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1. (WO1997009344) LIBRAIRIES OF BACKBONE-CYCLIZED PEPTIDOMIMETICS

Pub. No.:    WO/1997/009344    International Application No.:    PCT/IL1996/000091
Publication Date: Mar 13, 1997 International Filing Date: Aug 28, 1996
IPC: C07K 1/04
C07K 14/00
C07K 14/655
G01R 31/3185
Applicants: PEPTOR LIMITED
YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
HORNIK, Vered
GILON, Chaim
Inventors: HORNIK, Vered
GILON, Chaim
Title: LIBRAIRIES OF BACKBONE-CYCLIZED PEPTIDOMIMETICS
Abstract:
Libraries of novel backbone-cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units used in the synthesis of these backbone-cyclized peptide analogs are Nα (φ-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these Nα (φ-functionalized) amino acids are incorporated into a library of peptide sequences, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is exemplified by libraries of backbone-cyclized bradykinin analogs, somatostatin analogs, BPI analogs and Substance P analogs having biological activity. Further embodiments of the invention are Interleukin-6 receptor derived peptides having ring structures involving backbone cyclization.