• Title/Summary/Keyword: PET inhibitor

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Responses of Tobacco Photomixotrophic Cultured Cells to Various Herbicides (다양한 제초제에 대한 담배 Photomixotrophic 배양세포의 반응)

  • 권혜경;권석윤;이행순;윤의수;김진석;조광연;곽상수
    • Korean Journal of Plant Tissue Culture
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    • v.26 no.3
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    • pp.183-187
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    • 1999
  • To establish an efficient screening system for new herbicides using plant cultured cells, responses of tobacco photomixotrophic cultured (PH) cells to various herbicides with different modes of action were surveyed by measuring the cell growth and ion conductivity in medium. The cells were cultured in Murashige and Skoog (MS) medium containing 0.7mg/L 2,4-D, 0.3mg/L kinetin and 30 g/L sucrose at $25^{\circ}C$ in the light (100 rpm). Chemicals were treated to suspension cultures of tobacco PH cells at the time of subculture. The cell growth and ion conductivity in the medium were investigated on 12 days after chemical treatment. The ion conductivity assay gave well correlated results to the cell growth inhibition data. The responses of tobacco PM cells were dependent on the modes of action of chemicals tested. Atrazine, an inhibitor of photosynthetic electron transport (PET), strongly inhibited both the cell membrane and cell growth ($IC_{50}$/, about 1 $\mu$M). Butachlor (an inhibitor of cell division), glufosinate (an inhibitor of amino acid biosynthesis), and fluridone (an inhibitor of carotenoid biosynthesis) showed a dose-dependent inhibition. However, Quinclorac, a herbicide with an auxin activity, did not affect the cell growth and ion leakage. These results suggested that tobacco PM cells is suitable materials for the simple screening of new herbicides such as PET, amino acid biosynthesis, ceil division inhibitors by measuring the cell growth and ion conductivity.

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Development of radiolabelled histone deacetylase inhibitors for PET imaging study

  • Hee-Kwon Kim
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.6 no.2
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    • pp.165-170
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    • 2020
  • Histone Deacetylases (HDACs) are enzymes that have control gene expression regulation and cell state. In additions, inhibitions of HDACs are associated with growth arrest, differentiation, or apoptosis of tumor cell. Thus HDAC inhibition is one of the interesting biological targets. A variety of HDAC inhibitors has been developed by many scientists, and some of chemical structures related with HDAC inhibitors were modified to give radiolabeled HDAC inhibitors for positron emission tomography (PET) study. In this highlight review, the development of radiolabeled HDAC inhibitors for PET study are described.

Identification of Phosphatidylcholine-Phospholipase D and Activation Mechanisms in Rabbit Kidney Proximal Tubule Cells

  • Chung, Jin-Ho;Chae, Joo-Byung;Chung, Sung-Hyun
    • BMB Reports
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    • v.29 no.1
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    • pp.11-16
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    • 1996
  • The present study showed that receptor-mediated activation of rabbit kidney proximal tubule cells by angiotensin II, the $Ca^{2+}$ ionophore A23187, or the protein kinase C activator phorbol myristate acetate (PMA) all stimulated phospholipase D (PLD). This was demonstrated by the increased formation of phosphatidic acid, and in the presence of 0.5% ethanol, phosphatidylethanol (PEt) accumulation. Angiotensin II leads to a rapid increase in phosphatidic acid and diacylglycerol, and phosphatidic acid formation preceeded the formation of diacylglycerol. This result suggests that some phosphatidic acid seems to be formed directly from phosphatidylcholine hydrolyzed by Pill. On the other hand, EGTA substantially attenuated angiotensin II and A23187-induced PEt formation, and when the cells were pretreated with verapamil angiotensin II-induced Pill activation was completely abolished. These results provide the evidence that calcium ion influx is essential for the agonist-induced Pill activation. In addition, staurosporine, an inhibitor of protein kinase C, strongly inhibited PMA-induced PEt formation, but was ineffective on angiotensin II-induced PEt accumulation. $GTP{\gamma}S$ also stimulates PEt formation in digitonin-permeabilized cells, but pretreatment of the cells with pertussis toxin failed to suppress angiotensin II-induced PEt formation. From these results, we conclude that in the rabbit kidney proximal tubule cells the mechanisms of angiotensin II- and PMA-induced Pill activation are different from each other and mediated via a pertussis toxin-insensitive trimeric G protein.

