A Potent,Selective and Cell‐Active Allosteric Inhibitor of Protein Arginine Methyltransferase 3 (PRMT3)

PRMT3 catalyzes the asymmetric dimethylation of arginine residues of various proteins. It is essential for maturation of ribosomes, may have a role in lipogenesis, and is implicated in several diseases. A potent, selective, and cell‐active PRMT3 inhibitor would be a valuable tool for further investigating PRMT3 biology. Here we report the discovery of the first PRMT3 chemical probe, SGC707, by structure‐based optimization of the allosteric PRMT3 inhibitors we reported previously, and thorough characterization of this probe in biochemical, biophysical, and cellular assays. SGC707 is a potent PRMT3 inhibitor (IC₅₀=31±2 nM , K_D=53±2 nM ) with outstanding selectivity (selective against 31 other methyltransferases and more than 250 non‐epigenetic targets). The mechanism of action studies and crystal structure of the PRMT3‐SGC707 complex confirm the allosteric inhibition mode. Importantly, SGC707 engages PRMT3 and potently inhibits its methyltransferase activity in cells. It is also bioavailable and suitable for animal studies. This well‐characterized chemical probe is an excellent tool to further study the role of PRMT3 in health and disease.     

交流电激发下的聚合物PPV单层薄膜发光器件的电致发光

交流电激发下的聚合物ＰＰＶ单层薄膜发光器件的电致发光＊张凤玲ａ，ｂ）杨志敏ａ）徐征ａ）黄宗浩ｃ）徐长远ａ）王永生ａ）徐叙王容ａ，ｂ）ａ）（北方交通大学光电子技术研究所，北京１０００４４）ｂ）（天津理工学院材料物理研究所，天津３００１９１）ｃ）（东北师...     

N-+-烷基-N''-(对氨基苯磺酸钠)硫脲光度法测定铜

研完了新显色剂长链饱和脂肪烃取代基化合物(UPT)和微量Cu2+反应。试验表明，在pH 5.2～5.6的乙酸－乙酸钠介质中,Cu2+与试剂形成摩尔比为13的淡黄绿色稳定络合物，其最大吸收为 300.4nm，表观摩尔吸光系数为ε300.4nm＝2.39×105L·mol·cm-1。铜浓度在2～12μg/25m1的范围内符合比耳定律，相关系数r＝O.9990。方法简便、灵敏，应用于样品测定，结果满意。     

Effects of Light Exposure and Use of Intraocular Lens on Retinal Pigment Epithelial Cells In Vitro

To investigate the effect of a blue light-filtering intraocular lens (IOL) and a UV-absorbing IOL on light-induced damage to retinal pigment epithelial (RPE) cells laden with the lipofuscin fluorophore N -retinylidene- N -retinylethanolamine (A2E), A2E-laden RPE cells were exposed to white light which was filtered by either a blue light-filtering IOL or a UV-absorbing IOL. After 30 min of illumination the cell viability and the level of reactive oxygen species (ROS), free glutathione (GSH), vascular endothelial growth factor (VEGF) and pigment epithelium-derived factor (PEDF) were determined. In the absence of an IOL, the white light exposure decreased cell viability to 37.2% of the nonirradiated control. The UV-absorbing IOL tended to reduce light-induced cell death; however, the decrease was not significant. The blue light-filtering IOL significantly attenuated light-induced cell damage, increasing cell viability to 79.5% of the nonirradiated control. The presence of the blue light-filtering IOL significantly increased GSH and PEDF levels, and decreased ROS and VEGF levels. This study suggests that a blue light-filtering IOL may be more protective against A2E-induced light damage and inhibit more light-induced ROS and VEGF production than a conventional UV-absorbing IOL.     

α次积分半群的扰动

在n次积分半群及一次积分半群扰动理论的基础上,探讨了α次积分半群的扰动性,得到了α次积分半群的扰动定理.     

