Title:
【発明の名称】ジスルフィド結合含有生物活性ペプチドの安定類似体
Document Type and Number:
Japanese Patent JPH10503205
Kind Code:
A
Abstract:
Stable analogs of cyclic peptides containing disulfide linkages are disclosed. The disulfide linkage is modified by one of four methods: (a) sulfide contraction, (b) isosteric substitution, (c) thioketal expansion, or (d) alkylation expansion. In sulfide contraction the disulfide bond (-S-S-) is replaced with a monosulfide bond (-S-) in which a bifunctional effector molecule, such as a ligand or chemotoxic agent, is bound to the new peptide linkage. In isosteric substitution, one sulfur atom is replaced with a carbon atom and at least one of the carbon atoms at the modified site is a bifunctional effector molecule. In thioketal expansion, an alkylidene unit (-CR1R2-) is inserted between the two sulfur atoms. In alkylation expansion, an alkyl moiety of from C2 to C3, is inserted between the two sulfur atoms.
Inventors:
Srinivasan, Anansachari
Lyle, Leon Earle
Rajagopalan, Ragaban
Lyle, Leon Earle
Rajagopalan, Ragaban
Application Number:
JP50582796A
Publication Date:
March 24, 1998
Filing Date:
July 18, 1995
Export Citation:
Assignee:
Marin Rod Medical Incorporated
International Classes:
A61K45/00; A61K51/00; C07K1/00; C07K7/06; C07K7/16; C07K14/52; C07K14/655; C07K14/70; A61K38/00; C09K3/00; (IPC1-7): C07K7/06; C07K14/70; C07K14/655; C07K14/52
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)