From solution to in-cell study of the chemical reactivity of acid sensitive functional groups: a rational approach towards improved cleavable linkers for biospecific endosomal release
作者:Sylvain A. Jacques、Geoffray Leriche、Michel Mosser、Marc Nothisen、Christian D. Muller、Jean-Serge Remy、Alain Wagner
DOI:10.1039/c6ob00846a
日期:——
panel of tested chemicalfunctionalities. Even within a structural family, a slight modification of the substitution pattern has an unsuspected outcome on the hydrolysis stability. This work led us to establish a first classification of these groups based on their reactivities at pH 5.5 and their relative hydrolysis at pH 5.5 vs. pH 7.4. From this classification, four representative chemical functions were
与生理pH相比,设计用于在酸性pH下进行选择性水解的pH敏感接头可用于在其作用部位选择性释放治疗剂。在本文中,研究了许多分子结构的水解裂解,据报道它们可用于pH敏感的递送系统。在经过测试的化学官能团中发现了各种各样的水解稳定性。即使在一个结构家族中,对取代模式的轻微修饰也会在水解稳定性方面产生意想不到的结果。这项工作使我们基于这些基团在pH 5.5时的反应性和在pH 5.5 vs. 5时的相对水解建立了这些基团的第一个分类。pH值7.4。从该分类中,选择了四个代表性的化学功能并进行了体外研究。结果表明,根据流式细胞仪测量,只有最活跃的功能才发生了明显的溶酶体裂解。这些最新结果质疑已知药物释放系统的基于酸的作用机理,并主张采用量身定制的方法进行深入的结构反应性研究对于合理设计和开发生物反应性接头的重要性。
DNA CONTROLLED ASSEMBLY OF LIPID MEMBRANES
申请人:Vogel Stefan
公开号:US20100144848A1
公开(公告)日:2010-06-10
The present invention relates to detection of target nucleic acids by target nucleic acid induced liposome assembly. The invention provides oligonucleotides for use in detection and a method of detecting target nucleic acids. Other aspects of the invention are use of the oligonucleotide of the invention for detection, a kit for detection, a method of treatment comprising administrating the oligonucleotide of the invention and a pharmaceutical composition comprising the oligonucleotide of the invention.
MRI Sensing of Neurotransmitters with a Crown Ether Appended Gd<sup>3+</sup> Complex
作者:Fatima Oukhatar、Sandra Même、William Même、Frédéric Szeremeta、Nikos K. Logothetis、Goran Angelovski、Éva Tóth
DOI:10.1021/cn500289y
日期:2015.2.18
zwitterionic neurotransmitters that generate an MR signal change upon neurotransmitter binding. The gadoliniumcomplex (GdL) we report offers ditopic binding for zwitterionic amino acid neurotransmitters, via interactions (i) between the positively charged and coordinatively unsaturated metal center and the carboxylate function and (ii) between a triazacrown ether and the amine group of the neurotransmitters
PAG-Trz-Cl, have been developed. PAG-Trz-Cls were synthesized using a chlorotriazine with an acrylamide moiety, acrylamide, and N,N'-methylenebisacrylamide via both precipitation and solution polymerization. Because PAG-Trz-Cls adequately swell in aqueousmedia, the amidation between polar carboxylic acids and amines afforded the corresponding amides in good yields.