• Title/Summary/Keyword: Analogs

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Geochemistry and Petrogenesis of the Badwater Greenstones from Crystal Falls Terrane in Northeastern Wisconsin, U.S.A. (위스콘신주 북동부 지역에 분포하는 Badwater녹암에 대한 지화학적 연구)

  • Wee, Soo-Meen
    • Economic and Environmental Geology
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    • v.29 no.3
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    • pp.281-291
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    • 1996
  • Samples of Badwater greenstones from the Crystal Falls terrane in northeastern Wisconsin have been analyzed for major, trace and rare earth elements. Geochemical characteristics of the rocks provide clues to the petrologic character and paleotectonic environment of basaltic magma generation. They have chemical composition typical of continental tholeiites. The low Mg values and abundances of Ni and Cr indicate that the lavas were extensively fractionated prior to extrusion. The variations of incompatible elements suggest that the rocks were affected by interaction with crustal rocks. The samples least affected by contamination have trace element compositions similar to those of T-type mid-ocean ridge basalts. The parent was modified by crustal contamination process and this process shifted the rock compositions to that of continental tholeiites as the rock evolved. Interpretations of the chemical characteristics of the rocks, based on modem analogs, favor their emplacement in an extensional tectonic regime.

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Effects of Extracellular Stimulation of Different Niche Condition on the Transcriptional Regulation of Matrix Metalloproteinase Genes in the Mouse Embryonic Stem Cells

  • Yun, Jung Im;Kim, Min Seong;Lee, Seung Tae
    • Reproductive and Developmental Biology
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    • v.37 no.2
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    • pp.79-83
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    • 2013
  • Matrix metalloproteinases (MMPs) have been known to affect to cell migration, proliferation, morphogenesis and apoptosis by degrading the extracellular matrix. In the previous studies, undifferentiated mouse embryonic stem cells (ESCs) were successfully proliferated inside the extracellular matrix (ECM) analog-conjugated three-dimensional (3D) poly ethylene glycol (PEG)-based hydrogel. However, there is no report about MMP secretion in ESCs, which makes it difficult to understand and explain how ESCs enlarge space and proliferate inside 3D PEG-based hydrogel constructed by crosslinkers containing MMP-specific cleavage peptide sequence. Therefore, we investigated what types of MMPs are released from undifferentiated ESCs and how extracellular signals derived from various niche conditions affect MMP expression of ESCs at the transcriptional level. Results showed that undifferentiated ESCs expressed specifically MMP2 and MMP3 mRNAs. Transcriptional up-regulation of MMP2 was caused by the 3D scaffold, and activation of integrin inside the 3D scaffold upregulated MMP2 mRNAs synergistically. Moreover, mouse embryonic fibroblasts (MEFs) on 2D matrix and 3D scaffold induced upregulation of MMP3 mRNAs, and activation of integrins through conjugation of extracellular matrix (ECM) analogs with 3D scaffold upregulated MMP3 mRNAs synergistically. These results suggest that successful proliferation of ESCs inside the 3D PEG-based hydrogel may be caused by increase of MMP2 and MMP3 expression resulting from 3D scaffold itself as well as activation of integrins inside the 3D PEG-based scaffold.

Gonadotropin-releasing Hormone and Its Receptor as a Therapeutic Concept in the Progression of Epithelial Ovarian Cancer

  • Kim, Ki-Yon;Choi, Kyung-Chul
    • Journal of Embryo Transfer
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    • v.24 no.1
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    • pp.1-14
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    • 2009
  • Ovarian cancer is a significant cause of cancer-related death in women, but the main biological causes remain open questions. Hormonal factors have been considered to be an important determinant causing ovarian cancer. Recent studies have shown that gonadotropin-releasing hormone (GnRH)-I and its analogs have clinically therapeutic value in the treatment of ovarian cancer. In addition, numerous studies have shown that the potential of GnRH-II in normal reproductive system or reproductive disorder. GnRH-I receptors have been detected in approximately 80% of ovarian cancer biopsy specimens as well as normal ovarian epithelial cells and immortalized ovarian surface epithelium cells. GnRH-II receptors have also been found to be more widely expressed than GnRH-I receptors in mammals, suggesting that GnRH receptors may have additional functions in reproductive system including ovarian cancer. The signal transduction pathway following the binding of GnRH to GnRH receptor has been extensively studied. The activation of protein kinase A/C (PKA/PKC) pathway is involved in the GnRH-I induced anti-proliferative effect in ovarian cancer cells. In addition, GnRH-I induced mitogen-activated protein kinase (MAPK) activation plays a role in anti-proliferative effect and apoptosis in ovarian cancer cells and the activation of transcriptional factors related to cellular responses. However, the role of GnRH-I and II receptors, there are discrepancies between previous reports. In this review, the role of GnRH in ovarian cancer and the mechanisms to induce anti-proliferation were evaluated.

