• Title/Summary/Keyword: PiD

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Pharmacophore Based Screening and Molecular Docking Study of PI3K Inhibitors

  • Rupa, Mottadi;Madhavan, Thirumurthy
    • Journal of Integrative Natural Science
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    • v.9 no.1
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    • pp.41-61
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    • 2016
  • Non-small cell lung cancer (NSCLC) is the leading cause of cancer-related mortality worldwide. Phosphoinositide 3-kinases (PI3Ks) play important role in Non-Small Cell Lung Cancer. PI3Ks constitute a lipid kinase family which modulates the function of numerous substrates involved in the regulation of cell survival, cell cycle progression and cellular growth. Herein, we describe the ligand based pharmacophore combined with molecular docking studies methods to identify new potent PI3K inhibitors. Several pharmacophore models were generated and validated by Guner-Henry scoring Method. The best models were utilized as 3D pharmacophore query to screen against ZINC database (Chemical and Natural) and the retrieved hits were further validated by fitness score, Lipinski's rule of five. Finally four compounds were found to have good potential and they may act as novel lead compounds for PI3K inhibitor designing.

Properties and Thermostability of Gelatin-degrading Proteinases in the Fruit of Actinidia chinensis (Kiwifruit) (Kiwifruit 과육에 존재하는 단백질분해효소의 특성과 열안정성)

  • 오순자;김성철;고석찬
    • Journal of Life Science
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    • v.12 no.6
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    • pp.752-758
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    • 2002
  • This study was investigated on properties and thermostability of gelatin-degrading proteinases in the fruit of Actinidia chinensis (kiwifruit) for the industrial application. Three gelatin-degrading proteinases (PI, PII and PIII) were detected from the pulp of fruits. The molecular weights of these proteinases, PI, PII and PIII, were approximately 220 kD, 51 kD, and 26 kD respectively, on the basis of gelatin-containing SDS-PACE. The optimum pH of these proteinases ranged from 2.0 to 5.0 with a maximal activity at pH 4.0. These proteinases had a high sensitivity to E-64 and iodoacetate which are cysteine protease inhibitors, and required DTT, cysteine, and $\beta$-mercaptoethanol for their activities which are stimulators for cysteine proteases. These results indicate that these proteinases are cysteine proteinases and the proteinase PIII is actinidin (EC 3.4.22.14), based on the molecular weight and/or susceptibility against proteinase inhibitors. These proteinases were strongly activated by $Ca^{2+}$, $Mg^{2+}$ and $Mn^{2+}$, whereas strongly inhibited by Zn$^{2+}$ and Hg$^{2+}$. However, these proteinases have slightly different susceptibility against other cations ($Ca^{2+}$, $Cu^{2+}$, $Al^{3+}$, $Ca^{3+}$. The temperature stability of proteinase PIII was more stable than proteinases PI and PII. Moreover, proteinase PIII remained stable below $50^{\circ}C$ for 48hr, showing the residual activity above 75% of the enzyme activity.

Molecular Design for the Formation of Two-dimensional Molecular Networks: STM Study of ${\gamma}$-phenylalanine on Au(111)

  • Jeon, A-Ram;Youn, Young-Sang;Lee, Hee-Seung;Kim, Se-Hun
    • Proceedings of the Korean Vacuum Society Conference
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    • 2011.08a
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    • pp.205-205
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    • 2011
  • The self-assembly of ${\gamma}$-phenylalanine on Au(111) at 150 K was investigated using scanning tunneling microscopy (STM). Phenylalanine can potentially form two-dimensional (2D) molecular networks through hydrogen bonding (through the carboxyl and amino groups) and ${\pi}-{\pi}$ stacking interactions (via aromatic rings). We found that ${\gamma}$-phenylalanine molecules self-assembled on Au(111) surfaces into well-ordered structures such as ring-shaped clusters (at low and intermediate coverages) and 2D molecular domains (intermediate and monolayer coverages), whereas ${\alpha}$-phenylalanine molecules formed less-ordered structure on Au(111). The self-assembly of ${\gamma}$- but not ${\alpha}$-phenylalanine may be related to the flexibility of the carboxyl and amino groups in the molecule. Moreover, as expected, the 2D molecular network of ${\gamma}$-phenylalanine on Au(111) was mediated by a combination of hydrogen bonding and ${\pi}-{\pi}$ stacking interactions.

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Effect of Phospholipase D on the L-$\alpha$-Dimyristoyl-phosphatidyl Choline Liposome Containing Cholesterol, L-$\alpha$-Phosphatidylinositol and L-$\alpha$-Phosphatidylserine (Cholesterol, L-$\alpha$-Phosphatidylinositol, L-$\alpha$-Phosphatidylserine을 함유한 L-$\alpha$-Dimyristoyl-phosphatidyl Choline 리포솜에 대한 Phospholipase D의 작용에 관한 연구)

  • 이은옥
    • YAKHAK HOEJI
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    • v.27 no.4
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    • pp.249-256
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    • 1983
  • When the reaction rate constant k of phospholipase D on liposome was measured by the ANS fluorometry, k of phospholipase D on DMPC liposome which was made of L-$\alpha$-PI, cholesterol and L-$\alpha$-PS decreased than that of phospholipase D on DMPC liposome with cholesterol or with PI and cholesterol. Optimal $Ca^{2+}$ concentration, the most important factor on effect of phospholipase D, also decreased to 1mM, as compared with 10mM and 60mM respectively when cholesterol and PI were added, and cholesterol only was added. The change of cholesterol Mol% had a great influence on k value of phospholipase D. But in case of addition of L-$\alpha$-PS to cholesterol, the influence was relatively diminished.

