基于Hsp90 ATPase活性的抑制剂筛选模型研究

热休克蛋白90(Heat shock protein,Hsp90)作为分子伴侣,参与调控肿瘤细胞多条信号通路,对肿瘤细胞生长有重要作用.以pGEX-4T-1为载体,构建了Hsp90表达载体于宿主大肠杆菌中表达.通过孔雀绿磷钼酸铵-无机磷检测法,测定异源表达的Hsp90 ATPase活性.实验得出Hsp90对ATP的米氏常数(Km)为369.1 μmol/L,在Hsp90和ATP浓度分别为0.18,1 mmol/L时转换效率常数(kcat)为1.6 min-1,最大反应速率(Vmax)为1.0 μmol/(L·min).基于该方法,建立Hsp90 ATPase活性抑制剂筛选模型,以Geldanamycin和Radicicol为阳性对照,发现Rifamycin、Rugulosin及MycoE也有较强的Hsp90 ATPase抑制活性.该方法可用于筛选抗肿瘤候选化合物的研究,同时也可为具有ATPase活性蛋白的抑制剂筛选提供参考.     

Application of Standardization for Initial Design of Plastic Injection Moulds

Today, the time-to-market for plastic products ar e getting shorter, thus the lead-time for making the injection mould is decreasin g. There is potential in timesavings in the mould design stage because the design process that is repeatable for every mould design can be standardized. T he preliminary work of any final plastic injection mould design is to always pro vide an initial design of the mould assembly for product designers (customers) p rior to receiving the final product CAD data. Traditiona...     

Influence of hot-rolling on the microstructure and mechanical properties of a near β-type Ti-5.2Mo-4.8Al-2.5Zr-1.7Cr alloy

In this work, the 90° clock rolling and the uni-directionally rolling processes at high temperature were carried out on the near β-type Ti-5.2Mo-4.8Al-2.5Zr-1.7Cr titanium alloy cutting from an ingot, respectively. The corresponding microstructures were quantitatively characterized, and its effect on the dynamic mechanical properties and fracture mechanism were emphatically investigated. It was found that after 90° clock rolling, the microstructure composed of equiaxed primary α phase(α_p) with an average size of about 2 ?μm and the β transformed regions containing the acicular secondary α phase(α_s) with an average thickness of about 50 ?nm and the separated β phase was obtained. However, in the uni-directionally rolled titanium alloy, no acicular α_s was observed, and the corresponding microstructure consisted elongated lamellar α phase (average thickness: about 1.3 ?μm), few equiaxed α phase (average grain size: about 300 ?nm) and the inlaid β phase. The microstructural difference of the hot-rolled titanium alloys was closely related to the deformation process. Moreover, a great number of α_p and α_s in the 90° clock rolled titanium alloy effectively enhanced the strength, and the dynamic compressive strength reached to 1730 ?MPa. Furthermore, equiaxed α_p was conducive to the homogeneous deformation, which counteracted the localized deformation caused by acicular α_s to a certain extent and made the 90° clock rolled titanium alloy exhibit an acceptable critical fracture strain of about 10.5%. Moreover, the fracture microstructures showed that the main failure mode of the 90° clock rolled and the uni-directionally rolled titanium alloy were ductile fracture and brittle fracture, respectively.     

5A90铝锂合金显微组织及力学性能的研究

利用光学显微镜、扫描电镜及高分辨透射电镜等手段研究了5A90铝锂合金轧板经热处理后的显微组织与力学性能.结果表明:5A90合金轧板组织呈明显的各向异性,合金板材轧制平面的晶粒呈等轴状,纵截面和横截面均为轧制流线组织,有少量细小的再结晶晶粒；合金经460℃/20 min固溶处理后,在130℃时效过程中,随着时效时间的延长...