公开(公告)号：US20030229017A1

公开(公告)日：2003-12-11

申请号：US10308644

申请日：2002-12-03

Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGY

Inventor： Shih-Kwang Wu ,  Ting-Gung Chang ,  Chin-Lu Tseng ,  Li-Jung Chen ,  Kae-Shyang Shih

IPC: A61K038/17 ,  C07K014/775

CPC classification number: A61K9/1271 ,  A61K38/00 ,  C07K1/04 ,  C07K1/1077 ,  C07K14/4753 ,  C07K14/48 ,  C07K14/485 ,  C07K14/49 ,  C07K14/495 ,  C07K14/50 ,  C07K14/52 ,  C07K14/57563 ,  C07K14/65 ,  C07K14/655 ,  C07K14/75 ,  C07K14/78 ,  Y02P20/55

Abstract: A solid phase synthesis method for preparing peptide-spacer-lipid conjugates, the peptide-spacer-lipid conjugates synthesized by the method, and liposomes containing the peptide-spacer-lipid conjugates. The present invention provides a convenient solid phase synthesis method for preparing peptide-spacer-lipid conjugates and provides various linkage groups (such as amide group) for conjugating peptide, spacer and lipid, wherein the spacer may comprise PEG. Several advantages can be achieved, such as the synthetic procedure can be simplified, the synthesis process can be set to automation, the purification is easier in each reaction step, and the product losses can be reduced to minimal during synthesis. The present synthesis method is suitable for preparing a wide range of peptide-spacer-lipid conjugates, provides a peptide-spacer-lipid conjugate prepared by the solid phase synthesis method of the present invention, which can be incorporated into a liposome as the targeting moiety for liposomal drug delivery to specific cells, and provides a targeting liposome containing the present peptide-spacer-lipid conjugate.