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A Study on the Fabrication of Variable Attenuator using a Diode (다이오드를 이용한 가변 감쇠기의 설계 및 제작에 관한 연구)

  • Jeon, Joong-Sung
    • Journal of Advanced Marine Engineering and Technology
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    • v.32 no.1
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    • pp.147-152
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    • 2008
  • This paper has been fabricated the two different type of variable attenuators using a characteristics of a 3 dB directional coupler and pin diodes. One was not analyzed using the conventional even-odd modes but used simple two-port techniques. The resulting scattering parameters described operation characteristics for the general case where the terminating impedances are equal and unequal. After analyzing resistor role of the ${\pi}$ type fixed attenuator. this paper used a pin diode instead of a resistor. The variable attenuators were fabricated using pin diodes for current-controlled attenuation on the coupled ports of a 3 dB branch-line coupler and ${\pi}$ type fixed attenuator. The realized variable attenuators have more than 33 dB attenuation ranges at 2.1 GHz. and the input and output reflection coefficients are less than -13 dB. These results could be applied to mobile communication systems. It can be varied gain of the power amplifier according to change a outdoor environmental temperature and improved linearity.

Overview of 3-D IC Design Technologies for Signal Integrity (SI) and Power Integrity (PI) of a TSV-Based 3D IC

  • Kim, Joohee;Kim, Joungho
    • The Proceeding of the Korean Institute of Electromagnetic Engineering and Science
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    • v.24 no.2
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    • pp.3-14
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    • 2013
  • In this paper, key design issues and considerations for Signal Integrity(SI) and Power Integrity(PI) of a TSV-based 3D IC are introduced. For the signal integrity and power integrity of a TSV-based 3-D IC channel, analytical modeling and analysis results of a TSV-based 3-D channel and power delivery network (PDN) are presented. In addition, various design techniques and solutions which are to improve the electrical performance of a 3-D IC are investigated.

Sensorless Control of Non-salient Permanent Magnet Synchronous Motor Drives using Rotor Position Tracking PI Controller

  • Lee Jong-Kun;Seok Jul-Ki
    • KIEE International Transaction on Electrical Machinery and Energy Conversion Systems
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    • v.5B no.2
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    • pp.189-195
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    • 2005
  • This paper presents a new velocity estimation strategy for a non-salient permanent magnet synchronous motor drive without high frequency signal injection or special PWM pattern. This approach is based on the d-axis current regulator output voltage of the drive system, which contains the rotor position error information. The rotor velocity can be estimated through a rotor position tracking PI controller that controls the position error at zero. For zero and low speed operation, the PI gain of the rotor position tracking controller has a variable structure according to the estimated rotor velocity. Then, at zero speed, the rotor position and velocity have sluggish dynamics because the varying gains are very low in this region. In order to boost the bandwidth of the PI controller during zero speed, the loop recovery technique is applied to the control system. The PI tuning formulas are also derived by analyzing this control system by frequency domain specifications such as phase margin and bandwidth assignment.

Response Characteristics of Fast TN Cell on a Polyimide Surface (폴리이미드 표면에서의 고속 TN 셀의 응답 특성)

  • Jeon, Yong-Je;Hwang, Jeong-Yeon;Jeong, Youn-Hak;Seo, Dae-Shik
    • Proceedings of the Korean Institute of Electrical and Electronic Material Engineers Conference
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    • 2002.11a
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    • pp.514-517
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    • 2002
  • We investigated response characteristics of twisted nematic (TN) cell with different nematic liquid crystals (NLCs) and cell gap d on a rubbed polyimide (PI) surface. High transmittance and fast response time of the TN cell on the rubbed PI surface were achieved by using high birefringence (${\Delta}n$) and low cell gap d. The response time of TN cell on the rubbed PI surface was measured 5.1 ms. The transmittance and response time of the TN cell on the rubbed PI surface decreased with decreasing ${\Delta}nd$.

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A Study on Response Characteristics of TN Cell on a Polyimide Surface (폴리이미드 표면에서의 TN 셀의 응답 특성에 관한 연구)

  • 황정연;전용제;정연학;서대식
    • Journal of the Korean Institute of Electrical and Electronic Material Engineers
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    • v.15 no.9
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    • pp.808-811
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    • 2002
  • We investigated response characteristics of twisted nematic (TN) cell with different nematic liquid crystals (NLCs) and cell gap d on a rubbed polyimide (PI) surface. High transmittance and fast response time of the TN cell on the rubbed PI surface were achieved by using high birefringence (Δn) and low cell gap d. The response time of TN cell on the rubbed PI surface was measured 5.1 ms. The transmittance and response time of the TN cell on the rubbed PI surface decreased with decreasing Δnd.

New Method of SVPWM Implementation Using Single Carrier Wave and Comparision of PI/PR Current Control for the Vienna Converter (비엔나 컨버터를 위한 단일 반송파를 이용한 새로운 방식의 SVPWM 구현과 PI/PR 전류제어기의 비교)

  • Cho, Nam-Su;Ji, Jun-Keun;Lee, Tae-Won;Yun, Bong-Young
    • The Transactions of The Korean Institute of Electrical Engineers
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    • v.66 no.3
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    • pp.522-532
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    • 2017
  • In this paper, a new method of SVPWM implementation for 3-Phase 3-Leg 3-Level AC/DC converter known as the Vienna converter is proposed. Also the performances of PI and PR controller used in AC input current controller are compared. To verify the proposed method, PSIM, a power electronics simulation program, is utilized. The performances of the proposed new method and the two existing methods are compared through simulation and experiment. Also PI and PR controller in AC input current controller are compared through 10[kW] Vienna converter system.