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公开(公告)号：US20240042068A1
公开(公告)日：2024-02-08
申请号：US18329245
申请日：2023-06-05
Inventor： Min Chen , Yunfeng Cheng , Jianghong Rao , Zixin Chen , Jinghang Xie
CPC classification number: A61K51/088 , C07K5/1021 , C07K5/101
Abstract: Embodiments of the synthesis, radiolabeling and biological applications of an activatable tracer that undergoes intramolecular cyclization and aggregation upon activation by cleavage of a blocking moiety are provided. The probes of the disclosure allow for target-controlled self-assembly of small molecules in living subjects for imaging and drug delivery. The aggregated nanoprobes of the disclosure may be detectable optically, by PET detection, magnetic resonance imaging, and the like depending on the detectable reporter attached to the nanoprobe.
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公开(公告)号：US20170044593A1
公开(公告)日：2017-02-16
申请号：US15001591
申请日：2016-01-20
Inventor： Jianghong Rao , Yunfeng Cheng , Jinghang Xie
IPC: C12Q1/68 , C07D501/36 , C07D501/32
CPC classification number: C09B11/24 , C07D501/32 , C07D501/36 , C12Q1/689
Abstract: The compositions of the present disclosure provide novel fluorogenic probes for use in the specific imaging and detection of mycobacteria species, and in particular β-lactam-antibiotic resistant. Specificity for mycobacteria is conferred on these probes by incorporating a moiety that specifically targets the unique trapping mechanism of the DprE1 found in in mycobacteria. Accordingly, only Mycobacteria species that express both a β-lactamase and DprE1 enable both the activation of the caged fluorescent probe, and the affixing of the released fluorescent probes to the bacteria cells through the functioning reduction-covalent binding mechanism. Advantageously, such a probe is able, at its most sensitive, to allow single mycobacterium detection.
Abstract translation: 本公开的组合物提供用于特异性成像和检测分枝杆菌物种，特别是β-内酰胺抗生素抗性的新型荧光探针。 通过引入特异性靶向分枝杆菌中发现的DprE1的独特诱捕机制的部分，赋予这些探针的特异性。 因此，只有表达β-内酰胺酶和DprE1的分枝杆菌属物种能使活化的笼养的荧光探针和通过功能还原 - 共价结合机制将释放的荧光探针附着到细菌细胞。 有利地，这种探针能够在其最敏感的情况下允许单次分枝杆菌检测。
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公开(公告)号：US10370538B2
公开(公告)日：2019-08-06
申请号：US15001591
申请日：2016-01-20
Inventor： Jianghong Rao , Yunfeng Cheng , Jinghang Xie
IPC: C07D501/52 , C09B11/24 , C12Q1/689 , C07D501/32 , C07D501/36
Abstract: The compositions of the present disclosure provide novel fluorogenic probes for use in the specific imaging and detection of mycobacteria species, and in particular β-lactam-antibiotic resistant. Specificity for mycobacteria is conferred on these probes by incorporating a moiety that specifically targets the unique trapping mechanism of the DprE1 found in in mycobacteria. Accordingly, only Mycobacteria species that express both a β-lactamase and DprE1 enable both the activation of the caged fluorescent probe, and the affixing of the released fluorescent probes to the bacteria cells through the functioning reduction-covalent binding mechanism. Advantageously, such a probe is able, at its most sensitive, to allow single mycobacterium detection.
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