自然界中的肽,蛋白质,磷酸酯或羧酸酯的催化水解是由酶催化的,该酶是高效,快速和选择性的。迄今为止出版的大多数水解化学催化剂都模仿酶的活性位点,并含有金属络合物和氨基酸残基。它们的合成可能很费力,而与酶相比,水解活性仍然有限。我们提出了一种利用囊泡和胶束的流体膜作为两亲性添加剂的载体的方法,该两性添加剂可协同裂解芳基酯键。膜锚定的双-Zn (II)复合物1具有水解活性,并以0.9 M -1 s的二级速率常数(k 2)水解荧光素二乙酸酯(FDA)。-1。水解活性由带有共同氨基酸侧链官能团的共包埋膜添加剂调节。通过这种方法,与循环1( k 2 = 14.7 M -1 s -1)相比,系统的水解活性提高了16倍。DOPC和DSPC脂质分别在室温下形成流体或凝胶相膜。省略脂质,获得胶束溶液,其水解活性达到k 2 = 13.4 M -1 s -1。结果表明,在流体膜和胶束中有利于协同水解,使活性部分可
Synthesis And Use Of Fluorophore-Tagged Antimalarials
申请人:Lear Martin James
公开号:US20120100555A1
公开(公告)日:2012-04-26
This invention includes a fluorophore-tagged antimalarial represented by the following structural formula (1) or a salt thereof. This invention relates to the synthesis of fluorophore-tagged antimalarials and describes the synthesis of a fluorophore-tagged antimalarial. These fluorophore-tagged antimalarials can be used to image live cells to determine the location of the antimalarial in the cell, identify drug resistance and growth related pathways in
Plasmodium
isolates, identify new drug targets and chemo-sensitizers to reverse drug resistance.
US7771929B2
申请人:——
公开号:US7771929B2
公开(公告)日:2010-08-10
Cooperative hydrolysis of aryl esters on functionalized membrane surfaces and in micellar solutions
作者:M. Poznik、B. König
DOI:10.1039/c4ob00247d
日期:——
Catalytic hydrolysis of peptides, proteins, phosphates or carboxylate esters in nature is catalysed by enzymes, which are efficient, fast and selective. Most of the hydrolytic chemical catalysts published so far mimic the active site of enzymes and contain metal complexes and amino acid residues. Their synthesis can be laborious, while the hydrolytic activity is still limited compared to enzymes. We
自然界中的肽,蛋白质,磷酸酯或羧酸酯的催化水解是由酶催化的,该酶是高效,快速和选择性的。迄今为止出版的大多数水解化学催化剂都模仿酶的活性位点,并含有金属络合物和氨基酸残基。它们的合成可能很费力,而与酶相比,水解活性仍然有限。我们提出了一种利用囊泡和胶束的流体膜作为两亲性添加剂的载体的方法,该两性添加剂可协同裂解芳基酯键。膜锚定的双-Zn (II)复合物1具有水解活性,并以0.9 M -1 s的二级速率常数(k 2)水解荧光素二乙酸酯(FDA)。-1。水解活性由带有共同氨基酸侧链官能团的共包埋膜添加剂调节。通过这种方法,与循环1( k 2 = 14.7 M -1 s -1)相比,系统的水解活性提高了16倍。DOPC和DSPC脂质分别在室温下形成流体或凝胶相膜。省略脂质,获得胶束溶液,其水解活性达到k 2 = 13.4 M -1 s -1。结果表明,在流体膜和胶束中有利于协同水解,使活性部分可