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Synthesis and Reaction of 1,5,3,7-Diazadiphosphocine-1,5-Dicarboxylic Acids (1,5,3,7-Diazadiphosphocine-1,5-Dicarboxylic Acids의 합성과 반응)

  • Cho, Seung-Hwan;Song, Ju-Hyun;Lee, Do-Hun;Lee, Yong-Gyun;Park, Yu-Mi;Choi, Soon-Kyu;Hahn, Jung-Tai;Jung, Dai-Il
    • Journal of Life Science
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    • v.17 no.7 s.87
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    • pp.910-914
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    • 2007
  • In order to synthesize new bioactive compounds and contrasting agents, reactions of glycine and glutamic acid as an animo acid with paraformaldehyde and hypophosphorous acid were executed. Products are 3,7-dihydroxy-3,7-dioxoperhydro-1,5,3,7-diazadiphosphocine-1,5-diacetic acid 1 and 3,7-dihydroxy-3,7- dioxoperhydre-1,5,3,7-diazadiphosphocine-1,5-di-(2-glu taric acid) 3. 2-[5-(1,2-Dicarboxyethyl)-3,7-dihydroxy-3,7-dioxo-315.715-[1,5,3,7] diazadiphosphocan-1-yl]-succinic acid 2 by using aspartic acid was not obtained. Esterification of 3,7- dihydroxy-3,7-dioxoperkydro-1,5,3,7-diaza-diphosphocine-1,5-diacetic acid 1 by treatment of methanol, ethanol, and propanol were executed. 3,7-Dihydroxy-3,7-dioxoperhydro-1,5,3,7-diazadiphosphocine-1,5-diacetic acid methyl ester 4, 3.7-dihydroxy-3,7-dioxoperhydro-1,5,3,f-diazadiphosphocine-1.5-diacetic acid ethyl ester 5, and 3,7-dihydroxy-3,7-dioxoperhydro-1,5,3,7-diazadiphosphocine-1,5-diacetic acid propyl ester 6 were respectively synthesized in good yields. Continuously, we will try synthesis of novel compounds and evaluation of biological activity.

Differential Subcellular Localization of Ribosomal Protein L7 Paralogs in Saccharomyces cerevisiae

  • Kim, Tae-Youl;Ha, Cheol Woong;Huh, Won-Ki
    • Molecules and Cells
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    • v.27 no.5
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    • pp.539-546
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    • 2009
  • In Saccharomyces cerevisiae, ribosomal protein L7, one of the ~46 ribosomal proteins of the 60S subunit, is encoded by paralogous RPL7A and RPL7B genes. The amino acid sequence identity between RPl7a and RPl7b is 97 percent; they differ by only 5 amino acid residues. Interestingly, despite the high sequence homology, Rpl7b is detected in both the cytoplasm and the nucleolus, whereas Rpl7a is detected exclusively in the cytoplasm. A site-directed mutagenesis experiment revealed that the change in the amino acid sequence of Rpl7b does not influence its subcellular localization. In addition, introns of RPL7A and RPL7B did not affect the subcellular localization of Rpl7a and Rpl7b. Remarkably, Rpl7b was detected exclusively in the cytoplasm in rpl7a knockout mutant, and overexpression of Rpl7a resulted in its accumulation in the nucleolus, indicating that the subcellular localization of Rpl7a and Rpl7b is influenced by the intracellular level of Rpl7a. Rpl7b showed a wide range of localization patterns, from exclusively cytoplasmic to exclusively nucleolar, in knockout mutants for some rRNA-processing factors, nuclear pore proteins, and large ribosomal subunit assembly factors. Rpl7a, however, was detected exclusively in the cytoplasm in these mutants. Taken together, these results suggest that although Rpl7a and Rpl7b are paralogous and functionally replaceable with each other, their precise physiological roles may not be identical.

