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Hwang, Ki-Jun,Chun, Moon-Woo,Jacobson, Kenneth A.,Jeong, Lak-Shin,Lee, Jeong-A,Moon, Hyung-Ryong,Kim, Hea-Ok,Kim, Kyung-Ran,Lee, Kang-Man,Kim, Bum-Tae 이화여자대학교 약학연구소 2005 藥學硏究論文集 Vol.- No.16
On the basis of the biological activity of neplanocin A and apio-dideoxyadenosine (apio-ddA), novel apio-neplanocin A analogues 5a- d, combining the properties of two nucleosides, were stereoselectively synthesized. The apio moiety of the target nucleosides 5a-d was stereoselectively introduced by treating· lactol 10 with 37% formaldehyde in the presence of potassium carbonate. The carbasugar moiety of neplanocin A was successively built by exposing diene 12 on a Grubbs catalyst in methylene chloride. The final nucleosides 5a-d were synthesized from the condensation of the glycosyl donor 14 with nucleic bases under the standard Mitsunobu conditions. Similarly, apio-aristeromycin 6 and (N)-apio-methanocarbaadenosine 7 were derived from the common intermediate 13 using catalytic hydrogenation and Simmons-Smith cyclopropanation as key steps. All of the final nucleosides 5a-4, 6, and 7 did not show significant inhibitory activity against S-adenosylllolllocysteine hydrolase (SAH) up to 100 ㎛, maybe due to the absence of the secondary hydroxyl group at tile C3'-position, which should be oxidized by cofactor-bound NAD^(+). However, aplo-neplanocin A (5a) showed potent and highly selective binding affinity (K_(i), = 628 ± 69 nM) at the A_(3) adenosine receptor without any binding affinity at the A_(1) and A_(2A) adenosine receptors. In conclusion, we have first developed novel carbocyclic nucleosides with unnatural apio-carbasugarsusing stereoselective hydroxymethylation and RCM reaction and also discovered a new template of human A_(3) adenosine receptor agonist, which play a great rote in developing new A_(3) adenosine receptor agonist as well as in identifying the binding site of the receptor.
Yu, Jinha,Ahn, Seyeon,Kim, Hee Jin,Lee, Moonyoung,Ahn, Sungjin,Kim, Jungmin,Jin, Sun Hee,Lee, Eunyoung,Kim, Gyudong,Cheong, Jae Hoon,Jacobson, Kenneth A.,Jeong, Lak Shin,Noh, Minsoo American Chemical Society 2017 Journal of medicinal chemistry Vol.60 No.17
<P>A(3) adenosine receptor (AR) ligands including A(3) AR agonist, N-6-(3-iodobenzyl)adenosine-5'-N-methyluronamide (1a, IB-MEGA) were examined for adiponectin production in human bone marrow mesenchymal stem cells (hBM-MSCs). In this model, 1a significantly increased adiponectin production, which is associated with improved insulin sensitivity. However, A(3) AR antagonists also promoted adiponectin production in hBM-MSCs, indicating that the A(3) AR pathway may not be directly involved in the adiponectin promoting activity. In a target deconvolution study, their adiponectin-promoting activity was significantly correlated to their binding activity to both peroxisome proliferator activated receptor (PPAR) gamma and PPAR delta. They functioned as both PPAR gamma partial agonists and PPAR delta antagonists. In the diabetic mouse model, la and its structural analogues A(3) AR antagonists significantly decreased the serum levels of glucose and triglyceride, supporting their antidiabetic potential. These findings indicate that the polypharmacophore of these compounds may provide therapeutic insight into their multipotent efficacy against various human diseases.</P>
Design and Synthesis of A₃ Adenosine Receptor Ligands, 2´-Fluoro Analogues of Cl-IB-MECA
Kim, Hea Ok,Park, Jae Gyu,Moon, Hyung Ryong,Gunaga, Prashantha,Lim, Moo Hong,Chun, Moon Woo,Jacobson, Kenneth A.,Kim, Hee-Doo,Jeong, Lak Shin 梨花女子大學校 藥學硏究所 2003 藥學硏究論文集 Vol.- No.12
Synthesis of 2'-deoxy-2'-fluoro-N^(6) -substituted adenosines as bioisosteres of Cl-IB-MECA and their binding affinities to A₃ adenosine receptor are described.
