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.     

矿用钻孔深度测量仪的设计

设计了一种以STM32F103微控制器为控制核心,基于24位高精度模数转换器的钻孔深度测量仪器。利用弹性波回波测距原理,通过测量出钻孔中钻杆的长度,实现钻孔深度的快速、无损、准确的测量,主要用于井下瓦斯抽放钻孔、探放水钻孔等煤矿通防工作的施工验收。仪器小巧轻便,操作简单,单人即可完成测量工作,节约下井的人力物力,提高生产效率,最长测量长度可达250米,误差不超过1米。     

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%.     

安家岭露天矿过采空区危险源辨识及安全措施研究

危险源辨识对提高煤矿安全生产具有重要的现实意义。研究建立了基于层次分析法的安家岭露天矿危险源辨识模型,确定了危险源指标的权重。依据危险源辨识的权重研究了安家岭露天矿过采空区安全开采存在的主要危险源,并把采空区分为高温明火采空区、积水采空区、存在有毒气体的采空区、未冒实采空区,针对不同的类别的采空区提出了相应的安全开采措施。