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Stabilized compounds having secondary structure motifs
专利权人:
President and Fellows of Harvard College
发明人:
Gregory L. Verdine,Christian E. Schafmeister
申请号:
US15287513
公开号:
US09951099B2
申请日:
2016.10.06
申请国别(地区):
US
年份:
2018
代理人:
摘要:
The present invention provides novel stabilized crosslinked compounds having secondary structure motifs, libraries of these novel compounds, and methods for the synthesis of these compounds libraries thereof. The synthesis of these novel stabilized compounds involves (1) synthesizing a peptide from a selected number of natural or non-natural amino acids, wherein the peptide comprises at least two moieties capable of undergoing reaction to promote carbon-carbon bond formation; and (2) contacting the peptide with a reagent to generate at least one crosslinker and to effect stabilization of a secondary structure motif. The present invention, in a preferred embodiment, provides stabilized p53 donor helical peptides. Additionally, the present invention provides methods for disrupting the p53/MDM2 binding interaction comprising (1) providing a crosslinked stabilized α-helical structure; and (2) contacting the crosslinked stabilized α-helical structure with MDM2.
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中国工程科技知识中心
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