期刊
MACROMOLECULAR BIOSCIENCE
卷 6, 期 11, 页码 952-958出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/mabi.200600117
关键词
biopolymers; functionalization of polymers; polymer-drug conjugate; proteins; solid-phase synthesis
This report describes the efficient conjugation of doxorubicin-glycine-phenylaianine-leucine-glycine (1a) and rhodaniine-glycine-phenylalanine-leucine-glycine (1b) units to a monodisperse elastin-mimetic polypeptide (EMM)(7) bearing eight primary amine groups for chemical attachment. The synthetic approach is based on the solid-phase synthesis of 1a and 1b followed by chemical conjugation to the elastin-mimetic polypeptide in the presence of HOBt/PyBob as activating agents to form the polypeptide conjugates 2a and 2b. Conjugation efficiency was 61.2% (4.9 doxorubicin units per polypeptide chain) for 2a and 53.7% (4.3 rhodamine units per polypeptide chain) for 2b, demonstrating the feasibility of using these tailor-made, recombinant polypeptides as potential drug carriers for cancer therapy.
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