Stapled and stitched polypeptides and uses thereof

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专利权人:

President and Fellows of Harvard College

发明人:

Gregory L. Verdine,Gerard Hilinski

申请号：

US14775315

公开号：

US10081654B2

申请日:

2014.03.13

申请国别(地区):

US

年份:

2018

代理人:

摘要：

The present invention provides stapled polypeptides of the Formulae (I) and (VI): (I) (VI) and salts thereof； wherein the groups ； R1a, R1b, R1c, R2a, R3a, R2b, R3b, R4a, R4b, RA, RZ, L1a, L1b, L2, L3, XAA, v, w, p, m, s, n, t, and q are as defined herein. The present invention further provides methods of preparing the inventive stapled polypeptides from unstapled polypeptide precursors. The present invention further provides pharmaceutical compositions comprising a stapled polypeptide of Formula (I) or (VI), and methods of using the stapled peptides. The present invention also provides modifications of the staples post ring closing metathesis.

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