Sá Jacinto, Czapla-Masztafiak Joanna, Lipiec Ewelina, Kayser Yves, Kwiatek Wojciech, Wood Bayden, Deacon Glen B, Berger Gilles, Dufrasne François, Fernandes Daniel L A, Szlachetko Jakub
Department of Chemistry, Ångström Laboratory, Uppsala University, Sweden; Institute of Physical Chemistry, Polish Academy of Sciences, Warsaw, Poland.
Institute of Nuclear Physics, Polish Academy of Sciences, PL-31342 Krakow, Poland; Paul Scherrer Institute (PSI), 5232 Villigen, Switzerland.
Drug Discov Today Technol. 2015 Sep;16:1-6. doi: 10.1016/j.ddtec.2015.07.001. Epub 2015 Sep 1.
This review presents a new application of Resonant X-ray Emission Spectroscopy (RXES) to study the mechanism of action of metal containing anticancer derivatives and in particular platinum in situ and in vivo. The technique is an example of a photon-in photon-out X-ray spectroscopic approach, which enables chemical speciation of drugs to be determined and therefore to derive action mechanisms, and to determine drug binding rates under physiological conditions and therapeutic concentrations. This is made feasible due to the atomic specificity and high penetration depth of RXES. The review presents examples of the three main types of information that can be obtained by RXES and establishes an experimental protocol to perfect the measurements within cells.
本综述介绍了共振X射线发射光谱(RXES)在研究含金属抗癌衍生物,特别是铂的原位和体内作用机制方面的新应用。该技术是一种光子入射-光子出射的X射线光谱方法,它能够确定药物的化学形态,从而推导作用机制,并在生理条件和治疗浓度下测定药物结合率。由于RXES的原子特异性和高穿透深度,这一点得以实现。本综述给出了通过RXES可获得的三种主要信息类型的示例,并建立了一个实验方案以完善细胞内的测量。