Synthesis and Biochemical Evaluation of Monocarboxylic GRB2 SH2 Domain Inhibitors.

单羧酸 GRB2SH2 结构域抑制剂的合成及生化评价 [J].

• 发表时间: 2023
• 来源期刊: Methods Mol Biol
• DOI: 10.1007/978-1-0716-3393-9_15
• PMID: 37668980
• 文章类型: Journal Article
• 作者列表: Xiao T,Zhang M,Ji H

关键词: Diastereomeric selectivity; GRB2; Inhibitors; Macrocyclic peptides; Protein–protein interactions; SH2 domain; Synthesis

Mesh: src Homology Domains; Phosphotyrosine

Abstract

This protocol discloses the synthesis of monocarboxylic inhibitors with a macrocyclic peptide scaffold to bind with the GRB2 SH2 domain and disrupt the protein-protein interactions (PPIs) between GRB2 and phosphotyrosine-containing proteins.

摘要

该方案公开了具有大环肽支架的单羧酸抑制剂的合成，以与GRB2SH2结构域结合并破坏GRB2和含磷酸酪氨酸的蛋白质之间的蛋白质-蛋白质相互作用（PPI）。