• Title/Summary/Keyword: PtpA

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Screening of Marine Microbial Extracts for Tyrosine Phosphatase 1B Inhibitors

  • Sohn, Jae-Hak;Park, Sun Jung;Seo, Changon;Chun, Bokyung;Oh, Hyuncheol
    • Journal of Marine Bioscience and Biotechnology
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    • v.2 no.4
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    • pp.230-233
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    • 2007
  • Protein tyrosine phosphatase 1B (PTP1B) acts as a negative regulator of insulin signaling, and selective inhibition of PTP1B has served as a potential drug target for the treatment of type 2 diabetes. As part of our searching for PTP1B inhibitors from natural products, the extracts of marine microorganisms were screened for the inhibitory effects on the activity of protein tyrosine phosphatase 1B (PTP1B). Among the tested 304 extracts, 29 extracts exhibited inhibition rate ranging 40.1 - 83.6 % against PTP1B at the concentration level of $30{\mu}g/mL$.

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Screening of the Inhibitory Activity of Medicinal Plants against Protein Tyrosine Phosphatase 1B (생약의 Protein Tyrosine Phosphatase 1B (PTP1B) 저해활성 검색)

  • Hong, Jung-Hyun;Lee, Myung-Sun;Bae, Eun-Young;Kim, Young-Ho;Oh, Hyun-Cheol;Oh, Won-Keun;Kim, Bo-Yeon;Ahn, Jong-Seog
    • Korean Journal of Pharmacognosy
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    • v.35 no.1 s.136
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    • pp.16-21
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    • 2004
  • Protein tyrosine phosphatase 1B(PTP1B) is thought to be a negative regulator in insulin signal-transduction pathway. Insulin-resistance by the activation of PTP1B is a hallmark of both type 2 diabetes and obesity. Thus, the compounds inhibiting PTP1B can improve insulin resistance and can be effective in treating type 2 diabetes and obesity. The methanol extracts of 160 herbal medicines were screened for the inhibitory activity against PTP1B. Among the tested extracts, methanol extracts of Amsonia elliptica, Areca catechu, Benincasa hispida, Morus alba, Salvia miltiorrhiza, Siegesbeckia orientalis, and Trichosanthes kirilowii showed relatively strong inhibitory activity against PTP1B.

Alignment effects of the nematic liquid crystal on polythiophene Surfaces (Polythiophene막을 이용한 네마틱액정의 배향효과)

  • 서대식
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 1997.04a
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    • pp.127-129
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    • 1997
  • The high pretilt angles in nematic liquid crystals (NLCs) have been generated on robbed polythiophene (PTP) surfaces with alkyl chain lengths. The pretilt angle of the NLC was observed on unidirectionally rubbed PTP surfaces with alkyl chains with more than 9 carbon atoms. We obtained the Pretilt angle of 15~40$^{\circ}$ on rubbed PTP surfaces with 10 carbon atoms in the a1ky1 chain. Also, the pretilt angles of 65~80$^{\circ}$ of NLC were obtained on rubbed PTP surfaces with 11 and 12 carbon atoms in the alkyl chain. We suggest that this high pretilt angle generation in NLC is due to the surface-excluded volume effect by the alkyl chain lengths between. the LCs and the PTP surfaces. Finally, we conclude the odd-even effect on rubbed PTP surfaces is clearly contributed to the pretilt angle generation.

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The EphA8 Receptor Phosphorylates and Activates Low Molecular Weight Phosphotyrosine Protein Phosphatase in Vitro

  • Park, Soo-Chul
    • BMB Reports
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    • v.36 no.3
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    • pp.288-293
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    • 2003
  • Low molecular weight phosphotyrosine protein phosphatase (LMW-PTP) has been implicated in modulating the EphB1-mediated signaling pathway. In this study, we demonstrated that the EphA8 receptor phosphorylates LMW-PTP in vitro. In addition, we discovered that mixing these two proteins leads to EphA8 dephosphorylation in the absence of phosphatase inhibitors. Finally, we demonstrated that LMW-PTP, modified by the EphA8 autokinase activity, possesses enhanced catalytic activity in vitro. These results suggest that LMW-PTP may also participate in a feedback-control mechanism of the EphA8 receptor autokinase activity in vivo.

