• 제목/요약/키워드: PET inhibitor

검색결과 14건 처리시간 0.029초

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

  • 권혜경;권석윤;이행순;윤의수;김진석;조광연;곽상수
    • 식물조직배양학회지
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    • 제26권3호
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    • pp.183-187
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    • 1999
  • 식물배양세포를 이용하여 효율적인 제초제 검정시스템을 확립하기 위하여 다른 작용기작을 가진 몇가지 제초제를 사용하여 담배 PM세포에 대한 반응성을 세포생장과 배지의 이온전도도를 측정하여 조사하였다. 담배 PM세포는 0.7 mg/L 2,4-D, 0.3 mg/L kinetin, 30 g/L sucrose를 함유한 MS배지에서 $25^{\circ}C$, 광조건에서 현탁배양 (100rpm)하였다 계대배양시 약제를 처리한 후 12일째의 세포생장과 배지의 이온전도도를 측정한 결과, 이온전도도 측정결과는 세포생장의 것과 높은 상관관계를 나타내었다. 담배 PM세포에 대한 각 화합물의 반응성은 약제의 작용기작을 반영하면서 다양하였다. PET 저해화합물인 atrazine은 담배 PM세포에 가장 강한 활성을 나타내었다 (IC50, 1 $\mu$M). GS 저해제인 glufosinate, 세포분열저해제인 butachlor, carotenoid 생합성저해제인 fluridone은 농도에 비례하여 저해활성을 나타내었다. 그러나 오옥신활성을 지닌다고 알려진 quinclorac은 억제활성을 나타내지 않았다. 따라서 배지의 이온 전도도 측정은 간편하면서 재현성이 좋은 신규 제초제의 탐색방법으로 유용할 것으로 시사된다.

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Development of radiolabelled histone deacetylase inhibitors for PET imaging study

  • Hee-Kwon Kim
    • 대한방사성의약품학회지
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    • 제6권2호
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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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    • 제29권1호
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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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    • 제34권11호
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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.

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

  • 김혜림;송화순
    • 한국의류학회지
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    • 제32권6호
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    • pp.911-917
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    • 2008
  • 본 연구는 폴리에스터 직물에 리파제 처리시 첨가제에 따른 수분특성 변화를 검토하였다. 활성제(염화칼슘) 및 비이온 계면활성제(Triton X-100) 첨가가 수분율, 접촉각, 흡수속도, 표면형태변화에 미치는 영향을 비교, 분석하였다. 연구결과, 리파제 처리된 폴리에스터 직물의 수분율은 비이온 계면활성제인 Triton X-100 첨가시 현저히 감소하는 것으로 나타났다. 그러나 리파제의 활성제로 알려진 염화칼슘 첨가 시 폴리에스터 직물의 수분특성은 다소 증가하는 것으로 나타났다. 특히 리파제 처리 시 염화칼슘이 10mM이상 첨가된 경우 폴리에스터 직물의 수분특성이 증가되었다. 리파제 처리된 폴리에스터 직물의 표면관찰 결과, 섬유표면에 생성된 보이드와 크랙이 폴리에스터 직물의 수분특성 증가에 영향을 미치는 것으로 확인되었다. 이상의 결과를 통해, 폴리에스터 직물에 리파제 처리시 Triton X-100은 리파제의 활성을 저해하고, 염화칼슘은 리파제의 활성을 다소 증가시키는 것을 확인하였다.

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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    • 제25권1호
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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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    • 제21권4호
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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.

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

  • 김학로;김범석;박영식;김미소;김태민;김동완;허대석
    • The Korean Journal of Medicine
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    • 제93권6호
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    • pp.571-574
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    • 2018
  • 니볼루맙을 사용하는 도중 폐렴이 발생할 수 있고, 폐렴이 의심되면 치료하기 이전에 바이러스를 포함한 감염 여부와 림프관성 암의 진행 상태 및 울혈성 심장 기능 상실 여부 등의 감별이 필요하며 폐렴의 등급과 중증도를 평가하여 스테로이드를 경험적으로 쓰는 것이 중요하다. 본 증례에서는 감염을 배제하기 위하여 기관지 폐포세척을 시행한 후 폐포자충 폐렴이 진단된 사례로 드물기는 하지만 페포자충 폐렴의 감별이 필요함을 보여주어 증례로 보고하는 바이다.

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

  • 박기형;김성완;신동진;박현미;이영배;성영희
    • 생물정신의학
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    • 제15권1호
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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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    • 제31권6호
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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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