Thermally activated delayed fluorescence molecules and their new applications aside from OLEDs

Thermally activated delayed fluorescence (TADF) organic molecules feature with long-lived delayed fluorescence, because they can undergo not only efficient intersystem crossing (ISC), but also efficient reverse intersystem crossing (RISC) at room temperature. As a new type of luminescent molecules, they have exhibited successful applications in organic light emitting diodes (OLEDs). Aside from OLEDs, they are also found to have potential applications in time-resolved luminescence imaging based on long-lived fluorescence property. Meanwhile, due to their excited triplet characteristic originated from efficient ISC, they were found to be applied in triplet-triplet annihilation upconversion (TTA-UC), photodynamic therapy (PDT) and organic photocatalytic synthesis. This review briefly summarizes the characteristics and excellent photophysical properties of TADF organic compounds, then covers their applications to date aside from OLEDs based on their highly efficient ISC ability and RISC ability at room temperature.     

The binding of 3-(p-bromophenyl)-5-methyl-thiohydantoin with human serum albumin: Investigation by fluorescence spectroscopy and molecular model

The binding of 3-(p-bromophenyl)-5-methyl-thiohydantoin (BPMT) with human serum albumin (HSA) was investigated by fluorescence spectroscopy in combination with UV absorption spectrum under physiological conditions. The intrinsic fluorescence of HSA was quenched by BPMT through static quenching mechanism and the fluorescence emission spectrum of HSA exhibited appreciable hypsochromic shift with increasing concentration of BPMT. The binding constants (K) of HSA with BPMT and the number binding sites (n) at different temperatures, thermodynamic parameter enthalpy changes (ΔH) and entropy changes (ΔS) of HSA-BPMT have been calculated according to the relevant fluorescence data, indicating that the hydrophobic interaction played a major role, which was consistent with the result of molecular modeling study.     

Heptamethine cyanine dyes with a large stokes shift and strong fluorescence: a paradigm for excited-state intramolecular charge transfer

New heptamethine cyanine dyes with an alkylamino group at the central position were found to exhibit a large Stokes shift (>140 nm) and strong fluorescence. They were suggested to be a new paradigm for excited-state intramolecular charge transfer (ICT). The configuration change of the bridgehead amine accompanying ICT was investigated in different viscosity and pH media.     

两个压缩体融合为一个压缩体的充分必要条件北大核心CSCD

本文给出了两个压缩体沿紧致连通曲面(带边曲面或闭曲面)融合仍是一个压缩体(有非空负边界)的充分必要条件,还给出了两个3维流形沿着边界上的紧致连通带边曲面融合中的融合曲面为边界不可压缩的一个特征描述,同时还证明了压缩体的每个Heegaard分解是标准的.     

Facile fabrication of porous oil‐absorbent microspheres with high oil absorbency and fast oil absorption speed

A novel type of porous oil‐absorbent microspheres based on poly(stearyl methacrylate‐co‐butyl acrylate) was prepared via suspension polymerization. By investigating the effects of the cross‐linking agent, monomer ratio, initiator, stabilizer, water/oil ratio, and porogen agent on the oil absorbency of the prepared oil‐absorbents, an optimized oil‐absorbent microsphere OAM‐T was obtained, and characterized by FT‐IR and SEM. The oil absorbencies of OAM‐T toward chloroform, toluene, gasoline, and diesel were measured to be 61.9, 32.6, 28.8, and 28.2 g/g respectively, with oil absorption saturation time being 1.0, 1.5, 2.0, and 3.0 hr. The oil retention of OAM‐T toward the four oils is all above 95%. Besides in pure oils, OAM‐T also has high oil absorbencies in oil–water mixture. It can be reused at least 12 times with little change in oil absorbency. Owing to its excellent oil absorption performance, OAM‐T might find applications for removing oil spills and organic pollutants from water. Copyright © 2015 John Wiley & Sons, Ltd.