摘要：Several novel fluorescent probes targeting α_1-adrenergic receptors were well designed and synthesized by conjugating phenylpiperazine pharmacophore with coumarin and fluorescein fluorophores. These compounds showed suitable fluorescence property, high receptor affinity, and low cytotoxicity. Moreover, the cell imaging results displayed that these probes can be effective tools for the real-time detection of ligand-receptor interactions, as well as the visualization and location of α_1-adrenergic receptors in living cells.

摘要：Hydrophobic fluorescence:Tan and his colleagues recently introduced a brand new chemotype of environment-sensitive fluorescent turn-on probes to detect the hydrophobic ligand-binding domain by using SBD *** design strategy described in this report generalized the environment sensitivity turn-on mechanism to recognize a specific protein,which provides a robust breakthrough for interchanging fluorescence in conventional small-molecule fluorescent imaging.

摘要：This paper presents a series of first- and second-generation click-modified coumarin-based fluorescent probes for thiols. These molecules demonstrate high turn-on fluorescent response and good selectivity towards aromatic thiols over other relevant reac- tive sulfur species, reactive oxygen species and common nucleophiles. Moreover, probe la can detect thiols in the reduced rabbit plasma sample. Therefore, this approach provides a particularly impressive tool for detecting thiol in biological systems.

摘要：旨在验证牛INTS11基因在成肌细胞中的功能作用,通过生物信息学分析探讨INTS11的CDS区序列及其编码蛋白的特征,并使用不同分子试验技术验证其在牛成肌细胞增殖过程中发挥的作用。本研究对牛INTS11基因序列与其他物种进行同源性对比并构建生物进化树,对其编码蛋白进行理化性质和功能结构分析以及亚细胞定位。并以体外分离培养的3月龄健康胎牛成肌细胞为试验材料,克隆成肌细胞中INTS11的全部CDS区序列,构建INTS11的过表达载体并设计基因的干扰序列,通过CCK8、Edu、RT-qPCR等技术探究其对成肌细胞增殖的影响。生物信息分析结果表明,CDS区序列全长为1800 bp,具有MBL-foldmetallo-hydro和β-CASP基序两个功能结构域,属于非跨膜蛋白,且细胞定位主要分布于细胞质。在成肌细胞中转染pcDNA3.1-INTS11质粒,结果显示在72~96 h时试验组的成肌细胞比对照组的增殖速度显著增加(P<0.05);Edu试验发现阳性细胞数目显著增加(P<0.05);RT-qPCR结果表明增殖标志因子CDK2、CYCLIND1的mRNA表达水平与对照组相比显著上升(P<0.05)。转入干扰序列后,细胞增殖速度显著下降(P<0.05),同时增殖标志因子CDK2、cyclin D1的mRNA表达水平与对照组相比显著下降(P<0.05)。本研究预测了INTS11在家养动物中的保守性,并且INTS11蛋白具有两个功能结构域,发现其通过介导CDK2、CYCLIND1的mRNA转录促进牛成肌细胞增殖,其结果完善了调控骨骼肌的基因网络,为后序探讨调控骨骼肌生长机制提供理论支持。