Laboratoire des Biomolécules, LBM, Département de Chimie, Ecole Normale Supérieure, PSL University, Sorbonne Université, CNRS, 75005 Paris, France.
Département de Chimie, Ecole Normale Supérieure, PSL University, 75005 Paris, France.
Molecules. 2022 Aug 26;27(17):5476. doi: 10.3390/molecules27175476.
Catalase mimics are low molecular weight metal complexes that reproduce the activity of catalase, an antioxidant metalloprotein that participates in the cellular regulation of HO concentration by catalyzing its dismutation. HO is a reactive oxygen species that is vital for the normal functioning of cells. However, its overproduction contributes to oxidative stress, which damages cells. Owing to their biocompatibility, peptidyl complexes are an attractive option for clinical applications to regulate HO by enzyme mimics. We report here the synthesis and characterization of four new peptidyl di-copper complexes bearing two coordinating sequences. Characterization of the complexes showed that, depending on the linker used between the two coordinating sequences, their catalytic activity for HO dismutation, their thermodynamic stability and their resistance to HO degradation are very different, with (CATm2)Cu being the most promising catalyst.
过氧化氢酶模拟物是具有低分子量的金属配合物，可复制过氧化氢酶的活性，过氧化氢酶是一种抗氧化金属蛋白，通过催化其歧化作用参与 HO 浓度的细胞调节。HO 是一种活性氧，对细胞的正常功能至关重要。然而，其过度产生会导致氧化应激，从而损害细胞。由于其生物相容性，肽基配合物是通过酶模拟物来调节 HO 的临床应用的有吸引力的选择。我们在此报告了四种新的肽二铜配合物的合成和表征，这些配合物具有两个配位序列。配合物的表征表明，根据两个配位序列之间使用的连接子，它们对 HO 歧化的催化活性、热力学稳定性以及对 HO 降解的抗性差异很大，其中（CATm2）Cu 是最有前途的催化剂。
