Pharmaceutical compositions are provided for extending the serum half-life of a therapeutic agent. The composition may include a strained alkyne-labeled therapeutic agent. Also provided is a strained alkyne-carrier protein adduct including a vinyl thioether-linkage to a cysteine residue of the carrier protein. Methods of chemoselectively modifying a carrier protein are provided, that include conjugating a cysteine residue of a carrier protein with a cyclooctyne-labeled cargo agent to produce a vinyl thioether-linked conjugate. Also provided is a method of increasing the in vivo half-life of a bioactive agent including administering a strained alkyne-labeled bioactive agent to a subject.
提供了用于延长治疗剂血清半衰期的药物组合物。该组合物可包括一种经过拉伸的
炔烃标记的治疗剂。此外,还提供了一种含
乙烯基硫醚连接载体蛋白半胱
氨酸残基的受约束
炔烃-载体蛋白加合物。提供了
化学选择性修饰载体蛋白的方法,其中包括将载体蛋白的半胱
氨酸残基与
环辛炔标记的货物制剂共轭,生成
乙烯基硫醚连接的共轭物。此外,还提供了一种增加
生物活性剂体内半衰期的方法,包括向受试者施用经拉伸的炔类标记
生物活性剂。