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PESIN-Homodimers Combined with Multimodal Molecular Imaging Probes for Positron Emission Tomography (PET) and Optical Imaging (OI): Suited for Tracking of GRPR-Positive Malignant Tissue.
Chemistry - A European Journal ( IF 3.9 ) Pub Date : 2020-07-03 , DOI: 10.1002/chem.202002386 Ralph Hübner 1 , Xia Cheng 2 , Björn Wängler 2 , Carmen Wängler 1
Chemistry - A European Journal ( IF 3.9 ) Pub Date : 2020-07-03 , DOI: 10.1002/chem.202002386 Ralph Hübner 1 , Xia Cheng 2 , Björn Wängler 2 , Carmen Wängler 1
Affiliation
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We describe multimodal imaging probes for gastrin‐releasing peptide receptor (GRPR)‐specific targeting suited for positron emission tomography and optical imaging (PET/OI), consisting of PESIN (PEG3‐BBN7‐14) dimers connected to multimodal imaging subunits. These multimodal agents comprise a fluorescent dye for OI and the chelator ((1,4,7‐triazacyclononane‐4,7‐diyl)diacetic acid‐1‐glutaric acid) (NODA‐GA) for PET radiometal isotope labelling. Special focus was put on the influence of the used dyes on the properties of the whole bioconjugates. For this, several compounds with different fluorescent dyes and non‐dye carrying subunits were synthesized and investigated. As fluorescent dyes, dansyl, NBD, derivatives of fluorescein, coumarin and rhodamine as well as three pyrilium‐based dyes were employed. Considerable influence of the charge of the colored unit on hydrophilicity as well as in vitro target receptor binding was observed and classified. High radiochemical yields and purities were found during radiolabeling of the multimodal imaging subunits as well as their GRPR‐specific bioconjugates with 68Ga. Examinations of the photophysical properties of both molecule species displayed no loss or alteration of fluorescence characteristics.
中文翻译：
PESIN-同二聚体与多模态分子成像探针相结合，用于正电子发射断层扫描 (PET) 和光学成像 (OI)：适合跟踪 GRPR 阳性恶性组织。
我们描述了用于胃泌素释放肽受体（GRPR）特异性靶向的多模态成像探针，适用于正电子发射断层扫描和光学成像（PET/OI），由连接到多模态成像亚基的PESIN（PEG 3 -BBN 7-14 ）二聚体组成。这些多峰试剂包含用于 OI 的荧光染料和用于 PET 放射性金属同位素标记的螯合剂（（1,4,7-三氮杂环壬烷-4,7-二基）二乙酸-1-戊二酸）（NODA-GA）。特别关注所用染料对整个生物结合物性能的影响。为此，合成并研究了几种具有不同荧光染料和非染料携带亚基的化合物。使用丹磺酰、NBD、荧光素衍生物、香豆素和罗丹明以及三种基于吡啶鎓的染料作为荧光染料。观察并分类了有色单元的电荷对亲水性以及体外靶受体结合的显着影响。在对多模态成像亚基及其68 Ga 的 GRPR 特异性生物缀合物进行放射性标记期间，发现了高放射化学产率和纯度。对两种分子种类的光物理性质的检查显示荧光特性没有损失或改变。
更新日期：2020-07-03
中文翻译：
PESIN-同二聚体与多模态分子成像探针相结合，用于正电子发射断层扫描 (PET) 和光学成像 (OI)：适合跟踪 GRPR 阳性恶性组织。
我们描述了用于胃泌素释放肽受体（GRPR）特异性靶向的多模态成像探针，适用于正电子发射断层扫描和光学成像（PET/OI），由连接到多模态成像亚基的PESIN（PEG 3 -BBN 7-14 ）二聚体组成。这些多峰试剂包含用于 OI 的荧光染料和用于 PET 放射性金属同位素标记的螯合剂（（1,4,7-三氮杂环壬烷-4,7-二基）二乙酸-1-戊二酸）（NODA-GA）。特别关注所用染料对整个生物结合物性能的影响。为此，合成并研究了几种具有不同荧光染料和非染料携带亚基的化合物。使用丹磺酰、NBD、荧光素衍生物、香豆素和罗丹明以及三种基于吡啶鎓的染料作为荧光染料。观察并分类了有色单元的电荷对亲水性以及体外靶受体结合的显着影响。在对多模态成像亚基及其68 Ga 的 GRPR 特异性生物缀合物进行放射性标记期间，发现了高放射化学产率和纯度。对两种分子种类的光物理性质的检查显示荧光特性没有损失或改变。
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