气相色谱-质谱法测定浓缩苹果汁中丁酰肼残留量

采用在碱性条件下将样品中丁酰肼水解为不对称二甲基联氨,再用水杨醛与之发生衍生化反应的前处理方法,建立了浓缩苹果汁中丁酰肼残留量的气相色谱-质谱(GC-MS)测定方法。以丁酰肼浓度对峰面积作图得校正曲线,回归方程为y=100 211x-11 156(r=0.999 6),检出限(3S/N)为0.01 mg.kg-1,测定结果的相对标准偏差为1.60%~6.23%,回收率为92%~107%。     

A CE‐based assay for human protein kinase CK2 activity measurement and inhibitor screening

A new assay for protein kinase CK2 activity determination based on the quantification of a phosphorylated substrate was developed. The common CK2 substrate peptide RRRDDDSDDD, conjugated with the fluorophore 5‐[(2‐aminoethyl)amino]naphthalene‐1‐sulfonic acid at the C‐terminus served as the analyte. By means of CZE using 2 mol/L acetic acid as electrolyte and UV detection at 214 nm, the non‐phosphorylated and the phosphorylated peptide variants could be resolved within 6 min from a complex assay mixture. By this means, activity of human CK2 could be monitored by a kinetic, as well as an endpoint, method. Inhibition of human recombinant CK2 holoenzyme by 6‐methyl‐1,3,8‐trihydroxyanthraquinone and 4,5,6,7‐tetrabromobenzotriazole resulted in IC₅₀ values of 1.33 and 0.27 μM, respectively, which were similar to those obtained with the standard radiometric assay. These results suggest that the CE/UV strategy described here is a straightforward assay for CK2 inhibitor testing.     

Resonant fluorescence emission from the Ge and Cu valence band

Received: 16 March 1996     

Trusted Threat Intelligence Sharing in Practice and Performance Benchmarking through the Hyperledger Fabric Platform

Historically, threat information sharing has relied on manual modelling and centralised network systems, which can be inefficient, insecure, and prone to errors. Alternatively, private blockchains are now widely used to address these issues and improve overall organisational security. An organisation’s vulnerabilities to attacks might change over time. It is utterly important to find a balance among a current threat, the potential countermeasures, their consequences and costs, and the estimation of the overall risk that this provides to the organisation. For enhancing organisational security and automation, applying threat intelligence technology is critical for detecting, classifying, analysing, and sharing new cyberattack tactics. Trusted partner organisations can then share newly identified threats to improve their defensive capabilities against unknown attacks. On this basis, organisations can help reduce the risk of a cyberattack by providing access to past and current cybersecurity events through blockchain smart contracts and the Interplanetary File System (IPFS). The suggested combination of technologies can make organisational systems more reliable and secure, improving system automation and data quality. This paper outlines a privacy-preserving mechanism for threat information sharing in a trusted way. It proposes a reliable and secure architecture for data automation, quality, and traceability based on the Hyperledger Fabric private-permissioned distributed ledger technology and the MITRE ATT&CK threat intelligence framework. This methodology can also be applied to combat intellectual property theft and industrial espionage.     

Downfalls of Chemical Probes Acting at the Kinase ATP-Site: CK2 as a Case Study

Protein kinases are a large class of enzymes with numerous biological roles and many have been implicated in a vast array of diseases, including cancer and the novel coronavirus infection COVID-19. Thus, the development of chemical probes to selectively target each kinase is of great interest. Inhibition of protein kinases with ATP-competitive inhibitors has historically been the most widely used method. However, due to the highly conserved structures of ATP-sites, the identification of truly selective chemical probes is challenging. In this review, we use the Ser/Thr kinase CK2 as an example to highlight the historical challenges in effective and selective chemical probe development, alongside recent advances in the field and alternative strategies aiming to overcome these problems. The methods utilised for CK2 can be applied to an array of protein kinases to aid in the discovery of chemical probes to further understand each kinase’s biology, with wide-reaching implications for drug development.     

Kadomtsev-Petviashvilli方程的直接相似约化

Clarkson和Kruskal发展的直接法(CK直接法)是求解非线性微分方程相似约化的一种强有力的方法. 本文以Kadomtsev-Petviashvilli(KP)方程为例, 运用CK直接法把KP方程简化为3种类型的(1+1)维偏微分方程, 这3种偏微分方程等价于经典Lie方法得到的3种具有不同独立变量的相似约化方程. KP方程的解包含了更多经典Lie方法所遗漏的任意函数, 例如, CK直接法得到的第3类约化可以分为3个子情形, 而经典Lie法得到的KP方程的第3类解只是我们结果的一个子情形的特例.     

求非线性系统对称群的新方法

(1)从Lax可积系统的Lax对出发, 寻找非线性系统的对称及精确解, 利用这种方法可以解决不少(2＋1)维的可积系统, 它的优点在于比较简洁方便, 这从KP方程的求解对比就可以看出. (2)从CK直接法入手, 将这种方法进行修正, 利用这种修正的CK直接法求非线性系统的对称和精确解; 这种方法的最大优点在于不但可以用于可积系统, 而且也适用于不可积系统, 还可以求出离散群. 另外, 这种方法也适用于高维的不可积模型.     

Non-Lie Symmetry Groups of (2+1)-Dimensional Nonlinear Systems

A modified direct method is developed to find finite symmetry groups of nonlinear mathematical physics systems. Applying the modified direct method to the well-known (2 1)-dimensional asymmetric Nizhnik-Novikov-Vesselov equation and Nizhnik-Novikov-Vesselov equation, both the Lie point symmetry groups and the non-Lie symmetry groups are obtained. The Lie symmetry groups obtained via traditional Lie approaches are only special cases. Furthermore, the expressions of the exact finite transformations of the Lie groups are much simpler than those obtained via the standard approaches.     

Non-Lie Symmetry Groups of （2＋1）-Dimensional Nonlinear Systems

A modified direct method is developed to find finite symmetry groups of nonlinear mathematical physics systems. Applying the modified direct method to the well-known （2＋1）-dimensional asymmetric Nizhnik-Novikov-Vesselov equation and Nizhnik Novikov-Vesselov equation, both the Lie point symmetry groups and the non-Lie symmetry groups are obtained. The Lie symmetry groups obtained via traditional Lie approaches are only speciai cases. Furthermore, the expressions of the exact finite transformations of the Lie groups are much simpler than those obtained via the standard approaches.     

High quality drug screening by capillary electrophoresis: A review

High quality assays are needed in drug discovery to reduce the high attrition rate of lead compounds during primary screening. Capillary electrophoresis (CE) represents a versatile micro-separation technique for resolution of enzyme-catalyzed reactions, including substrate(s), product(s), cofactor(s) and their stereoisomers, which is needed for reliable characterization of biomolecular interactions in free solution. This review article provides a critical overview of new advances in CE for drug screening over the past five years involving biologically relevant enzymes of therapeutic interest, including transferases, hydrolases, oxidoreductases, and isomerases. The basic principles and major configurations in CE, as well as data processing methods needed for rigorous characterization of enzyme inhibition are described. New developments in functional screening of small molecules that modulate the activity of disease-related enzymes are also discussed. Although inhibition is a widely measured response in most enzyme assays, other important outcomes of ligand interactions on protein structure/function that impact the therapeutic potential of a drug will also be highlighted, such as enzyme stabilization, activation and/or catalytic uncoupling. CE offers a selective platform for drug screening that reduces false-positives while also enabling the analysis of low amounts of complex sample mixtures with minimal sample handling.