VERDINE GREGORY L,GROSSMANN TOM N,MOELLERING RAYMOND E,YEH JOHANNES TSUNG HAN,LIANG YUE,OAK YOUBEAN
申请号:
IN321/KOLNP/2012
公开号:
IN2012KN00321A
申请日:
2012.02.13
申请国别(地区):
IN
年份:
2012
代理人:
摘要:
The invention relates to bifunctional stapled or stiched peptides comprising a targeting domain, a linker moiety, and an effector domain, that can be used to tether, or to bring into close proximity, at least two cellular entities (e.g., proteins). Certain aspects relate to bifunctional stapled or stiched peptides that bind to an effector biomolecule through the effector domain and bind to a target biomolecule through the targeting domain. Polypeptides and/or polypeptide complexes that are tethered by the bifunctional stapled or stiched peptides of the invention, where the effector polypeptide bound to the effector domain of the bifunctional stapled or stiched peptide modifies or alters the target polypeptide bound to the targeting domain of the bifunctional peptide. Usesses of the inventive bifunctional stapled or stiched peptides including methods for treatment of disease (e.g., cancer, inflammatory diseases) are also provided.