Synthesis of 7-Deazahypoxanthine and 7-Deazaadenine Derivatives (7-데아자하이포크산틴과 7-데아자아데닌 유도체의 합성)

  • Sin, Kwan-Seog;Kim, Nam-Ho;Lee, Joo-Heon;Sung, Sun-Young;Pachaly, Peter
    • YAKHAK HOEJI
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    • v.41 no.2
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    • pp.181-186
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    • 1997
  • A series of 7-deazahypoxanthine and 7-deazaadenine derivatives[6,7.8.9.10,13] as purine antagonists was prepared. The pyrrolidine-5-one derivatives[4,11] were treated vith $(C_2H_5)_3OBF_4$ to give 3- aryl-5-ethoxy-2H-3,4-dihydropyrrole[5,12], which were converted to 7-aryl-7,8-dihydro-7(9H)-deazahy-poxanthine[6,7,8,9,10] and 7-phenyl-2-methyl-7,8- dihydro-7(9H)-deazaadenine[13].

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Effects of Anti-B7.1/B7.2 Antibodies on LPS-Stimulated Macrophages

  • Won, Tae-Joon;Huh, Yoon-Joo;Lim, Young-Tae;Song, Dong-Sup;Hwang, Kwang-Woo
    • Biomolecules & Therapeutics
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    • v.18 no.4
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    • pp.463-468
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    • 2010
  • T-cell activation depends on signals received by the T-cell receptor and CD28 co-stimulatory receptor. Since B7.1 and B7.2 molecules expressed on the surface of antigen presenting cells provide co-stimulatory signals through CD28 to T-cells, an inhibitor of CD28-B7.1/B7.2 binding has been proposed as a therapeutic agent for suppression of excessive T-cell activity. Although anti-B7.1/B7.2 antibodies are known to block B7.1 and B7.2 molecules, their effects on intracellular events in antigen presenting cells remain unclear. In this study, anti-B7.1/B7.2 antibodies decreased secretion of nitric oxide and pro-inflammatory cytokines such as TNF-$\alpha$, IL-$1{\beta}$, and IL-12 in LPS-activated RAW264.7 macrophage-like cells and peritoneal macrophages. Moreover, anti-B7.1/B7.2 antibodies inhibited $I{\kappa}B{\alpha}$ phosphorylation and down-regulated expression of co-stimulatory molecules including B7.1, B7.2, and PD-L1 in LPS-stimulated peritoneal macrophages. These findings suggest that CTLA4-Ig and anti-B7.1/B7.2 antibodies may be candidates to treat chronic inflammatory diseases and autoimmune responses caused by excessive activation of both T-cells and macrophages.

Involvement of Transient Receptor Potential Melastatin 7 Channels in Sophorae Radix-induced Apoptosis in Cancer Cells - Sophorae Radix and TRPM7 -

  • Kim, Byung-Joo
    • Journal of Pharmacopuncture
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    • v.15 no.3
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    • pp.31-38
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    • 2012
  • Sophorae Radix (SR) plays a role in a number of physiologic and pharmacologic functions in many organs. Objective: The aim of this study was to clarify the potential role for transient receptor potential melastatin 7 (TRPM7) channels in SR-inhibited growth and survival of AGS and MCF-7 cells, the most common human gastric and breast adenocarcinoma cell lines. Methods: The AGS and the MCF-7 cells were treated with varying concentrations of SR. Analyses of the caspase-3 and - 9 activity, the mitochondrial depolarization and the poly (ADPribose) polymerase (PARP) cleavage were conducted to determine if AGS and MCF-7 cell death occured by apoptosis. TRPM7 channel blockers ($Gd^{3+}$ or 2-APB) and small interfering RNA (siRNA) were used in this study to confirm the role of TRPM7 channels. Furthermore, TRPM7 channels were overexpressed in human embryonic kidney (HEK) 293 cells to identify the role of TRPM7 channels in AGS and MCF-7 cell growth and survival. Results: The addition of SR to a culture medium inhibited AGS and MCF-7 cell growth and survival. Experimental results showed that the caspase-3 and -9 activity, the mitochondrial depolarization, and the degree of PARP cleavage was increased. TRPM7 channel blockade, either by $Gd^{3+}$ or 2-APB or by suppressing TRPM7 expression with small interfering RNA, blocked the SR-induced inhibition of cell growth and survival. Furthermore, TRPM7 channel overexpression in HEK 293 cells exacerbated SR-induced cell death. Conclusions: These findings indicate that SR inhibits the growth and survival of gastric and breast cancer cells due to a blockade of the TRPM7 channel activity. Therefore, TRPM7 channels may play an important role in the survival of patients with gastric and breast cancer.

