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作为钡分子受体的改性杯[4]冠醚

Modified Calix[4]crowns as Molecular Receptors for Barium.

作者信息

Steinberg Janine, Bauer David, Reissig Falco, Köckerling Martin, Pietzsch Hans-Jürgen, Mamat Constantin

机构信息

Institut für Radiopharmazeutische Krebsforschung Helmholtz-Zentrum Dresden-Rossendorf Bautzner Landstraße 400 01328 Dresden Germany.

Fakultät Chemie und Lebensmittelchemie TU Dresden 01062 Dresden Germany.

出版信息

ChemistryOpen. 2018 May 15;7(6):431. doi: 10.1002/open.201800065. eCollection 2018 Jun.

Abstract

Invited for this month's cover picture is the group around Dr. Constantin Mamat at the Institute of Radiopharmaceutical Cancer Research at the Helmholtz-Zentrum Dresden-Rossendorf (Germany) together with Prof. Martin Köckerling from the University of Rostock (Germany). The cover picture shows the ability of special functionalized calix[4]crown-6 derivatives to stably bind group 2 metals like barium. This binding mode is highly important for radiopharmaceutical applications not to lose the respective radiometal in vivo to avoid high background signals and/or false positive results and damages in other tissues. For this purpose, different calix[4]crowns were tested, based upon their potential to stably bind barium as surrogate for radium. Radium nuclides are known to be good candidates for usage in α-targeted therapies. Currently, radium-223 is used for α-therapy of bone metastases because of its calcium mimetics. Our aim is to apply the radium to treat other cancer tissues. That's why we need novel chelators to stably fix groups 2 metals like barium and radium. Read the full text of their Full Paper at https://doi.org/10.1002/open.201800019.

摘要

本期封面图片的受邀者是德国亥姆霍兹-德累斯顿-罗森多夫研究所放射性药物癌症研究部的康斯坦丁·马马特博士团队,以及德国罗斯托克大学的马丁·柯克林教授。封面图片展示了特殊功能化杯[4]冠-6衍生物稳定结合钡等第2族金属的能力。这种结合模式对于放射性药物应用非常重要,可避免体内相应放射性金属流失,从而避免高背景信号和/或假阳性结果以及对其他组织的损害。为此,基于其稳定结合钡作为镭替代物的潜力,对不同的杯[4]冠进行了测试。镭核素是α靶向治疗的良好候选者。目前,镭-223因其钙模拟物而用于骨转移的α治疗。我们的目标是将镭应用于治疗其他癌症组织。这就是为什么我们需要新型螯合剂来稳定固定钡和镭等第2族金属。可在https://doi.org/10.1002/open.201800019阅读他们的全文。

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