Libraries of backbone-cyclized peptidomimetics

Details Libraries of backbone-cyclized peptidomimetics Libraries of backbone-cyclized peptidomimetics

1995-12-07

2000-09-12

Celsa, Bennett

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Cyclic peptides

530333, 436501, A61K 3812, A61K 3800, C07K 1046

Patent

active

061179744

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 N(((-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N(((-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.

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