• Title/Summary/Keyword: Pim-3

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1,3,4-Oxadiazole-2(3H)-thione as a New Scaffold for Pim Kinase Inhibitors

  • Lee, Ah Yeon;Hong, Victor Sukbong;Lee, Jinho
    • Quantitative Bio-Science
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    • v.37 no.2
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    • pp.113-124
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    • 2018
  • Pim kinases are important targets for cancer therapies because they are mainly responsible for cancer metastasis and overall therapeutic treatment responses. Because of their unusual structural feature in the hinge region of the ATP-binding site, new binding motifs have been discovered and used for the development of Pim kinases inhibitors. The results of a screening of 5-membered heteroaromatic compounds and the effects of structural modifications on the inhibition of Pim kinases' activities showed the potential scaffold for Pim inhibitors. 1,3,4-Oxadiazole-2(3H)-thione was found as a new scaffold for Pim kinase inhibitors.

Fabrication Studies for PZT Preform Using PIM (PIM을 이용한 PZT 프리폼의 제조에 대한 연구)

  • Shin, Ho-Yong;Kim, Jong-Ho;Jang, Jong-Soo;Im, Jong-In
    • The Journal of the Acoustical Society of Korea
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    • v.28 no.8
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    • pp.796-805
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    • 2009
  • In this paper, a fabrication process for PZT preform of 1-3 type piezo-composite were studied using powder injection molding (PIM). The viscosity and the Pressure-Volume-Temperature (PVT) characteristics of the fabricated PZT feedstock were analyzed. The filling patterns, pressure, temperature distributions, and forming defects of the preform were analyzed with 3D TIMON commercial packages during PIM process. Also the fabrication conditions and the delivery system of the preform were optimized during the entire PIM process. Based on the simulated results, the preform having uniform distributions of the PZT rod was fabricated with the PIM process.

Aberrant Expression of Pim-3 Promotes Proliferation and Migration of Ovarian Cancer Cells

  • Zhuang, Hao;Zhao, Man-Yin;Hei, Kai-Wen;Yang, Bai-Cai;Sun, Li;Du, Xue;Li, Yong-Mei
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.8
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    • pp.3325-3331
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    • 2015
  • Pim kinase-3(Pim-3), a member of serine/threonine protein kinases, has been implicated in multiple human cancers and involved in Myc-induced tumorigenesis. However, little is known regarding its expression and biological function in human ovarian cancer. In this study we showed that the clinical significance and biological functions of Pim-3 in ovarian cancer and found that higher Pim-3 mRNA level are detected in ovarian cancer tissues than those in normal ovarian tissues. There are significant correlations between higher Pim-3 expression levels with the FIGO stage, histopathological subtypes, and distant metastasis in ovarian cancer patients. Lentivirus-mediated gene overexpression of Pim-3 significantly promotes the proliferation and migration of SKOV3 cell lines. Furthermore, MACC1 and Pim-3 expression were significantly correlated in human ovarian cancer cells, and overexpression of Pim-3 in ovary cancer cells increased MACC1 mRNA and protein expression. The data indicate that Pim-3 acts as a putative oncogene in ovary cancer and could be a viable diagnostic and therapeutic target for ovarian cancer.

3,5-Bis(aminopyrimidinyl)indole Derivatives: Synthesis and Evaluation of Pim Kinase Inhibitory Activities

  • Lee, Jinho;More, Kunal N.;Yang, Seun-Ah;Hong, Victor S.
    • Bulletin of the Korean Chemical Society
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    • v.35 no.7
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    • pp.2123-2129
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    • 2014
  • Pim kinases are promising targets in the treatment of hematopoietic and solid cancers. Meridianin C was chosen as a starting point to discover novel pim kinase inhibitors. Using known pim kinase's structural information, aminopyrimidine was introduced to provide the hydrogen-bonding interactions with the conserved lysine residue in the ATP binding pocket of all three Pim kinases. Synthesized 3,5-bis(aminopyrimidinyl)indole derivatives showed pan-pim inhibitory activity. Aminoalkyl substituent was attached on the aminopyrimidine to further enhance the potency and physicochemical properties of compound. The research reveals a significative way of designing compounds with high potency and kinase selectivity for pan-pim kinases.