Protein Tyrosine Phosphatase Profiling Analysis of HIB-1B Cells during Brown Adipogenesis

  • Choi, Hye-Ryung;Kim, Won Kon;Kim, Eun Young;Jung, Hyeyun;Kim, Jeong-Hoon;Han, Baek-Soo;You, Kwan-Hee;Lee, Sang Chul;Bae, Kwang-Hee
    • Journal of Microbiology and Biotechnology
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    • v.22 no.7
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    • pp.1029-1033
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    • 2012
  • A number of evidence have been accumulated that the regulation of reversible tyrosine phosphorylation, which can be regulated by the combinatorial activity of protein tyrosine kinases (PTKs) and protein tyrosine phosphatases (PTPs), plays crucial roles in various biological processes including differentiation. There are a total of 107 PTP genes in the human genome, collectively referred to as the "PTPome." In this study, we performed PTP profiling analysis of the HIB-1B cell line, a brown preadipocyte cell line, during brown adipogenesis. Through RT-PCR and real-time PCR, several PTPs showing differential expression pattern during brown adipogenesis were identified. In the case of PTP-RE, it was shown to decrease significantly until 4 days after brown adipogenic differentiation, followed by a dramatic increase at 6 days. The overexpression of PTP-RE led to decreased brown adipogenic differentiation via reducing the tyrosine phosphorylation of the insulin receptor, indicating that PTP-RE functions as a negative regulator at the early stage of brown adipogenesis.

Inhibition of protein tyrosine phosphatase non-receptor type 2 by PTP inhibitor XIX: Its role as a multiphosphatase inhibitor

  • Le, Hien Thi Thu;Cho, Young-Chang;Cho, Sayeon
    • BMB Reports
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    • v.50 no.6
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    • pp.329-334
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    • 2017
  • Protein tyrosine phosphatases (PTPs) play crucial roles in signal transduction and their functional alteration has been detected in many diseases. PTP inhibitors have been developed as therapeutic drugs for diseases that are related to the activity of PTPs. In this study, PTP inhibitor XIX, an inhibitor of CD45 and PTEN, was investigated whether it inhibits other PTPs. Protein tyrosine phosphatase non-receptor type 2 (PTPN2) was selectively inhibited by the inhibitor in a competitive manner. Drug affinity responsive target stability (DARTS) analysis showed that the inhibitor induces conformational changes in PTPN2. Phosphorylation levels of signal transducer and activator of transcription 3 (STAT3) at Tyr-705, a crucial site for STAT3 activation and target site of PTPN2, decreased upon exposure to the inhibitor. Our results suggest that PTP inhibitor XIX might be considered as an effective regulator of PTPN2 for treating diseases related to PTPN2.

Neuroprotective Effects of Protein Tyrosine Phosphatase 1B Inhibition against ER Stress-Induced Toxicity

  • Jeon, Yu-Mi;Lee, Shinrye;Kim, Seyeon;Kwon, Younghwi;Kim, Kiyoung;Chung, Chang Geon;Lee, Seongsoo;Lee, Sung Bae;Kim, Hyung-Jun
    • Molecules and Cells
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    • v.40 no.4
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    • pp.280-290
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    • 2017
  • Several lines of evidence suggest that endoplasmic reticulum (ER) stress plays a critical role in the pathogenesis of many neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, and amyotrophic lateral sclerosis. Protein tyrosine phosphatase 1B (PTP1B) is known to regulate the ER stress signaling pathway, but its role in neuronal systems in terms of ER stress remains largely unknown. Here, we showed that rotenone-induced toxicity in human neuroblastoma cell lines and mouse primary cortical neurons was ameliorated by PTP1B inhibition. Moreover, the increase in the level of ER stress markers ($eIF2{\alpha}$ phosphorylation and PERK phosphorylation) induced by rotenone treatment was obviously suppressed by concomitant PTP1B inhibition. However, the rotenone-induced production of reactive oxygen species (ROS) was not affected by PTP1B inhibition, suggesting that the neuroprotective effect of the PTP1B inhibitor is not associated with ROS production. Moreover, we found that MG132-induced toxicity involving proteasome inhibition was also ameliorated by PTP1B inhibition in a human neuroblastoma cell line and mouse primary cortical neurons. Consistently, downregulation of the PTP1B homologue gene in Drosophila mitigated rotenone- and MG132-induced toxicity. Taken together, these findings indicate that PTP1B inhibition may represent a novel therapeutic approach for ER stress-mediated neurodegenerative diseases.

