Abstract: The invention discloses site-specific mono-PEGylated Exendin analogs in which any amino groups can be mono-PEGylated as well as their preparation method and use. The method of the present invention adopts a more stable protective group Dde (N-?-1-(4,4-dimethyl-2,6-dioxo-cyclohexylene)) to avoid multi-PEGylated side reactions rendered by unstable protecting groups, achieving mono-PEGylated Exendin analogs at a high recovery with a low reaction molar ratio.
Abstract: Exendins or exendin analogs modified by one or more PEG derivatives that may be linked to one or more amino acids of the exendins or exendin analogs are provided. The PEG derivatives may have branched structure set forth in any one of formulas I-IV. Compositions including the PEG derivative modified exendin or exendin analog, methods of making or administering the modified exendin or exendin analog, and various uses thereof are also provided.
Type:
Application
Filed:
November 13, 2007
Publication date:
September 23, 2010
Applicant:
Shanghai Huayi Bio-Lab Co., Ltd.
Inventors:
Wenchao Bao, Hongling Xu, Gang Yu, Yajun Zuo
Abstract: The present invention is directed to the development of novel exendin-4 derivatives exhibiting advantageous glucose-regulatory properties, and to methods of producing these derivatives, including recombinant methods in which these derivatives are produced by cleavage of a fusion protein containing multiple copies of the exendin-4 derivative peptide. The methods of the present invention can be used to simplify the process of producing the disclosed exendin-4 derivatives, thereby lowering the cost of their production.
© 2024 Justia
