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  1. Article ; Online: Corrigendum to "Therapeutic potential of fucosyltransferases in cancer and recent development of targeted inhibitors" [Drug Discov. Today 28(1) (2023) 103394].

    Lv, Yixin / Zhang, Zhoudong / Tian, Sheng / Wang, Weipeng / Li, Huanqiu

    Drug discovery today

    2022  Volume 28, Issue 3, Page(s) 103484

    Language English
    Publishing date 2022-12-29
    Publishing country England
    Document type Published Erratum
    ZDB-ID 1324988-5
    ISSN 1878-5832 ; 1359-6446
    ISSN (online) 1878-5832
    ISSN 1359-6446
    DOI 10.1016/j.drudis.2022.103484
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4725: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  2. Article ; Online: Therapeutic potential of fucosyltransferases in cancer and recent development of targeted inhibitors.

    Lv, Yixin / Zhang, Zhoudong / Tian, Sheng / Wang, Weipeng / Li, Huanqiu

    Drug discovery today

    2022  Volume 28, Issue 1, Page(s) 103394

    Abstract: Fucosyltransferases (FUTs) have significant roles in various pathophysiological events. Their high expression is a signature of malignant cell transformation, contributing to many abnormal events during cancer development, such as uncontrolled cell ... ...

    Abstract Fucosyltransferases (FUTs) have significant roles in various pathophysiological events. Their high expression is a signature of malignant cell transformation, contributing to many abnormal events during cancer development, such as uncontrolled cell proliferation, tumor cell invasion, angiogenesis, metastasis, immune evasion, and therapy resistance. Therefore, FUTs have evolved as an attractive therapeutic target for treating solid cancers, and many substrate analogs have been discovered with potential as FUT inhibitors for cancer therapy. Meanwhile, the development of FUT protein structures represents a significant advance in the design of FUT inhibitors with nonsubstrate structures. In this review, we summarize the role of FUTs in cancers, the resolved protein crystal structures and progress in the development of FUT inhibitors as cancer therapeutics.
    MeSH term(s) Humans ; Fucosyltransferases/chemistry ; Fucosyltransferases/metabolism ; Glycosylation ; Neoplasms/drug therapy ; Cell Proliferation
    Chemical Substances Fucosyltransferases (EC 2.4.1.-)
    Language English
    Publishing date 2022-10-09
    Publishing country England
    Document type Journal Article ; Review ; Research Support, Non-U.S. Gov't
    ZDB-ID 1324988-5
    ISSN 1878-5832 ; 1359-6446
    ISSN (online) 1878-5832
    ISSN 1359-6446
    DOI 10.1016/j.drudis.2022.103394
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4725: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  3. Article ; Online: LSD1 inhibitors for anticancer therapy: a patent review (2017-present).

    Lv, Yi-Xin / Tian, Sheng / Zhang, Zhou-Dong / Feng, Tao / Li, Huan-Qiu

    Expert opinion on therapeutic patents

    2022  Volume 32, Issue 9, Page(s) 1027–1042

    Abstract: Introduction: Lysine-specific demethylase 1 (LSD1), which belongs to the demethylase of non-histone proteins, is believed to promote cancer cell proliferation and metastasis by modifying histones. LSD1 dysfunction may play a key role in a variety of ... ...

    Abstract Introduction: Lysine-specific demethylase 1 (LSD1), which belongs to the demethylase of non-histone proteins, is believed to promote cancer cell proliferation and metastasis by modifying histones. LSD1 dysfunction may play a key role in a variety of cancers, such as acute myeloid leukemia and non-small cell lung cancer, indicating that LSD1 is a promising epigenetic target for cancer therapy. Many different types of small molecule LSD1 inhibitors have been developed and shown to inhibit tumor cell proliferation, invasion, and migration, providing a new treatment strategy for solid tumors.
    Areas covered: This review summarizes the progress of LSD1 inhibitor research in the last four years, including selected new patents and article publications, as well as the therapeutic potential of these compounds.
    Expert opinion: Natural products offer a promising prospect for developing novel potent LSD1 inhibitors, as structural design and activity of irreversible and reversible inhibitors have been continuously optimized since the discovery of the LSD1 target in 2004. The use of 'microtubule-binding agents' and 'dual-agent combination' has recently become a new anticancer technique, reducing the resistance and adverse reactions of traditional drugs. Several microtubule-binding drugs have been used successfully in clinical practice, providing structural scaffolds and new ideas for the development of safer drugs.
    MeSH term(s) Carcinoma, Non-Small-Cell Lung ; Enzyme Inhibitors/pharmacology ; Histone Demethylases ; Histones/chemistry ; Histones/metabolism ; Humans ; Lung Neoplasms ; Patents as Topic
    Chemical Substances Enzyme Inhibitors ; Histones ; Histone Demethylases (EC 1.14.11.-)
    Language English
    Publishing date 2022-08-09
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 1186201-4
    ISSN 1744-7674 ; 0962-2594 ; 1354-3776
    ISSN (online) 1744-7674
    ISSN 0962-2594 ; 1354-3776
    DOI 10.1080/13543776.2022.2109332
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 3962: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
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    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  4. Article ; Online: Discovery of Selective P2Y

