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Session lectures-Enzyme-triggered CO-releasing molecules (ETCORMs)

机译:会议讲座-酶触发的CO释放分子(ETCORM)

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摘要

In recent years, carbon monoxide has been recognized as an important signaling molecule in mammals. It is endogenously produced in the course of oxidative heme degradation and induces several beneficial biological effects, such as cytoprotection, vasodilation, or inhibition of inflammation [1, 2]. In the search of new therapeutically useful CO-releasing molecules, which deliver CO to a target tissue only after activation of a specific release mechanism, we have recently introduced acyloxybutadiene-Fe(CO)_3 complexes as enzyme-triggered CO-releasing molecules (ET-CORMs) [3,4]. While the esters (1) represent stable (and storable) compounds, their intracellular enzymatic cleavage leads to highly oxidation-sensitive dienol complexes of type 2, which rapidly decompose under physiological condition to liberate up to three molecules of CO together with the enone ligand (3) and Fe ions.
机译:近年来,一氧化碳已被认为是哺乳动物中重要的信号分子。它是在氧化血红素降解过程中内生产生的,并诱导了几种有益的生物学作用,例如细胞保护,血管舒张或炎症抑制[1、2]。在寻找仅在激活特定释放机制后才将CO传递至靶组织的,对治疗有用的新CO释放分子的过程中,我们最近引入了酰氧基丁二烯-Fe(CO)_3复合物作为酶触发的CO释放分子(ET -CORMs)[3,4]。尽管酯(1)代表稳定的(可储存的)化合物,但它们在细胞内的酶促裂解导致2型氧化敏感的二烯醇复合物在生理条件下迅速分解,以与烯类配体一起释放多达3个CO分子( 3)和铁离子。

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