Docetaxel单用和与batimastat 联用对人肺巨细胞癌模型的抗肿瘤作用

目的 研究docetaxel 和batimastat (BB-94)对人肺巨细胞癌(PG) 的作用并与阿霉素做比较。方法和结果 docetaxel 对PG 细胞有明显的细胞毒作用, BB-94 则无此作用, 而且BB-94 体外不能增强docetaxel 的细胞毒作用。体内在早期PG 瘤裸鼠模型上应用最大耐受量的docetaxel 和阿霉素(iv, q4d×3) 、BB-94 (30 mg·kg^-1, ip, qd×20), docetaxel 联用 BB-94 的抑瘤率(97.3 %)大于阿霉素联用BB-94 (86.5 %)、docetaxel (92.0 %)、阿霉素(74.0 %)和BB-94 (31.0 %)。docetaxel 对晚期PG 瘤也具有明显的抑制作用, 而且强于阿霉素。结论 docetaxel 对PG 瘤裸鼠模型具有显著抑制作用, 联用BB-94 可增强docetaxel的抗肿瘤作用。     

非线性规划在坦克武器系统火力分配中的应用

为解决在战场上可视条件差、对射击效果观察困难时的坦克射击问题，运用非线性规划模型就坦克武器系统如何在射击前对现有目标进行有效的火力分配及使火力分配最佳进行了研究，给出了最佳方案的计算方法，并设计出具体的解法流程，以利于计算机实现。     

Beam Tracking Particle Filter for Hybrid Beamforming and Precoding Systems

Because millimeter wave (mmWave) systems can span notably wide spectral bands, mmWave systems are expected to dominate fifth-generation (5G) communication systems. Due to the short wave-length of mmWave radiation, multiple-input multiple-output (MIMO) systems can use massive antennas and precoding technology to overcome signal attenuation in mmWave channels. However, the cost and power consumption of radio frequency (RF) chains would increase substantially with the number of antennas. Hence, hybrid beamforming was proposed to reduce the number of RF chains in massive MIMO systems. Hybrid beamforming involves RF beamforming matrix construction and baseband precoding matrix derivation. This study focused on the design and implementation of an algorithm for the RF beamforming matrix construction for mobile environments. Accordingly, this study presents a mixture particle filter that exploits the temporal continuity of beam clusters in a mobile mmWave channel to reduce the computational complexity of RF beamforming matrix construction. Moreover, this beam-tracking particle filter is based on parallel processing architecture to support the tracking of multiple beam clusters in the mmWave channel. Finally, the beam-tracking particle filter was implemented on a field-programmable gate array platform and was verified in a hybrid beamforming system for mmWave MIMO systems. The particle filter processor achieved a maximal throughput of 9.198k matrices/s with a clock rate of 192 MHz, which could support a speed of up to 88.5 km/h for mobile users.

     

Towards more accurate pharmacophore modeling: Multicomplex-based comprehensive pharmacophore map and most-frequent-feature pharmacophore model of CDK2

Pharmacophore modeling, including ligand- and structure-based approaches, has become an important tool in drug discovery. However, the ligand-based method often strongly depends on the training set selection, and the structure-based pharmacophore model is usually created based on apo structures or a single protein-ligand complex, which might miss some important information. In this study, multicomplex-based method has been suggested to generate a comprehensive pharmacophore map of cyclin-dependent kinase 2 (CDK2) based on a collection of 124 crystal structures of human CDK2-inhibitor complex. Our multicomplex-based comprehensive pharmacophore map contains almost all the chemical features important for CDK2-inhibitor interactions. A comparison with previously reported ligand-based pharmacophores has revealed that the ligand-based models are just a subset of our comprehensive map. Furthermore, one most-frequent-feature pharmacophore model consisting of the most frequent pharmacophore features was constructed based on the statistical frequency information provided by the comprehensive map. Validations to the most-frequent-feature model show that it can not only successfully discriminate between known CDK2 inhibitors and the molecules of focused inactive dataset, but also is capable of correctly predicting the activities of a wide variety of CDK2 inhibitors in an external active dataset. Obviously, this investigation provides some new ideas about how to develop a multicomplex-based pharmacophore model that can be used in virtual screening to discover novel potential lead compounds.