Effects of Invasive Low Level Laser Acupuncture Therapy(LLLAT) at LU7, LR5, LU7+LR5 on the Hyperlipemia Rats Induced by High Fat Diet (열결(列缺), 여구, 열결배여구에 침습적(侵襲的)으로 조사(照射)된 레이저침료법(鍼療法)이 고지혈증(高脂血症) 백서(白鼠)에 미치는 영향(影響))

  • Ihm, Seon-Joo;Youn, Dae-Hwan;Na, Chang-Su
    • Korean Journal of Acupuncture
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    • v.22 no.3
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    • pp.1-15
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    • 2005
  • Objectives: This research was performed to investigate the effect of invasive low level laser acupuncture therapy(LLLAT) at Yolgyol(LU7), Yogu(LR5) and Yolgyol+Yogu(LU7+LR5) on weight gain, food intake, food efficiency, lipid metabolism, atherogenic index, HTR(HDL-cholesterol to total cholesterol ratio) and liver function in hyperlipidemia rats. Methods : Experimental groups were divided into high fat diet group(Control group), high fat diet and LLLAT at LU7(LU7 group), high fat diet and LLLAT at LR5(LR5 group), LLLAT at LU7 and LR5(LU7+LR5 group). Animals was treated by the LLLAT at 30mW-5min once a 2day during 5 weeks. Results: Body weight was decreased significantly in LU7+LR5 group when compared with control group. Food intake was increased significantly in LU7, LR5, LU7+LR5 group when compared with control group. Food efficiency was decreased significantly in LU7, LR5, LU7+LR5 group when compared with control group. In the lipid metabolism, total cholesterol and HDL-cholesterol was decreased significantly in LU7+LR5 group, LDL-cholesterol and phospholipids were decreased significantly in LR5, LU7+LR5 group, triglyceride and fee fatty acid were decreased significantly in LU7 group when compared with control group. Atherogenic index was decreased significantly in LU7, LR5, LU7+LR5 group when compared with control group. HTR was increased significantly in LU7 group when compared with conool group. In the liver function, the significance was not showed in AST and ALT, ALP was decreased significantly in LU7+LR5 group when compared with control group. Conclusions: LLLAT at LU7 and LR5 maybe can manage hyperlipidemia by controlling body weight, food intake, food efficiency ratio and lipid metabolism.

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Purification and Characterization of Two Alkaline Proteases Produced by Pseudomonas sp. BK7