3D-QSAR Study on Imidazopyridazines Derivatives as Potent Pim-1 Kinase Inhibitors using Region-Focused CoMFA

  • Balasubramanian, Pavithra K.;Balupuri, Anand;Cho, Seung Joo
    • Journal of Integrative Natural Science
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    • v.10 no.2
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    • pp.95-104
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    • 2017
  • Proviral Integration site of Moloney (Pim) murine Leukemia virus kinases is a serine/threonine specific protein kinase. It is largely involved in cell survival and proliferation. Pim-1 phosphorylates multiple cellular substrates to inhibit apoptosis and promote cell cycle progression. Over expression of Pim-1 kinase is observed in a range of malignancies and various solid cancers. High level of Pim-1 expression is seen in myeloma, acute myeloid leukemia, prostate cancer and liver carcinomas. Hence, Pim-1 is considered as an interesting cancer target. In the present study, we have performed region-focused CoMFA study on a series of imidazopyridazine derivatives as Pim-1 kinase inhibitors. A statistically acceptable region-focused CoMFA model ($q^2=0.571$; ONC=3; $r^2=0.909$) was developed. The model was then validated using Bootsrapping and progressive sampling. The contour map highlighted the regions favorable to increase the activity. Bulky substitutions in $R^2$ position of the phenyl ring could increase the activity. Similarly, small negative substitution in the $R^1$ position of the Pyridine ring could increase the activity considerably. Our results will be useful to design novel Pim-1 kinase inhibitors of this series.

The current states of Powder Injection Molding Industry in Korea (국내 PIM 산업 현황)

  • 성환진;하태권;안상호
    • Proceedings of the Korean Powder Metallurgy Institute Conference
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    • 2002.04b
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    • pp.13-13
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    • 2002
  • 분말사출성형(PIM, Powder Injection Molding) 기술은 금속, 초경 또는 세라믹 등과 같은 소결 가능한 분말을 유기결합체와 혼압하고 이를 기존의 사출성형법을 이용하여 일정한 형상으로 성형한 다음 결합제 제거정 공정을 거처 최종 고온 소결함으로써 3차원의 복잡한 형상의 부품을 후가공 없이 정밀하게 대량 생산 할 수 있는 신분말 성형 기술이다.기계 , 항공,전자정보,반도체,의료 등의 제반 분야에서 산업 및 생활기기들이 초소형화, 초정밀, 및 고기능호 되어 감에 따라 부품 또한 일반 공정에서 제조하기 힘든 크기로 초소형화 되고, 형상이 더욱 복잡화 되며 우수한 기계적 특성 또한 요구되고 있다. 세계 분말 사출성 ; 산업은 이러한 산업적 요구에 맞춰 급격히 발전함과 동싱에 시장 또한 급격히 성장되고 있다. 그러나 국내의 PIM 산업은 88년 기술이 도입된 이후 세계 PIM 산업의 성장 속도를 따라가지 못하고 있는 실정이다. 이번 발표에서 국내의 PIM 산업 현황을 조사하여 국내 시장 규모. 성장 속도, 주요 PIM업체의 소개할 예정이다. 그리고 국내 PIM 산업의 상대적인 저성장 요인을 분석하고 향후 국내 PIM 업계의 발전 방안을 제시할 예정이다. 예정이다.

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Polypharmacy and Potentially Inappropriate Medication Use in Elderly Patients Hospitalized after Falls (낙상으로 입원한 노인의 다약제복용과 잠재적 부적절 약물 사용)

  • Kim, Ji-Yeon;Choi, Suyoung
    • Journal of Korean Biological Nursing Science
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    • v.24 no.3
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    • pp.161-170
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    • 2022
  • Purpose: The purpose of this study was to investigate polypharmacy and potentially inappropriate medication (PIM) use in elderly patients admitted to hospitals after falls. Methods: The study surveyed 283 patients 65 or older admitted January 1-December 31, 2016. Data were collected from electronic medical records, and medications administered immediately prior to admission were examined. PIM use for patients was investigated using the Beers criteria, and data were analyzed by Chi-square test and independent ttest. Results: The average age of participants was 79.42± 8.16, and the study included 226 women (79.9%) and 57 men (20.1%). The average number of self-administered medications daily was 4.94± 3.68, and 55.1% took five or more medications. PIM use was found in 107 patients (37.8%). There was a significant difference in polypharmacy according to age, and the proportion of medical aid beneficiaries and prevalence of cardiocerebrovascular, endocrine, and other chronic diseases were higher in the polypharmacy and PIM use patients than in the non-polypharmacy and non-PIM use patients. The number of chronic diseases and medications taken were significantly high among polypharmacy and PIM use patients. Conclusion: It is necessary to minimize polypharmacy and PIM use, and establish a system for systematically evaluating and managing medication use to prevent falls in the elderly.

