Design and Synthesis of a Novel PLK1 Inhibitor Scaffold Using a Hybridized 3D-QSAR Model

Polo-like kinase 1 (PLK1) plays an important role in cell cycle progression and proliferation in cancer cells. PLK1 also contributes to anticancer drug resistance and is a valuable target in anticancer therapeutics. To identify additional effective PLK1 inhibitors, we performed QSAR studies of two series of known PLK1 inhibitors and proposed a new structure based on a hybridized 3D-QSAR model. Given the hybridized 3D-QSAR models, we designed and synthesized 4-benzyloxy-1-(2-arylaminopyridin-4-yl)-1H-pyrazole-3-carboxamides, and we inspected its inhibitory activities to identify novel PLK1 inhibitors with decent potency and selectivity.     

Rheology of poly(vinyl chloride) blends

PVC/EVA blends were studied with an extrusion plastometer in order to examine the effect of EVA on the processability of PVC. The melt flow of PVC/EVA blends containing from 4 to 30 weight percent EVA follows a simple power law between 160 and 180°C. EVA reduced the melt viscosity and enhanced processability. Blends of PVC and EVA were morphologically incompatible. The molecular weight of extruded PVC in the blends was unchanged.     

Synthesis and characterization of new aromatic polyimides containing well‐defined conjugation units

A series of aromatic polyimides composed of well‐defined conjugation units were synthesized form 5,5′‐bis(4‐aminophenyl)‐2,2′‐bifuryl (PFDA) and 2,2′‐bis(furyl) benzidine (FurylBZ) with various dianhydrides. The synthesized polyimides emit blue to green light with a quantum yield of 7.3–14.9%, depending on the polymer backbone. In particular, PFDA‐based polymers exhibit extremely narrow photo‐luminescence. The structure, thermal stability, refractive index and dielectric properties of the polymer films were also determined.     

An analysis of muscles from ultrasound image using morphological information of fascia and thoracic vertebra

In this paper, we propose a new fully computerized image analysis method for measuring the thickness of muscles from ultrasound image obtained by muscle endurance test using morphological information of fascia and thoracic vertebra. Firstly, we divide the image into lumbar region and thoracolumbar region by the difference of density in image for measuring the thickness of muscles. In lumbar region, we notice that the intensity of fascia is relatively higher than other parts. Thus, we measure the thickness of muscles surrounding the fascia area. In the process, we apply median filter to candidate fascia areas for extracting candidate muscle layers between fascias. Then, the thickness of muscles we measure is that of the third layer. In thoracolumbar region, we apply region expansion method for classifying the region into subcutaneous fat part and part including thoracic vertebra. Then, we apply counting method and evolutionary computation search model to find the measuring location that is in between subcutaneous fat area and thoracic vertebra. In experiment, the proposed method is effective in measuring the thickness of muscles and avoids failures of previous studies. The performance of this approach is sufficiently comparable to that of medical experts.     

Development and control of a new AUV platform

This paper presents an architecture of a newly developed autonomous underwater vehicle (AUV) platform, named KAUV-1, which is designed as a torpedo with very light weight and small size, suitable for use in marine exploration and monitoring. The KAUV-1 has a unique ducted propeller located at the aft end with yawing actuation acting as a rudder. For depth motion, the KAUV-1 is designed to have a mass shifter mechanism inside to change the vehicle center of gravity and to control its pitch angle and depth motion. The paper also presents an analysis on the equations of motion of the KAUV-1 with mass shifter mechanism and a new depth control strategy for the KAUV-1. The feasibility of the proposed control strategy is validated through simulation and experiment of performance of the vehicle.     