  • 이은구;박은희;현형환
    • Journal of Microbiology and Biotechnology
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    • v.10 no.5
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    • pp.667-667
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    • 2000
  • Pseudomonas sp. BK7, an alkalophile, displayed the highest growth and protease activity when grown in a fermenter which was controlled at a pH level of 9.0, and the enzyme production was significantly enganced by the increase of agitation speed. Two formas of alkaline proteases (BK7-1 and BK7-2) were fractionated and purified to near homogeneity. Protease BK7-1 was purified through CM-Sepharose CL-6B and Sephadex G-75 column chromatographies, and Protease BK7-2 was purified through CM-Sepharose CL-6B and Sephadex G-75 column chromatographies, and Protease BK7-2 was purified through CM-Sepharose CL-6B, DEAE-Sepharose, and Sephadex G-75 column chromatographies. The molecular weights of proteases BK7-1 and BK7-2 determined by gel filtration chromatography were 20,700 and 40,800, respectively. The $K_m$ value, isoelectric point, and optimum pH of protease BK7-1 were 2.55 mg/ml, 11.0 and 11.0, respectively, whereas those of protease BK7-2 were 1.57 mg/ml, 7.2, and 10.0, respectively. Both protease were practically stable in the pH range of 5-11. The optimum temperatures for the activities of both protease BK7-1 and BK7-2 were 50℃ and 45℃, respectively. About 56% of the original protease BK7-2 activity remained after being treated at 50℃ for 30 min but protease BK7-1 was rapidly inactivated at above 25℃. Both proteases were completely inhibited by phenylmethane sulfonyl fluoride, a serine protease inhibitor. Protease BK7-2 was stable against EDTA, EGTA, STP, and detergents such as SDS and LAS, whereas protease BK7-1 was found to be unstable.

C7 Fracture as a Complication of C7 Dome-Like Laminectomy : Impact on Clinical and Radiological Outcomes and Evaluation of the Risk Factors

  • Yang, Seung Heon;Kim, Chi Heon;Lee, Chang Hyun;Ko, Young San;Won, Youngil;Chung, Chun Kee
    • Journal of Korean Neurosurgical Society
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    • v.64 no.4
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    • pp.575-584
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    • 2021
  • Objective : Cervical expansive laminoplasty is an effective surgical method to address multilevel cervical spinal stenosis. During surgery, the spinous processes of C2 and C7 are usually preserved to keep the insertion points of the cervical musculature and nuchal ligament intact. In this regard, dome-like laminectomy (undercutting of C7 lamina) instead of laminoplasty is performed on C7 in selected cases. However, resection of the lamina can weaken the C7 lamina, and stress fractures may occur, but this complication has not been characterized in the literature. The objective of the present study was to investigate the incidence and risk factors for C7 laminar fracture after C7 dome-like laminectomy and its impact on clinical and radiological outcomes. Methods : Patients who underwent cervical open-door laminoplasty combined with C7 dome-like laminectomy (n=123) were classified according to the presence of C7 laminar fracture. Clinical parameters (neck/arm pain score and neck disability index) and radiologic parameters (C2-7 angle, C2-7 sagittal vertical axis, and C7-T1 angle) were compared between the groups preoperatively and at postoperatively at 3, 6, 12, and 24 months. Risk factors for complications were evaluated, and a formula estimating C7 fracture risk was suggested. Results : C7 lamina fracture occurred in 32/123 (26%) patients and occurred at the bilateral isthmus in 29 patients and at the spinolaminar junction in three patients. All fractures appeared on X-ray within 3 months postoperatively, but patients did not present any neurological deterioration. The fracture spontaneously healed in 27/32 (84%) patients at 1 year and in 29/32 (91%) at 2 years. During follow-up, clinical outcomes were not significantly different between the groups. However, patients with C7 fractures showed a more lordotic C2-7 angle and kyphotic C7-T1 angle than patients without C7 fractures. C7 fracture was significantly associated with the extent of bone removal. By incorporating significant factors, the probability of C7 laminar fracture could be assessed with the formula 'Risk score = 1.08 × depth (%) + 1.03 × length (%, of the posterior height of C7 vertebral body)', and a cut-off value of 167.9% demonstrated a sensitivity of 90.3% and a specificity of 65.1% (area under the curve, 0.81). Conclusion : C7 laminar fracture can occur after C7 dome-like laminectomy when a substantial amount of lamina is resected. Although C7 fractures may not cause deleterious clinical outcomes, they can lead to an unharmonized cervical curvature. The chance of C7 fracture should be discussed in the shared decision-making process.

