Title:
USE OF VPS18-TARGETING RICCARDIN D-N(RDN) IN TUMOR IMMUNOTHERAPY
Document Type and Number:
WIPO Patent Application WO/2023/060727
Kind Code:
A1
Abstract:
A use of VPS18-targeting Riccardin D-N(RDN) in tumor immunotherapy, which solves the current problem of poor sensitivity of an existing immune checkpoint inhibitor. Existing small-molecule inhibitors reducing PD-L1 expression still have the problem of tumor immune evasion in an action process. RDN has significant activity in combating cancer and reversing tumor resistance, and has low toxicity. Meanwhile, in-vivo and in-vitro experiments prove that RDN significantly down-regulates the expression of PD-L1, becomes a novel small-molecule inhibitor for blocking PD-1/PD-L1 signals, and has application prospects in reversing tumor immune evasion and sensitizing immune checkpoint inhibitors.
Inventors:
LOU HONGXIANG (CN)
YUAN HUIQING (CN)
NIU HUANMIN (CN)
SUN BIN (CN)
QIAN LILIN (CN)
YUAN HUIQING (CN)
NIU HUANMIN (CN)
SUN BIN (CN)
QIAN LILIN (CN)
Application Number:
PCT/CN2021/135496
Publication Date:
April 20, 2023
Filing Date:
December 03, 2021
Export Citation:
Assignee:
UNIV SHANDONG (CN)
UNIV SHANDONG 2ND HOSPITAL (CN)
UNIV SHANDONG 2ND HOSPITAL (CN)
International Classes:
A61K31/40; A61K31/335; A61K31/435; A61K31/5375; A61P35/00; A61P37/04
Foreign References:
| CN102127050A | 2011-07-20 | |||
| CN107011312A | 2017-08-04 |
Other References:
GAO, YANHUI ET AL.: "Determination of the in vitro metabolic stability and metabolites of the anticancer derivative riccardin D-N in human and mouse hepatic S9 fractions using HPLC-Q-LIT-MS", JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, vol. 174, 1 July 2019 (2019-07-01), XP085750158, DOI: 10.1016/j.jpba.2019.06.045
LI LIN, SUN BIN, GAO YUN, NIU HUANMIN, YUAN HUIQING, LOU HONGXIANG: "STAT3 contributes to lysosomal-mediated cell death in a novel derivative of riccardin D-treated breast cancer cells in association with TFEB", BIOCHEMICAL PHARMACOLOGY, ELSEVIER, US, vol. 150, 1 April 2018 (2018-04-01), US , pages 267 - 279, XP093057324, ISSN: 0006-2952, DOI: 10.1016/j.bcp.2018.02.026
SUN BIN, LIU JUN, GAO YUN, ZHENG HONG-BO, LI LIN, HU QING-WEN, YUAN HUI-QING, LOU HONG-XIANG: "Design, synthesis and biological evaluation of nitrogen-containing macrocyclic bisbibenzyl derivatives as potent anticancer agents by targeting the lysosome", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, ELSEVIER, AMSTERDAM, NL, vol. 136, 1 August 2017 (2017-08-01), AMSTERDAM, NL , pages 603 - 618, XP093057323, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2017.05.050
LI LIN, SUN BIN, GAO YUN, NIU HUANMIN, YUAN HUIQING, LOU HONGXIANG: "STAT3 contributes to lysosomal-mediated cell death in a novel derivative of riccardin D-treated breast cancer cells in association with TFEB", BIOCHEMICAL PHARMACOLOGY, ELSEVIER, US, vol. 150, 1 April 2018 (2018-04-01), US , pages 267 - 279, XP093057324, ISSN: 0006-2952, DOI: 10.1016/j.bcp.2018.02.026
SUN BIN, LIU JUN, GAO YUN, ZHENG HONG-BO, LI LIN, HU QING-WEN, YUAN HUI-QING, LOU HONG-XIANG: "Design, synthesis and biological evaluation of nitrogen-containing macrocyclic bisbibenzyl derivatives as potent anticancer agents by targeting the lysosome", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, ELSEVIER, AMSTERDAM, NL, vol. 136, 1 August 2017 (2017-08-01), AMSTERDAM, NL , pages 603 - 618, XP093057323, ISSN: 0223-5234, DOI: 10.1016/j.ejmech.2017.05.050
Attorney, Agent or Firm:
JINAN SHENGDA INTELLECTUAL PROPERTY AGENCY CO., LTD. (CN)
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