Kyoung-Mee Kim,Eunsook Chung,Selvam Ayarpadikannan,Hyun-A So,Kenneth Ryan Schraufnagle,Ji Hae Park,Se Hyun Park,Jai-Heon Lee 한국육종학회 2013 한국육종학회 심포지엄 Vol.2013 No.07
Heat shock transcription factors (HSFs) are the major heat shock factors regulating the heat stress response. They participate in regulating the expression of heat shock proteins (HSPs), which are critical in the protection against stress damage and many other important biological processes. In this study, a genome-wide analysis was carried out to identify all HSFs soybean genes. Twenty six nonredundant HSF genes (GmHsf) were identified in the latest soybean genome sequence. Chromosomal location, protein domain and motif organization of GmHsfs were analyzed in soybean genome. The phylogenetic relationships, gene duplications and expression profiles of GmHsf genes were also presented in this study. According to their structural features, the predicted members were divided into the previously defined classes A–C, as described in Arabidopsis. Using RT-PCR, the expression patterns of 26 GmHsf genes were investigated under heat stress. The data revealed that these genes presented different expression levels in response to heat stress conditions. Real-time (q)RT-PCR was performed to investigate transcript levels of five GmHsfs in response to multiple abiotic stresses. Differential expression of five GmHsfs implies their role during abiotic stresses. Subcellular localization using GFP-fusion protein demonstrated that GmHsf12 and GmHsf34 were restricted to the nucleus and GmHsf28 was localized in the nucleus and cytoplasm in plant. The results provide a fundamental clue for understanding of the complexity of the soybean HSF gene family and cloning specific function genes in further studies and applications.
Jeong, Lak Shin,Choe, Seung Ah,Gunaga, Prashantha,Kim, Hea Ok,Lee, Hyuk Woo,Lee, Sang Kook,Tosh, Dilip K.,Patel, Amit,Palaniappan, Krishnan K.,Gao, Zhan-Guo,Jacobson, Kenneth A.,Moon, Hyung Ryong 이화여자대학교 약학연구소 2008 藥學硏究論文集 Vol.- No.18
Truncated D-4'-thioadenosine derivatives lacking the 4'-hydroxymethylene moiety were synthesized starting from D-mannose, using cyclization to the 4-thiosugar and one-step conversion of the diol to the acetate as key steps At the human A₃ adenosine receptor (AR), N^(6)-substituted purine analogues bound potently and selectively and acted as antagonists in a cyclic AMP functional assay An N^(6)-(3-chlorobenzyl)purine analogue 9b displayed a K, value of 1 66 nM at the human A₃ AR Thus, truncated D-4'-thioadenosine is an excellent template for Ihe design of novel A₃ AR antagonists to act at both human and murine species.
Eunsook Chung,Kyoung-Mee Kim,Selvam Ayarpadikannan,Hyun-A So,Kenneth Ryan Schraufnagle,Kim Hyo Young,Jae-Sung Kwak,Hai Yang Yu,Jai-Heon Lee 한국육종학회 2012 한국육종학회 심포지엄 Vol.2012 No.07
Heat shock transcription factors (HSFs) are the major heat shock factors regulating the heat stress response. They participate in regulating the expression of heat shock proteins (HSPs), which are critical in the protection against stress damage and many other important biological processes. In this study, a genome-wide analysis was carried out to identify all HSFs soybean genes. Twenty six nonredundant HSF genes (GmHsf) were identified in the latest soybean genome sequence. Chromosomal location, protein domain and motif organization of GmHsfs were analyzed in soybean genome. The phylogenetic relationships, gene duplications and expression profiles of GmHsf genes were also presented in this study. According to their structural features, the predicted members were divided into the previously defined classes A–C, as described in Arabidopsis. Using RT-PCR, the expression patterns of 26 GmHsf genes were investigated under heat stress. The data revealed that these genes presented different expression levels in response to heat stress conditions. Real-time (q)RT-PCR was performed to investigate transcript levels of five GmHsfs in response to multiple abiotic stresses. Differential expression of five GmHsfs implies their role during abiotic stresses. Subcellular localization using GFP-fusion protein demonstrated that GmHsf12 and GmHsf34 were restricted to the nucleus and GmHsf28 was localized in the nucleus and cytoplasm in plant. The results provide a fundamental clue for understanding of the complexity of the soybean HSF gene family and cloning specific function genes in further studies and applications.
