receptors, the intracellular domain of some RTKs is cleaved by the caspases. Among the RTKs that belong to dependence receptors, we focused on eight RTKs (RET, HER2, MET, ALK, TrkC, EphA4, EphB3, and c-KIT) that are cleaved by caspases. In this review, we describe the features of the receptors, their cleavage sites, and the fate of the cleaved products, as well as recent implications on them being used as potential therapeutics for cancer treatment.
Structure-Based Classification and Anti-Cancer Effects of Plant Metabolites
Shin, Seong-Ah,Moon, Sun Young,Kim, Woe-Yeon,Paek, Seung-Mann,Park, Hyun Ho,Lee, Chang Sup MDPI 2018 INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES Vol.19 No.9
<P>A variety of malignant cancers affect the global human population. Although a wide variety of approaches to cancer treatment have been studied and used clinically (surgery, radiotherapy, chemotherapy, and immunotherapy), the toxic side effects of cancer therapies have a negative impact on patients and impede progress in conquering cancer. Plant metabolites are emerging as new leads for anti-cancer drug development. This review summarizes these plant metabolites with regard to their structures and the types of cancer against which they show activity, organized by the organ or tissues in which each cancer forms. This information will be helpful for understanding the current state of knowledge of the anti-cancer effects of various plant metabolites against major types of cancer for the further development of novel anti-cancer drugs.</P>
약학박사 정 시련 교수 정년퇴임 기념호 : 연구논문(재록) ; 생명과학 : 폴록사머와 프로필렌글리콜을 사용한 클로트리마졸함유 좌제의 항암효능 증대 및 간 독성 감소 효과
용철순 ( Chul Soon Yong ),현경희 ( Jing Ji Xuan ),백승환 ( Seung Hwan Paek ),오유경 ( Yu Kyoung Oh ),우종수 ( Jong Soo Woo ),최한곤 ( Han Gon Choi ),김정애 ( Jung Ae Kim ),( Mann Hyung Lee ) 영남대학교 약품개발연구소 2006 영남대학교 약품개발연구소 연구업적집 Vol.16 No.-