Protein Tyrosine Phosphatase 1B Activity of Quercetin from Houttuynia Cordata (어성초로부터 분리된 Quercetin의 Protein Tyrosine Phosphatase 1B 활성)

  • Choi, Hwa-Jung;Bae, Eun-Young;No, Yong-Ju;Baek, Seung-Hwa
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.22 no.6
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    • pp.1532-1536
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    • 2008
  • Quercetin which isolated form the roots of Houttuynia cordata. was determined on the basis of IR, ID and 2D NMR specta by direct comparison with authentic compounds. Protein tyrosine phophatase 1B (PTP1B) is thought to be a negative regulator in insulin signal-transduction pathway. Insulin-resistance by the activation of PTP1B is a hallmark of both type 2 diabetes and obesity. Thus, the compound inhibiting PTP1B can improve insulin resistance and can be effective in treating type 2 diabetes and obesity. Quercetin which measured the inhibitory activity against PTP1B was 92.1% inhibition in the 30 ${\mu}g$/mL, 83.4% inhibition in the 6 ${\mu}g$/mL and 76.5% inhibition in the 3 ${\mu}g$/mL. These results suggest that quercetin retains a potential PTP1B activity.

A Survey of IEEE 1588 Time Synchronization Performance (IEEE 1588 시간 동기화 성능에 대한 조사)

  • Jahja, Rico Hartono;Jeon, Seong-Yong;Shin, Seok-Joo
    • The Journal of the Korea institute of electronic communication sciences
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    • v.10 no.2
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    • pp.165-176
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    • 2015
  • Clock or time synchronization protocol is one of the crucial factors that could determine the quality of the communication. With the rapid development of the network technology, more robust clock synchronization algorithm is required. IEEE 1588 is one of the possible solutions for a robust clock synchronization algorithm; however, there are still some challenges that need to be concerned in IEEE 1588 in term of reducing and stabilizing the PDV value. This survey paper shows several solutions that could improve the performance of IEEE 1588, including modifying the PTP message transmission, optimizing PTP method, filtering techniques, and using the hardware timestamp instead of application layer timestamp, and so on. Despite the improvement that is created with these techniques, the clock synchronization algorithm is still an open issue in the network communication.

Molecular Docking Study of Anti-diabetic Xanthones from Garcinia Xanthochymus

  • Babu, Sathya
    • Journal of Integrative Natural Science
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    • v.10 no.3
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    • pp.137-140
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    • 2017
  • Diabetes mellitus has become a major growing public health problem worldwide. More than 90% of all diabetes cases are classified as type 2 diabetes (T2D), which is also known as non-insulin dependent diabetes. Protein tyrosine phosphatase 1B (PTP1B) plays an important role in the negative regulation of insulin signal transduction pathway and has emerged as novel therapeutic strategy for the treatment of type 2 diabetes. PTP1B inhibitors enhance the sensibility of insulin receptor (IR) and have favorable curing effect for insulin resistance-related diseases. Recently twelve anti-diabetic xanthones were isolated from the bark of Garcinia xanthochymus. Hence, in the present study, molecular docking was carried out for these twelve xanthones. The objective of this work is to study the interaction of the newly isolated xanthones with PTP1B. The docking results showed that xanthones have good interactions and has better docking score with PTP1B and suggest LYS120 and ASP181 are the important residues involved in interaction between PTP1B enzyme and the xanthones.