Lim, Moo Hong,Kim, Hea Ok,Moon, Hyung Ryoung,Lee, Seung Jin,Chun, Moon Woo,Gao, Zhan-Guo,Melman, Neli,Jacobson, Kenneth A.,Kim, Joong Hyup,Jeong, Lak Shin 梨花女子大學校 藥學硏究所 2003 藥學硏究論文集 Vol.- No.12
Several 3'-fluoro analogues, la, lb, and lc of selective and potent adenosine A₃ receptor agonist, Cl-IB-MECA were synthesized from D-xylose via highly regioselective opening of lyxo-epoxides, 8a and 8b with fluoride anion. Compared to the high binding affinity of CI-IB-MECA to the A₃ adenosine receptor, the corresponding 3'-fluoro derivative showed remarkably decreased binding affinity, indicating that 3'-hydroxyl group acts as hydrogen bonding acceptor, not hydrogen bonding donor like fluorineatom in binding to the A₃ adenosine receptor.
Eunsook Chung,Chang-Woo Cho,Hyun-A So,Kyoung-Mee Kim,Selvam Ayarpadikannan,Kenneth Ryan Schraufnagle,Ji Hae Park,Se Hyun Park,Jai-Heon Lee 한국육종학회 2013 한국육종학회 심포지엄 Vol.2013 No.07
The ubiquitin conjugating enzyme E2 (UBC E2) mediates selective ubiquitination, acting with E1 and E3 enzymes to designate specific proteins for subsequent degradation. In the present study, we characterized the function of the mung bean VrUBC1 gene (Vigna radiata UBC 1). RNA gel-blot analysis showed that VrUBC1 mRNA expression was induced by either dehydration, high salinity or by the exogenous abscisic acid (ABA), but not by low temperature or wounding. Biochemical studies of VrUBC1 recombinant protein and complementation of yeast ubc4/5 by VrUBC1 revealed that VrUBC1 encodes a functional UBC E2. To understand the function of this gene in development and plant responses to osmotic stresses, we overexpressed VrUBC1 in Arabidopsis (Arabidopsis thaliana). The VrUBC1-overexpressing plants displayed highly sensitive responses to ABA and osmotic stress during germination, enhanced ABA- or salt-induced stomatal closing, and increased drought stress tolerance. The expression levels of a number of key ABA signaling genes were increased in VrUBC1-overexpressing plants compared to the wild-type plants. Yeast two-hybrid and bimolecular fluorescence complementation demonstrated that VrUBC1 interacts with AtVBP1 (A. thaliana VrUBC1 Binding Partner 1), a C3HC4-type RING E3 ligase. Overall, these results demonstrate that VrUBC1 plays a positive role in osmotic stress tolerance through transcriptional regulation of ABA-related genes and possibly through interaction with a novel RING E3 ligase.
Jeong, Lak Shin,Shantanu Pal,Choe, Seung Ah,Choi, Won Jun,Kenneth A. Jacobson,Zhan-Guo Gao,Athena M. Klutz,Xiyan Hou,Kim, Hea Ok,Lee, Hyuk Woo,Lee, Sang Kook,Dilip K. Tosh,Moon, Hyung Ryong 이화여자대학교 약학연구소 2009 藥學硏究論文集 Vol.- No.19
Novel D- and L-4´-thioadenosine derivatives lacking the 4´-hydroxymethyl moiety were synthesized, starting from D-mannose and D-gulonic γ-lactone, respectively, as potent and selective species-independent A₃ adenosine receptor (AR) antagonists. Among the novel 4´-truncated 2-H nucleosides tested, a N^(6)-(3-chlorobenzyl) derivative 7c was the most potent at the human A₃ AR (K_(i) = 1.5 nM), but a N^(6)-(3-bromobenzyl) derivative 7d showed the optimal species-independent binding affinity.
Stereoselective Synthesis of 1'-Functionalized-4'-Thionucleosides
Jeong, Lak Shin,Gunaga, Prashantha,Kim, Hea Ok,Tosh, Dilip K.,Lee, Hyuk Woo,Choe, Seung Ah,Moon, Hyung Ryong,Gao, Zhan-Guo,Jacobson, Kenneth A.,Chun, Moon Woo Taylor Francis 2007 NUCLEOSIDES NUCLEOTIDES AND NUCLEIC ACIDS Vol. No.
<P> Stereoselective functionalization of the 1'-position of 4'-thionucleosides was achieved using a stereoselective SN2 reaction controlled by 5-membered ring coordination.</P>