School of Natural Sciences (Chemistry), University of Tasmania, Private Bag 75, Hobart TAS 7001, Australia.
Chem Commun (Camb). 2018 Sep 13;54(74):10491-10494. doi: 10.1039/c8cc05682j.
A PtIV prodrug needs to be reduced to PtII by a biomolecule in order to show efficacy. Among biomolecules, those containing an l-Cys residue have the highest potential to be involved in reduction. Tautomerisation from HSCH2CH(NH3+)CO2- to the unusual zwitterion form -SCH2CH(NH3+)CO2H is the prerequisite for l-Cys to become a potent reductant at a low pH.
A PtIV prodrug 需要被生物分子还原为 PtII 才能显示疗效。在生物分子中，那些含有 l-Cys 残基的分子最有可能参与还原反应。HSCH2CH(NH3+)CO2- 到不寻常的两性离子形式 -SCH2CH(NH3+)CO2H 的互变异构是 l-Cys 在低 pH 值下成为有效还原剂的前提。