TP-Sim: A Trace-driven Processing-in-Memory Simulator (TP-Sim: 트레이스 기반의 프로세싱 인 메모리 시뮬레이터)

  • Jeonggeun Kim
    • Journal of the Semiconductor & Display Technology
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    • v.22 no.3
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    • pp.78-83
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    • 2023
  • This paper proposes a lightweight trace-driven Processing-In-Memory (PIM) simulator, TP-Sim. TP-Sim is a General Purpose PIM (GP-PIM) simulator that evaluates various PIM system performance-related metrics. Based on instruction and memory traces extracted from the Intel Pin tool, TP-Sim can replay trace files for multiple models of PIM architectures to compare its performance. To verify the availability of TP-Sim, we estimated three different system configurations on the STREAM benchmark. Compared to the traditional Host CPU-only systems with conventional memory hierarchy, simple GP-PIM architecture achieved better performance; even the Host CPU has the same number of in-order cores. For further study, we also extend TP-Sim as a part of a heterogeneous system simulator that contains CPU, GPGPU, and PIM as its primary and co-processors.

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Wavelet Packet Based Watermarking Using PIM (PIM을 이용한 웨이블릿 패킷 기반 워터마킹)

  • 한수영;이두수
    • Journal of the Korea Society of Computer and Information
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    • v.8 no.3
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    • pp.61-65
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    • 2003
  • In this paper, a novel watermarking technique that based on wavelet packet transform using PIM is proposed for the copyright of the digital images. We divide wavelet packet coefficients into detailed blocks and calculate the complexity of each block using PIM. Because human is impervious to the change in the complex area, the embedding watermark to the selected coefficients using PIM enhances invisibility. From the experimental results, the proposed algorithm shows better invisibility and robustness performance in a general signal processing such as JPEG and SPIHT lossy compression, median filtering. Especially, it demonstrates better performance for the low bit-rate compression in the images that include many high frequency components.

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Assessment of Potentially Inappropriate Medication Use in Korean Elderly Patients with Chronic Heart Failure (국내 노인 심부전 환자에서의 잠재적으로 부적절한 약물사용 현황에 대한 연구)

  • Bae, Min Kyung;Lee, Iyn-Hyang;Yoon, Jeong-Hyun
    • Korean Journal of Clinical Pharmacy
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    • v.24 no.2
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    • pp.115-125
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    • 2014
  • Purpose: The purpose of the present study was to assess the incidence of the potentially inappropriate medication (PIM) use in Korean elderly patients with heart failure, and to evaluate factors that influence PIM use. Method: Korean National Health Insurance claims database between January 2009 and December 2009 was used. Using 2012 updated Beers criteria, PIM use in heart failure patients aged 65 years or older was examined. Result: The incidence of PIM use in elderly heart failure patients was higher than in overall elderly patients. Among the 12,759 elderly patients with heart failure, 46.2% of study subjects were prescribed PIM(s) at least once. The number of PIM per 10 medications that patients received per patient was 1.53. The most commonly used PIMs in elderly heart failure patients were benzodiazepines (30.9%), non-steroidal anti-inflammatory drugs (NSAIDs) including COX-2 inhibitors (16.3%), digoxin (9.9%), and spironolactone (9.0%). Women (odds ratio, 1.20; 95% CI, 1.17-1.24), medical aid (odds ratio, 1.11; 95% CI, 1.08-1.13), and long-term facilities (odds ratio, 2.69; 95% CI, 2.44-2.96) were revealed to be important factors associated with PIM use. In addition, patient's age also seems to influence PIM use. Conclusion: Elderly heart failure patients are at a greater risk for adverse drug events attributed by inappropriate medication use. Efforts to increase awareness of PIM use in elderly heart failure patients are needed. In addition, various comprehensive strategies and policies to identify and prevent PIM use should be established nationwide.