Phosphate Number and Acyl Chain Length Determine the Subcellular Location and Lateral Mobility of Phosphoinositides

  • Cho, Hana;Kim, Yeon A;Ho, Won-Kyung
    • Molecules and Cells
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    • v.22 no.1
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    • pp.97-103
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    • 2006
  • Phosphoinositides are critical regulators of ion channel and transporter activity. There are multiple isomers of biologically active phosphoinositides in the plasma membrane and the different lipid species are non-randomly distributed. However, the mechanism by which cells impose selectivity and directionality on lipid movements and so generate a non-random lipid distribution remains unclear. In the present study we investigated which structural elements of phosphoinositides are responsible for their subcellular location and movement. We incubated phosphatidylinositol (PI), phosphatidylinositol 4-monophosphate (PI(4)P) and phosphatidylinositol 4,5-bisphosphate ($PI(4,5)P_2$) with short or long acyl chains in CHO and HEK cells. We show that phosphate number and acyl chain length determine cellular location and translocation movement. In CHO cells, $PI(4,5)P_2$ with a long acyl chain was released into the cytosol easily because of a low partition coefficient whereas long chain PI was released more slowly because of a high partition coefficient. In HEK cells, the cellular location and translocation movement of PI were similar to those of PI in CHO cells, whereas those of $PI(4,5)P_2$ were different; some mechanism restricted the translocation movement of $PI(4,5)P_2$, and this is in good agreement with the extremely low lateral diffusion of $PI(4,5)P_2$. In contrast to the dependence on the number of phosphates of the phospholipid head group of long acyl chain analogs, short acyl chain phospholipids easily undergo translocation movement regardless of cell type and number of phosphates in the lipid headgroup.

THE SYNTHESIS, PHYSICAL PROPERTY, AND THE BIOLOGICAL ACTIVITY OF NOVEL NEO-CERAMIDES

  • Kim, Duck-Hee;Lee, Bo-Seaub;Koo, Myeong-Soo;Kim, Hyun-Jun;Lee, Hae-Kwang;Park, Moon-Jae;Lee, Ok-Sub
    • Journal of the Society of Cosmetic Scientists of Korea
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    • v.24 no.3
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    • pp.6-16
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    • 1998
  • Ceramides are currently emerging as the major skin care ingredients due to !heir barrier properties in the stratum corneum of the human skin. Thus, major cosmetic companies have developed synthetic ceramide analogs for their own use. In this study, several ceramide mimic compounds , new skin barrier lipids, were designed and synthesized, and their physical and biological properties were investigated to evaluate their skin care capability. Several structures were designed from the variation of hydrophobic alkyl chain and hydrophilic moiety by the use of molecular modeling software. The selected targets were synthesized, and their properties and activities were studied as the pure form, in the emulsion, or in the lamellar mixture containing cholesterol and fatty acid. Some compounds, such as 1,3-bis(N-(2-hydroxyethyl)-palmitoylamino)-2-hydroxypropane, enhanced the restoration of skin barrier damaged by SDS(sodium dodecyl sulfate), and by acetone treatment. The rate of restoration was comparable to that of natural ceramides. The synthesized compounds alleviated SDS induced skin irritation and facilitated lamellar phase liquid crystal formation. The treatment of 1,3-Dis(N-(2-hydroxyethyl)-palmitoylam ino)-2-hyd roxypropane on the acetone damaged skin revealed that the compound promoted the recovery of intercellular lipid lamellar structure of stratum corneum layer. The replacement of palmitoyl groups of the compound with shorter alkyl chain gave lower emulsion viscosity and liquid crystal density, suggesting easier formulation and poorer barrier activity. Most of the synthesized compounds were non-irritable in various toxicological tests proving that they can be safely introduced to the skin care formulations.

