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用于细胞死亡正电子发射断层显像(PET)成像的二硫醇反应性探针的制备

Preparation of a Dithiol-Reactive Probe for PET Imaging of Cell Death.

作者信息

Ho Shon Ivan, Gotsbacher Michael P, Guille Jennifer, Kumar Divesh, Codd Rachel, Hogg Philip

机构信息

Department of Nuclear Medicine and PET, Prince of Wales Hospital, Randwick, NSW, Australia.

Prince of Wales Clinical School, University of New South Wales, Sydney, NSW, Australia.

出版信息

Methods Mol Biol. 2019;1967:295-304. doi: 10.1007/978-1-4939-9187-7_19.

DOI:10.1007/978-1-4939-9187-7_19
PMID:31069779
Abstract

Conjugates of 4-(N-(S-glutathionylacetyl)amino)phenylarsonous acid (GSAO) with optical or radionuclide probes are able to image cell death in vivo. GSAO conjugates are retained in the cytosol of dying and dead cells via the formation of covalent bonds between the As(III) ion and the thiol groups of proximal cysteine residues. Here we describe the method for preparing a NODAGA-GSAO conjugate and its radiolabeling with gallium-68 (Ga-NODAGA-GSAO) for positron-emission tomography (PET) imaging of cell death.

摘要

4-(N-(S-谷胱甘肽乙酰基)氨基)苯亚胂酸(GSAO)与光学或放射性核素探针的缀合物能够在体内对细胞死亡进行成像。GSAO缀合物通过As(III)离子与近端半胱氨酸残基的硫醇基团之间形成共价键而保留在垂死和死亡细胞的胞质溶胶中。在此,我们描述了制备NODAGA-GSAO缀合物及其用镓-68(Ga-NODAGA-GSAO)进行放射性标记以用于细胞死亡的正电子发射断层扫描(PET)成像的方法。

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