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Folate Receptor-Specific Positron Emission Tomography Imaging with Folic Acid-Conjugated Tissue Inhibitor of Metalloproteinase-2

  • Kim, Sung-Min;Choi, Naeun;Hwang, Seungkyun;Yim, Min Su;Lee, Jung-Sik;Lee, Sang-Mok;Cho, Gyunggoo;Ryu, Eun Kyoung
    • Bulletin of the Korean Chemical Society
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    • v.34 no.11
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    • pp.3243-3248
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    • 2013
  • The tissue inhibitor of metalloproteinase-2 (TIMP-2) inhibits matrix metalloproteinases activity and modulates cellular proliferation and apoptosis. The human serum albumin-TIMP-2 with folic acid conjugate (termed HT2-folate) was synthesized to promote uptake through folate receptors (FRs), and a corresponding radio-labeled compound was prepared for tumor diagnosis by positron emission tomography (PET). $^{68}Ga$-NOTA-HT2-folate was synthesized from $^{68}Ga$ and the NOTA chelator with HT2-folate. The fusion protein was identified using MALDI-TOF mass spectrometry. The radioligand was prepared with a high radiochemical yield. Cell-surface association of $^{68}Ga$-NOTA-HT2-folate significantly increased over time in FR-positive tumor cells. In animal PET and biodistribution studies, tumor uptake was very high as early as 1 h after radioligand injection. Folate conjugation enhanced the selective receptor-targeting efficacy of HT2 in FRexpressing tumors, and its radioligand will be useful as an in vitro tool and for in vivo tumor diagnosis by PET imaging.

Effects of Triton X-100 and Calcium Chloride on the Porcine Pancreas Lipase Treatment of PET Fabrics (폴리에스터 직물의 리파제 처리시 Triton X-100 및 염화칼슘의 영향)

  • Kim, Hye-Rim;Song, Wha-Soon
    • Journal of the Korean Society of Clothing and Textiles
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    • v.32 no.6
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    • pp.911-917
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    • 2008
  • In this study, we reported the effect of porcine pancreas lipase treatment in the presence of a calcium chloride and Triton X-100 on moisture regain and wettability of PET fabrics. The moisture regain of PET fabrics in the presence of 0.5% surfactant showed a 1.5-fold decrease, compared to the absence of it. Triton X-100 acted as an inhibitor to porcine pancreas lipase hydrolytic activity. The moisture regain and wettability of porcine pancreas lipase treated PET fabrics improved when more than 10mM of calcium chloride was added to the treatment solution. Porcine pancreas lipase treatment caused voids and cracks on PET fabrics.

Imaging Evaluation of Peritoneal Metastasis: Current and Promising Techniques

  • Chen Fu;Bangxing Zhang;Tiankang Guo;Junliang Li
    • Korean Journal of Radiology
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    • v.25 no.1
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    • pp.86-102
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    • 2024
  • Early diagnosis, accurate assessment, and localization of peritoneal metastasis (PM) are essential for the selection of appropriate treatments and surgical guidance. However, available imaging modalities (computed tomography [CT], conventional magnetic resonance imaging [MRI], and 18fluorodeoxyglucose positron emission tomography [PET]/CT) have limitations. The advent of new imaging techniques and novel molecular imaging agents have revealed molecular processes in the tumor microenvironment as an application for the early diagnosis and assessment of PM as well as real-time guided surgical resection, which has changed clinical management. In contrast to clinical imaging, which is purely qualitative and subjective for interpreting macroscopic structures, radiomics and artificial intelligence (AI) capitalize on high-dimensional numerical data from images that may reflect tumor pathophysiology. A predictive model can be used to predict the occurrence, recurrence, and prognosis of PM, thereby avoiding unnecessary exploratory surgeries. This review summarizes the role and status of different imaging techniques, especially new imaging strategies such as spectral photon-counting CT, fibroblast activation protein inhibitor (FAPI) PET/CT, near-infrared fluorescence imaging, and PET/MRI, for early diagnosis, assessment of surgical indications, and recurrence monitoring in patients with PM. The clinical applications, limitations, and solutions for fluorescence imaging, radiomics, and AI are also discussed.

Silica Induced Phospholipase D (PLD) Activation in Rat2 Fibroblasts

  • Ahn Eun-Kyung;Lim Oh-Kyung;Nam Hae-Yun;Kim Hyung Jung;Chung Namhyun;Bae Gwi-Nam;Lim Young
    • Toxicological Research
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    • v.21 no.4
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    • pp.291-295
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    • 2005
  • To define the effect of silica on the stimulator of signaling pathway, we studied the phospholipase D (PLD) activity in the Rat2 fibroblasts. Silica stimulated the accumulation of labeled $[^3H]$ phosphatidylethanol$([^3H]\;PEt)$ in a time- and concentration-dependent manner. This Silicainduced PLD activity was partially attenuated by the pretreatment with U73122 (phospholipase C inhibitor), genistein (protein tyrosine kinase inhibitor), PD 98056 (MEK inhibitor) and mepacrine (phospholipase $A_2$ inhibitor). But, sphingosine (protein kinase C inhibitor) and DPI (NADPH reductase inhibitor) had not effect the PLD activity. Silica also increased the PLD activity about four fold, which imply that the PLD activity is more influenced by the mobilization of PLD than other signaling mediators. The PLD activity also partially inhibited calcium chelator EGTA or/and BAPTA/AM compared to silica. Finally, we concluded that a silica-stimulated phospholipase D activity is present in the Rat2 fibroblasts and is modulated by combination of various signaling mediators.

