CYCLIC PEPTIDES AS PROTEIN TARGETING AGENTS

摘要

Peptides having activity as protein binding agents are disclosed. The peptides have the following structure (I):;;including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R, R1, L1, L2, G, M, Y1 Y2 and SEQ are as defined herein. Methods associated with preparation and use of such peptides, as well as pharmaceutical compositions comprising such peptides, are also disclosed.

主权项

1. A cyclic peptide having the following structure (I): or a salt, tautomer, prodrug or stereoisomer thereof, wherein:
L1 and L2 are each individually optionally substituted linker moieties, each linker moiety optionally comprising a linkage to a solid support, a linkage to a reporter moiety, a linkage to a peptide ligand, a linkage to an azide or alkyne moiety or combinations thereof;G is a triazole, a carbon-carbon double bond or an amide;M is methionine;R is H, -L3-A or —C(═O)-L3-A, where L3 is a linker moiety and A is an alkyne, azide or a bond to a peptide ligand;R1 is H or C1-C6alkyl;Y1 and Y2 are each individually 0 or 1; andSEQ is an amino acid sequence comprising from 2 to 20 amino acids selected from natural and non-natural amino acids.