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Conformational Analysis of Cyclodextrins and Their Methylated Analogs (시클로 덱스티린과 그 메틸유도체의 구조분석)

  • Hee-Sook Choi
    • Journal of the Korean Chemical Society
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    • v.36 no.2
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    • pp.324-328
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    • 1992
  • The $^1H$ NMR chemical shifts and coupling constants for ${\alpha}$-, permethyl-${\alpha}$-, ${\beta}$-and permethyl-${\beta}$-cyclodextrins in neutral aqueous media were assigned based on the 470MHz spectra. In order to obtain accurate chemical shifts and coupling constants the experimental spectra were analyzed with the Raccoon spin simulation program. The rotamer distribution around the$C_{5-}C_6$ bond of the cyclodextrins evaluated from the coupling constants of $J_{56a}$ and $J_{56b}$. In our calculation of the ${\alpha}$-, and ${\beta}$-cycliodextrin showed that gg conformers were most favorable form and tg conformers were least favorable form. It is very interesting to note the changes in $J_{56a}$, $J_{56b}$ coupling constants of permethylated ${\alpha}$- and ${\beta}$-cyclodextrins from unmodified one. The gg conformers were more increased than unmodified one and instead of tg conformers gt conformers were least favorable one upon methylation.

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Effects of Eyestalk Ablation on the Embryogenesis of Spider Crab, Libinia emarginata

  • Jo Que-Tae;Park Mi Seon;Jeon Im Gi;Laufer Hans
    • Fisheries and Aquatic Sciences
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    • v.1 no.2
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    • pp.269-275
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    • 1998
  • Spider crabs, Libinia emarginata, were eyestalk-ablated unilaterally and bilaterally to manipulate endogenous methyl farnesoate (MF) to increase during the embryogenesis. Endogenous MF were measured weekly over the embryogenesis of the crab, using HPLC with the aids of GC/MS and MS database (CAS 010485-70-8) for the identification of the hormone. Initial MF titers both in the hemolymph and embryos of intact control were at bottom levels and the hormone concentrations kept unchanged (p<0.05), reflecting physiological unnecessaries of the hormone in the embryogenesis. Eyestalk ablation significantly stimulated the crabs to increase endogenous MF in both tissues (p<0.0l). In the response of the embryos to the increased MF, no growth stimulations were observed, at least, in the first part of embryogenesis. The increased mortalities and immature sheddings of embryos resulted from the crabs under the influence of elevated MF in both tissues, instead, suggesting that the elevated MF against the crab's requirement blocked the normal developmental process of the crab embryos. These data can give crustacean endocrinologists some insights to understand the effects of the hormone on the crustacean reproduction studied previously in which JH analogs ambiguously affected the crustacean reproduction depending on the reproductive stages. The data also can give shrimp aquaculturists some implication of a possible generation of unfavorable shrimp seeds attributed to elevated egg MF originated from their eyestalk-ablated mother shrimp.

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Exploration of the Glycosyltransferase BmmGT1 from a Marine-Derived Bacillus Strain as a Potential Enzyme Tool for Compound Glycol-Diversification

  • Liu, Quanquan;Ren, Pengfei;Liu, Yang;Qin, Wen;Li, Huayue;Li, Wenli
    • Journal of Microbiology and Biotechnology
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    • v.28 no.6
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    • pp.931-937
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    • 2018
  • Glycosyltransferases (GTs) from microbes are an emerging and rich source for efficient glycol-transformation of natural/unnatural compounds. Here, we probed the catalytic capability and substrate promiscuity of BmmGT1 from marine-derived Bacillus methylotrophicus B-9987. The regioselectivity of BmmGT1 on macrolactin A (1) was explored by optimization of the reaction conditions, in which a series of O-glycosylated macrolactins (1a-1e) were generated, including two new di/tri-O-glucosyl analogs (1b and 1e). Furthermore, BmmGT1 was able to catalyze the glycosylation of the thiol (S-) or amine (N-) sites of phenolic compounds (2 and 3), leading to the generation of N- (2a) or S-glycosides (3a and 3b). The present study demonstrates that BmmGT1 could serve as a potential enzyme tool for O-, N-, or S-glycosyl structural diversification of compounds for drug discovery.

