A Dual Inhibitor of DYRK1A and GSK3β for β-Cell Proliferation: Aminopyrazine Derivative GNF4877

Loss of β-cell mass and function can lead to insufficient insulin levels and ultimately to hyperglycemia and diabetes mellitus. The mainstream treatment approach involves regulation of insulin levels; however, approaches intended to increase β-cell mass are less developed. Promoting β-cell proliferation with low-molecular-weight inhibitors of dual-specificity tyrosine-regulated kinase 1A (DYRK1A) offers the potential to treat diabetes with oral therapies by restoring β-cell mass, insulin content and glycemic control. GNF4877, a potent dual inhibitor of DYRK1A and glycogen synthase kinase 3β (GSK3β) was previously reported to induce primary human β-cell proliferation in vitro and in vivo. Herein, we describe the lead optimization that lead to the identification of GNF4877 from an aminopyrazine hit identified in a phenotypic high-throughput screening campaign measuring β-cell proliferation.     

On stochastic comparisons of finite mixtures for some semiparametric families of distributions

In this paper, we consider the classical finite mixture model, which is an effective tool for modeling lifetime distributions for random samples from heterogeneous populations. We discuss new results on stochastic comparison for two finite mixtures when each of them is drawn from one of the following semiparametric families, i.e., proportional hazards, accelerated lifetime and proportional reversed hazards.     

基于光纤技术的采空区发火监测系统的应用

基于光纤技术的采空区发火监测系统由传感器、数据传输、数据分析与控制三大部分构成,研发新一代适合煤矿安全领域应用的先进传感器、并以此为基础构建新型煤矿安全灾害监测预警系统,对于实现煤矿安全发展具有十分重要的意义。     

Is the List of Incomplete Open Cubes Complete?

Variations of Incomplete Open Cubes is the major project by the twentieth-century conceptual artist Sol LeWitt. In this paper we interpret the enumerative component of the project as embeddings of graphs. This formulation permits use of an algorithm to check the completeness of the list of the structures produced by the artist. Our conclusion is that the artist found the correct number of structures (that is, 122), but that his list contains a mistake in the presentation of a pair of incomplete cubes, a discovery that appears not to have been noted before.     

A method for rapidly evaluating reliability and predicting remaining useful life using two-dimensional convolutional neural network with signal conversion

Journal of Mechanical Science and Technology - Real-time monitoring and rapid evaluation of bearing operating conditions, especially for the reliability evaluation and remaining useful life (RUL)...     

Bamboo biochar-catalytic degradation of lignin under microwave heating

Abstract

Lignin biochar-catalytic depolymerization using biochar Fe-600, Fe-800, Ni-600, Ni-800 catalysts under microwave-heating (180?°C for 30?min) was explored in an ethanol/formic acid (1:1) media. Non-catalyst depolymerization was also studied and compared with the biochar-catalysts results. Characteristics of the bio-char catalysts were analyze by BET, XRD, and FT-IR. GPC, FT-IR, and MALDI-TOF MS spectrometry were also used to characterize the depolymerization products. The experimental results showed that the S_BET, V_t, and V_mec and average pore diameter of the biochars are considerably dependent on the preparation temperature and type of cation (Ni²⁺ or Fe³⁺). The maximum yield of bio-oil product was obtained as 85?wt% with the addition of biochar Ni-600 and the total amount of oligomers or monomers with a molecular weight of 164 to 446 reaches 80.4%.     

A computer aided design method for car form and its application based on shape parameters

In the early design stage, automotive modeling should both meet the requirements of aesthetics and engineering. Therefore, a vehicle CAD (computer aided design) model that can be easily adjusted by feedbacks is necessary. Based on CE-Bézier surface, this paper presents a set of algorithms for parametric segmentation and fairing surface generation in a car model. This model is defined by a simplified automotive template and relevant control points, shape parameters and segmentation parameters, which can be modified to alter the car form efficiently. With this model and the corresponding adjustment method, more than fifty various vehicle models are established in this research according to different parameters. And two methods for calculating similarity index between car models are constructed, which are suitable for brand design trend analysis and modelling design decisionmaking.