单羧酸 GRB2 SH2 结构域抑制剂的合成与生化评价。
Synthesis and Biochemical Evaluation of Monocarboxylic GRB2 SH2 Domain Inhibitors.
机构信息
Drug Discovery Department, H. Lee Moffitt Cancer Center & Research Institute, Tampa, FL, USA.
Departments of Oncologic Sciences and Chemistry, University of South Florida, Tampa, FL, USA.
出版信息
Methods Mol Biol. 2023;2705:269-290. doi: 10.1007/978-1-0716-3393-9_15.
PMID:37668980
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
本方案揭示了具有大环肽支架的单羧酸抑制剂的合成，以与 GRB2 SH2 结构域结合并破坏 GRB2 和含磷酸酪氨酸蛋白之间的蛋白质-蛋白质相互作用（PPIs）。
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