Studies on Mammalian Homolog and Flanking Sequence of Mouse MT Transposon-like Element, Clone MTi7(MTi7) (생쥐의 MT Transposon-like Element, Clone MTi7(MTi7) 유전자의 포유류 Homolog 및 Flanking Sequence에 대한 연구)

  • Kim Young-Hoon;Ko Minsu;Woo Dae-Gyun;Choi Donchan;Lee Kyung-Ah
    • Development and Reproduction
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    • v.7 no.2
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    • pp.119-126
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    • 2003
  • In the previous study, we obtained list of differentially expressed genes between postnatal day 1 and day 5 mouse ovaries using suppression subtractive hybridization(SSH) and found that MT Oansposon-like element, clone MTi7(MTi7) was one of the highly expressed genes in the day 5 mouse ovary(Park et at., 2002). Results of in situ hybridization and RNA interference revealed that the expression of MTi7 is oocyte-specific in the ovary and may be involved in the regulation of oocyte maturation(Park et at., 2003). At present, MTi7 sequence has been known only in the mouse. Therefore, the present study was accomplished 1) to identify MTi7 sequence in the other mammalian species, such as bovine, porcine, rat, and human, and 2) to evaluate the flanking sequence of the mouse MTi7 since it has transposon characteristics. Using ovarian cDNAs derived from low different species, we cloned and identified new MTi7 sequence showing a high degree of sequence homology with the mouse MTi7(87∼98%). By using inverse PCR, we found that the mouse MTi7 may intercalated the beta-carotene 15, 15'-monooxygenase(Bcdo) gene and/or serine protease inhibitor, Kunitz Dpe I(Spint 1) gene. By finding the MTi7 sequences in the other mammalian species and the flanking gene of the MTi7 in mouse, it is expected to reveal the role(s) of MTi7 in the oogenesis as well as folliculogenesis in the near future.

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Effect of DHEA Administration before, during and after Dexamethasone Treatment on Body Weight and Mass of TypeI,II Muscles in Rats (DHEA의 투여 시기가 Dexamethasone 치료 쥐의 체중과 TypeI,II 근육무게에 미치는 영향)

  • 최명애;신기수;안경주;이은주
    • Journal of Korean Academy of Nursing
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    • v.32 no.5
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    • pp.727-734
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    • 2002
  • This study was to determine the effect of DHEA administration before, during, and after dexamethasone treatment on body weight and TypeI,II muscle weight of rat receiving dexamethasone treatment. Method: Wistar rats were divided into 6 groups: control(C), dexamethasone(D), DHEA administration for 3days after dexamethasone treatment for 7days(7D+3DH), dexamethasone treatment for 7days after DHEA administration for 3days(3DH+7D), DHEA administration during dexamethasone treatment for 4days after dexamethasone treatment for 3days(3D+4DDH), DHEA administration during dexamethasone treatment for 7days(7DDH). Dexamethasone was injected by subcutaneously daily at a dose of 5mg/kg. DHEA was orally administered daily at a dose of 5mg/kg for 7 days. Soleus(TypeI) muscle, and both plantaris and gastro- cnemius(TypeII) muscles were dissected on the 7th day of experiment. Result: Body weight of both 3DH+7D group and 3D+4DDH group increased significantly compared with that of 7D group. Body weight of 7D+3DH group decreased significantly compared with that of 7D group, 7DDH group, 3DH+7D group and 3D+4DDH group. Muscle weight of both plantaris and gastro- cnemius tended to decrease compared with that of 7D group. Muscle weight of 7DDH group, 3D+4DDH group and 3DH+7D group increased significantly compared with that of 7D+3DH group. Muscle weight of gastrocnemius of both 3DH+7D group and 3D+4DDH group increased significantly compared with that of 7D group. Conclusion: Based on these results, it can be suggested that DHEA administration before and during dexamethasone treatment can increase both body weight and mass of atrophied TypeII muscle induced by dexa- methasone treatment.