Robust optimization of foam-filled thin-walled structure based on sequential Kriging metamodel

Deterministic optimization has been successfully applied to a range of design problems involving foam-filled thin-walled structures, and to some extent gained significant confidence for the applications of such structures in automotive, aerospace, transportation and defense industries. However, the conventional deterministic design could become less meaningful or even unacceptable when considering the perturbations of design variables and noises of system parameters. To overcome this drawback, a robust design methodology is presented in this paper to address the effects of parametric uncertainties of foam-filled thin-walled structure on design optimization, in which different sigma criteria are adopted to measure the variations. The Kriging modeling technique is used to construct the corresponding surrogate models of mean and standard deviation for different crashworthiness criteria. A sequential sampling approach is introduced to improve the fitness accuracy of these surrogate models. Finally, a gradient-based sequential quadratic program (SQP) method is employed from 20 different initial points to obtain a quasi-global robust optimum solution. The optimal solutions were verified by using the Monte Carlo simulation. The results show that the presented robust optimization method is fairly effective and efficient, the crashworthiness and robustness of the foam-filled thin-walled structure can be improved significantly.     

Comparison of liquid-phase and methanol-swelling crosslinking processes of polyimide dense membrane for CO2/CH4 separation

To overcome the plasticization effect in polyimide membranes, many researchers have proposed crosslinking method. This can reduce an inter-segmental mobility by tightening and rigidifying the polymer chains. However, it is difficult to modify the whole polymer chains throughout the membrane because the reaction can be hindered by the diffusion rate of the crosslinker. In particular, it is hard for bulky crosslinker to penetrate a dense membrane with a small d-spacing. This study investigated the effect of crosslinking a dense Matrimid membrane with p-phenylenediamine (p-PDA) via two different crosslinking methods (i.e., methanol-swelling crosslinking process [M-SCP] and liquid-phase crosslinking process [L-PCP]). Most of the crosslinking reaction in M-SCP occurs on the membrane surface due to difficulty in penetration of the bulky p-PDA into the Matrimid dense membrane. In contrast, the L-PCP allows uniform crosslinking across the membrane. The membranes crosslinked using L-PCP showed excellent chemical resistance. Furthermore, the plasticization phenomenon was not observed in the membranes crosslinked using L-PCP with p-PDA more than 15%. Meanwhile, the membrane crosslinked using M-SCP exhibited poor plasticization and chemical resistance properties. These results showed that the L-PCP method can be more effective for the crosslinking of dense membrane to deliver both high plasticization and chemical resistance.     

A timing controller embedded driver IC with 3.24‐Gbps eDP interface for chip‐on‐glass TFT‐LCD applications

This paper presents a timing controller embedded driver (TED) IC with 3.24‐Gbps embedded display port (eDP), which is implemented using a 45‐nm high‐voltage CMOS process for the chip‐on‐glass (COG) TFT‐LCD applications. The proposed TED‐IC employs the input offset calibration scheme, the zero‐adjustable equalizer, and the phase locked loop‐based bang‐bang clock and data recovery to enhance the maximum data rate. Also, the proposed TED‐IC provides efficient power management by supporting advanced link power management feature of eDP standard v1.4. Additionally, the smart charge sharing is proposed to reduce the dynamic power consumption of output buffers. Measured result demonstrates the maximum data rate of 3.24 Gbps from a 1.1 V supply voltage with a 7.9‐inch QXGA 60‐Hz COG‐LCD prototype panel and 44% power saving from the display system.     

Scalable digital hardware for a trapped ion quantum computer

Quantum Information Processing - Many of the challenges of scaling quantum computer hardware lie at the interface between the qubits and the classical control signals used to manipulate them....     

A novel part-based approach to mean-shift algorithm for visual tracking

Visual tracking is one of the most important problems considered in computer vision. To improve the performance of the visual tracking, a part-based approach will be a good solution. In this paper, a novel method of visual tracking algorithm named part-based mean-shift (PBMS) algorithm is presented. In the proposed PBMS, unlike the standard mean-shift (MS), the target object is divided into multiple parts and the target is tracked by tracking each individual part and combining the results. For the part-based visual tracking, the objective function in the MS is modified such that the target object is represented as a combination of the parts and iterative optimization solution is presented. Further, the proposed PBMS provides a systematic and analytic way to determine the scale of the bounding box for the target from the perspective of the objective function optimization. Simulation is conducted with several benchmark problems and the result shows that the proposed PBMS outperforms the standard MS.