Pneumocystis Pneumonia Developing during Treatment of Recurrent Renal Cell Cancer with Nivolumab (니볼루맙 치료 도중 발생한 폐포자충 폐렴 1예)

  • Kim, Hak Ro;Keam, Bhumsuk;Park, Young Sik;Kim, Miso;Kim, Tae Min;Kim, Dong-Wan;Heo, Dae Seog
    • The Korean Journal of Medicine
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    • v.93 no.6
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    • pp.571-574
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    • 2018
  • Nivolumab is an immune checkpoint inhibitor approved for the treatment of metastatic cancers. Here, we report the case of a 65-year-old male with recurrent renal cell carcinoma. After six cycles of nivolumab treatment, positron emission tomography/computed tomography (PET/CT) was performed to evaluate the response. PET/CT revealed diffuse ground glass opacities in both lungs. He developed a cough, sputum, chills, and a febrile sense. After bronchoscopic bronchoalveolar lavage, pneumocystis pneumonia was finally diagnosed.

A case of Posterior Cortical Atrophy Presenting with Features of Atypical Dementia (비전형적 치매양상을 보이는 후부대뇌피질위축 증례보고)

  • Park, Kee Hyung;Kim, Sung-Wan;Shin, Dong-Jin;Park, Hyun-Mi;Lee, Yeong-Bae;Seung, Young-Hee
    • Korean Journal of Biological Psychiatry
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    • v.15 no.1
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    • pp.46-53
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    • 2008
  • Posterior cortical atrophy(PCA) is a presenile dementia that presents primarily with signs and symptoms of cortical visual dysfunction, while memory is relatively preserved until the late stage of the disease. We report a patient with PCA, confirmed by brain magnetic resonance imaging (MRI) and $F^{18}$-fluorodeoxyglucose positron emission tomography(FDG PET). A 58-year-old right-handed woman presented initially with visual dimness and difficulty finding things around her. She had partial Balint's syndrome, partial Gerstmann syndrome, and idiomotor apraxia. She also had a mild memory disturbance, but preserved insight of her disease. Neuropsychological evaluation showed decreased parietal and left temporal functions bilaterally. Brain MRI and $F^{18}$-FDG PET revealed typical bilateral occipitoparietal atrophy and hypometabolism, which were slightly worse on the right side. Cholinesterase inhibitor administration for 6 months improved the memory impairment slightly, but not the cortical visual dysfunction. This is a typical case of PCA, confirmed by neurologic signs and imaging findings.

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Participation of SRE4, an URE1 Enhancer Core Sequence, in the Sterol-Mediated Transcriptional Upregulation of the Human Apolipoprotein E Gene

  • Min, Jung-Hwa;Paik, Young-Ki
    • BMB Reports
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    • v.31 no.6
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    • pp.565-571
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    • 1998
  • The expression of the endogenous human apolipoprotein(apo)E gene was significantly induced when HepG2 cells were treated with exogenous 25-hydroxy-cholesterol. This sterol-mediated apoE gene upregulation appears to require the participation of a positive element for the apoE gene transcription (PET) ( -169/ -140), a core sequence of upstream regulatory element (URE)1 enhancer of the human apoE gene. This PET was renamed as sterol regulatory element (SRE)4 based on its new role as a sensor for the level of intracellular sterol. Furthermore, a gel mobility shift analysis showed that binding activity of the SRE4 binding protein (BP) obtained from HepG2 cells was induced by sterol treatment, while that from either MCF7 or BT20 cells remained unchanged. Binding activity of SRE4BP was also induced in mouse macrophage cells, J774A.1, by sterol treatment, but it was drastically reduced when cells were subjected to treatment of AY-9944, a potent inhibitor for sterol synthesis. However, binding activity of Spl, which is a co-binding protein to the SRE4 region, remained the same in either condition, suggesting that SRE4BP (formally known as PETBP) may be mainly responsible for the sterol-mediated regulation of the apoE gene expression. Deletion analysis of the core binding site of SRE4BP by gel mobility shift assays showed that the minimal sequence of the SRE4BP binding appears to reside between -157 and -140, confirming the identity of SRE4 with the previously determined core sequence of URE1.

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