    Zhu, Yifan / Zhou, Mengze / Cheng, Xiangyu / Wang, Hui / Li, Yehong / Guo, Yueyue / Wang, Yaxuan / Tian, Sheng / Mao, Tianqi / Zhang, Zhoudong / Li, Duxin / Hu, Qinghua / Li, Huanqiu

    Journal of medicinal chemistry

    2023  Volume 66, Issue 9, Page(s) 6315–6332

    Abstract: As a member of purinoceptors, the ... ...

    Abstract As a member of purinoceptors, the P2Y
    MeSH term(s) Animals ; Mice ; Colitis/chemically induced ; Colitis/drug therapy ; Colitis, Ulcerative/chemically induced ; Colitis, Ulcerative/drug therapy ; Dextran Sulfate ; Inflammasomes/metabolism ; Mice, Inbred C57BL ; NLR Family, Pyrin Domain-Containing 3 Protein
    Chemical Substances Dextran Sulfate (9042-14-2) ; Inflammasomes ; NLR Family, Pyrin Domain-Containing 3 Protein ; purinoceptor P2Y6
    Language English
    Publishing date 2023-04-20
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.3c00210
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.B 151: Show issues Location:
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    ab Jg. 2022: Lesesaal (EG)
    Zs.MB 1: Show issues

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  5. Article ; Online: Network pharmacology-based analysis of Jin-Si-Wei on the treatment of Alzheimer's disease.

    Zhi, Jiayi / Yin, Li / Zhang, Zhoudong / Lv, Yaozhong / Wu, Fan / Yang, Yang / Zhang, Enming / Li, Huanqiu / Lu, Ning / Zhou, Mengze / Hu, Qinghua

    Journal of ethnopharmacology

    2023  Volume 319, Issue Pt 3, Page(s) 117291

    Abstract: Ethnopharmacological relevance: Jin-Si-Wei (JSW), a traditional Chinese medicine (TCM) formula, have cognitive enhancing effect and delay the memory decline in an animal model of AD， which has been reported. However, the therapeutic mechanism of JSW in ... ...

    Abstract Ethnopharmacological relevance: Jin-Si-Wei (JSW), a traditional Chinese medicine (TCM) formula, have cognitive enhancing effect and delay the memory decline in an animal model of AD， which has been reported. However, the therapeutic mechanism of JSW in the treatment of AD remains unclear.
    Aim of the study: This study aimed to verify the pharmacodynamics of JSW in the treatment of AD, and to explore its potential mechanism based on network pharmacology, molecular docking and experimental validation both in vitro and in vivo.
    Materials and methods: In this study, the underlying mechanism of JSW against AD was investigated by the integration of network pharmacology. Then, the core pathways and biological process of JSW were verified by experiment, including behavioral test and pathological and biochemical assays with 6-month-old APP
    Results: A Drug-Ingredient-Target network was established, which included 363 ingredients and 116 targets related to the JSW treatment of AD. The main metabolic pathway of JSW treatment for AD is neuroactive ligand-receptor interaction pathway, and biological processes are mainly involved in Aβ metabolic process. In vivo experiments, compared with APP/PS1 mice, the cognitive and memory ability of mice was significantly improved after JSW administration. In brain tissue of APP/PS1 mice, JSW could increase the contents of low-density lipoprotein receptor-related protein 1 (LRP-1), enkephalinase (NEP) and Acetyl choline (ACh), and decrease the contents of Aβ
    Conclusions: JSW improves AD in APP/PS1 mice, and this therapeutic effect may be achieved in part by altering the neuroactive ligand-receptor interaction pathway.
    MeSH term(s) Humans ; Animals ; Mice ; Alzheimer Disease/drug therapy ; Ligands ; Molecular Docking Simulation ; Network Pharmacology ; Neuroblastoma ; Amyloid beta-Protein Precursor/genetics ; Amyloid Precursor Protein Secretases
    Chemical Substances Ligands ; Amyloid beta-Protein Precursor ; Amyloid Precursor Protein Secretases (EC 3.4.-)
    Language English
    Publishing date 2023-11-02
    Publishing country Ireland
    Document type Journal Article
    ZDB-ID 134511-4
    ISSN 1872-7573 ; 0378-8741
    ISSN (online) 1872-7573
    ISSN 0378-8741
    DOI 10.1016/j.jep.2023.117291
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 1494: Show issues Location:
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    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

