申请人:Saxon Eliana
公开号:US20080214801A1
公开(公告)日:2008-09-04
The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
本发明涉及一种可在生理条件下进行的化学选择性连接反应。一般而言,该发明涉及特别设计的膦化合物的缩合反应,该膦化合物可以提供在两个反应物之间形成酰胺键的反应,从而产生包含膦基团的最终产物,或者可以被设计成包含可切断的连接剂,以便将膦的取代基转移到偶氮化物上,释放氧化的膦副产物并在最终产物中产生天然的酰胺键。该反应的选择性及其与水环境的兼容性使其适用于体内应用(例如,在细胞表面或细胞内)和体外应用(例如,合成肽和其他聚合物,生产修饰(例如,标记)的氨基酸)。