Anions as Connectors for Higher Dimensions. Silver(I) Trifuoracetate with 3,3'-Oxybispyridine vs 3,3'-Thiobispyridine

  • Kim, Yun-Ju;Yoo, Kyung-Ho;Park, Ki-Min;Hong, Jong-Ki;Jung, Ok-Sang
    • Bulletin of the Korean Chemical Society
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    • v.23 no.12
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    • pp.1744-1748
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    • 2002
  • Trifluoroacetate anion as a connector has been studied on $AgCF_3CO_2$ with 3,3'-$Py_2X$(X=O vs S) produces 1 : 1 adducts of [Ag($CF_3CO_2$)(3,3'-$Py_2X<$)]. Crystallographic characterization of [Ag($CF_3CO_2$)(3,3'-$Py_2X$)](monoclinic $P2_1$a=7.383(1)$\AA$b=19.801(3)$\AA$c=9.297(3)$\AA$,$\beta$=$100.26(2)^{\circ}$,V=1337.4(5) $\AA^3$, Z=2, R=0.0386) reveals that the 3,3'-$Py_2O$ spacer connects two silver ions to give a single strand and that the single strands are linked via the trifluoroacetate anions in an "up and down even-bridge" to give an elegant molecular grid. The framework of [$Ag(CF_3CO_2)(3,3'-Py_2X)$](monoclinic $P2_1/c$a=8.331(2)$\AA$b=14.010(2)$\AA$,c=11.926(3 $\AA$$\beta$=$93.70(2)^{\circ}$=1385.1(6)$\AA^3$, Z=4, R=0.0589) is a single-strand. The single strands are connected via the trifluoroacetate anions in a double-bridge, resulting in a typical molecular chicken-wire. The trifluoroacetate anion as a connector appears to be primarily associated with its moderately coordinating ability. Their structural features have been discussed based on the anion exchangeability. Thermal analyses indicate that the compounds are stable up to approximately $200^{\circ}C$.

Protectors of Oxidative Stress Inhibit AB(1-42) Aggregation in vitro

  • Kong, Byung-Mun;Ueom, Jeong-Hoon;Kim, In-Kyung;Lim, Dong-Yeol;Kang, Jong-Min;Lee, Kyung-Hee
    • Bulletin of the Korean Chemical Society
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    • v.23 no.12
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    • pp.1773-1777
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    • 2002
  • Reactive oxygen species(ROS) have been investigated to have pivotal roles on amyloidogenecity of $\beta-amyloidpeptide(A\beta)$, the major component of senile plaques in Alzheimer's disease(AD) brain. Addition of radical scavengers is one of the on-going strategies for therapeutic treatment for AD patients. Hsp104 protein including two ATP binding sites from Saccharomyces cerevisiae, as a molecular chaperone, was known to function as a protector of ROS generation when exposed to oxidative stress in our previous study. This observation has led us to investigate Hsp104 protein as a molecular mediator of $A{\beta}$ aggregation in this study. We have developed a new way of expression for Hsp104 protein using GST-fusion tag. As we expected, formation of $A{\beta}$ aggregate was protected by wild type Hsp104 protein, but not by the two ATP-binding site mutant, based on Thioflavin-T fluorescence. Interestingly, Hsp104 protein was observed to keep $A{\beta}$ from forming aggregates independent of ATP binding. On the other hand, disaggregation of $A{\beta}$ aggregates by wild type Hsp104 was totally dependent on the presence of ATP. On the other hand, mutant Hsp104 with two ATP binding sites altered exhibited no inhibition. Another effective antioxidant, hydrazine analogs of curcumin were also effective in $A{\beta}$ fibrilization as protectors against oxidative stress. Based on these observations we conclude that Hsp104 and curcumin derivatives, as protectors of oxidative stress, inhibit $A{\beta}$ aggregation in virto and can be candidates for therapeutic approaches in cure of some neurodegenerative disease.