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  6. Article ; Online: FDW028, a novel FUT8 inhibitor, impels lysosomal proteolysis of B7-H3 via chaperone-mediated autophagy pathway and exhibits potent efficacy against metastatic colorectal cancer.

    Wang, Mengmeng / Zhang, Zhoudong / Chen, Mengxi / Lv, Yixin / Tian, Sheng / Meng, Fanyi / Zhang, Yawen / Guo, Xuqin / Chen, Yinshuang / Yang, Man / Li, Jiawei / Qiu, Tian / Xu, Fang / Li, Zhi / Zhang, Qi / Yang, Jie / Sun, Jing / Zhang, Hongjian / Zhang, Haiyang /
    Li, Huanqiu / Wang, Weipeng

    Cell death & disease

    2023  Volume 14, Issue 8, Page(s) 495

    Abstract: Metastatic colorectal cancer (mCRC) is a major cause of cancer-related mortality due to the absence of effective therapeutics. Thus, it is urgent to discover new drugs for mCRC. Fucosyltransferase 8 (FUT8) is a potential therapeutic target with high ... ...

    Abstract Metastatic colorectal cancer (mCRC) is a major cause of cancer-related mortality due to the absence of effective therapeutics. Thus, it is urgent to discover new drugs for mCRC. Fucosyltransferase 8 (FUT8) is a potential therapeutic target with high level in most malignant cancers including CRC. FUT8 mediates the core fucosylation of CD276 (B7-H3), a key immune checkpoint molecule (ICM), in CRC. FUT8-silence-induced defucosylation at N104 on B7-H3 attracts heat shock protein family A member 8 (HSPA8, also known as HSC70) to bind with 106-110 SLRLQ motif and consequently propels lysosomal proteolysis of B7-H3 through the chaperone-mediated autophagy (CMA) pathway. Then we report the development and characterization of a potent and highly selective small-molecule inhibitor of FUT8, named FDW028, which evidently prolongs the survival of mice with CRC pulmonary metastases (CRPM). FDW028 exhibits potent anti-tumor activity by defucosylation and impelling lysosomal degradation of B7-H3 through the CMA pathway. Taken together, FUT8 inhibition destabilizes B7-H3 through CMA-mediated lysosomal proteolysis, and FDW028 acts as a potent therapeutic candidate against mCRC by targeting FUT8. FDW028, an inhibitor specifically targeted FUT8, promotes defucosylation and consequent HSC70/LAMP2A-mediated lysosomal degradation of B7-H3, and exhibits potent anti-mCRC activities.
    MeSH term(s) Animals ; Mice ; Chaperone-Mediated Autophagy ; Autophagy/physiology ; Proteolysis ; Lung Neoplasms/drug therapy ; Lung Neoplasms/metabolism ; Colonic Neoplasms/metabolism ; Rectal Neoplasms ; Lysosomes/metabolism
    Language English
    Publishing date 2023-08-03
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2541626-1
    ISSN 2041-4889 ; 2041-4889
    ISSN (online) 2041-4889
    ISSN 2041-4889
    DOI 10.1038/s41419-023-06027-0
    Database MEDical Literature Analysis and Retrieval System OnLINE

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