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Title:
ASPARTIC ACID PROTEASE TARGETED RECOGNITION PET MOLECULAR PROBE AND USE
Document Type and Number:
WIPO Patent Application WO/2024/066540
Kind Code:
A1
Abstract:
The present application relates to an aspartic acid protease targeted recognition PET molecular probe and use, which pertain to the technical field of chemistry. The present application provides a molecular probe. In the molecular probe, one glycine is added between CBT and lysine to construct an intramolecular cyclization skeleton GPN. The extended self-assembly skeleton can improve the flexibility of the compound, thereby allowing CBT to more easily undergo a click condensation reaction with the intramolecular cysteine for intramolecular condensation cyclization and making the probe less affected by high concentrations of free cysteines, further promoting the condensation cyclization of the probe and the self-assembly of aggregates from the probe in tumors to achieve a lasting high-quality visualized tumor apoptosis level. The molecular probe has good selectivity for caspase-3 and has an ability for in-vitro specific monitoring of tumor cell apoptosis. Furthermore, the molecular probe shows a good ability for monitoring of immunotherapy-induced cell apoptosis in a tumor xenograft tumor model undergoing immunotherapy.

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Inventors:
QIU LING (CN)
LIN JIANGUO (CN)
LIU QINGZHU (CN)
Application Number:
PCT/CN2023/102803
Publication Date:
April 04, 2024
Filing Date:
June 27, 2023
Export Citation:
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Assignee:
JIANGSU INST NUCLEAR MEDICINE (CN)
International Classes:
C07K7/06; A61K51/08; C07K1/13
Domestic Patent References:
WO2016065174A12016-04-28
WO2016090169A12016-06-09
Foreign References:
CN113354712A2021-09-07
US20150056137A12015-02-26
US20200085980A12020-03-19
CN113388003A2021-09-14
Other References:
LING QIU: "Rational design of caspase-responsive smart molecular probe for positron emission tomography imaging of drug-induced apoptosis", THERANOSTICS, IVYSPRING INTERNATIONAL PUBLISHER, AU, vol. 9, no. 23, 1 January 2019 (2019-01-01), AU , pages 6962 - 6975, XP093156181, ISSN: 1838-7640, DOI: 10.7150/thno.35084
Attorney, Agent or Firm:
SUNSHINE INTELLECTUAL PROPERTY INTERNATIONAL CO., LTD. (CN)
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