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  1. Article ; Online: Design strategies and recent development of bioactive modulators for glutamine transporters.

    Cheng, Xinying / Wang, Yezhi / Gong, Guangyue / Shen, Pei / Li, Zhiyu / Bian, Jinlei

    Drug discovery today

    2024  Volume 29, Issue 2, Page(s) 103880

    Abstract: Glutamine transporters are integral to the metabolism of glutamine in both healthy tissues and cancerous cells, playing a pivotal role in maintaining amino acid balance, synthesizing biomolecules, and regulating redox equilibrium. Their critical ... ...

    Abstract Glutamine transporters are integral to the metabolism of glutamine in both healthy tissues and cancerous cells, playing a pivotal role in maintaining amino acid balance, synthesizing biomolecules, and regulating redox equilibrium. Their critical functions in cellular metabolism make them promising targets for oncological therapies. Recent years have witnessed substantial progress in the field of glutamine transporters, marked by breakthroughs in understanding of their protein structures and the discovery of novel inhibitors, prodrugs, and radiotracers. This review provides a comprehensive update on the latest advancements in modulators targeting the glutamine transporter, with special attention given to LAT1 and ASCT2. It also discusses innovative approaches in drug design aimed at these transporters.
    MeSH term(s) Glutamine/metabolism ; Amino Acids ; Membrane Transport Proteins
    Chemical Substances Glutamine (0RH81L854J) ; Amino Acids ; Membrane Transport Proteins
    Language English
    Publishing date 2024-01-11
    Publishing country England
    Document type Journal Article ; Review
    ZDB-ID 1324988-5
    ISSN 1878-5832 ; 1359-6446
    ISSN (online) 1878-5832
    ISSN 1359-6446
    DOI 10.1016/j.drudis.2024.103880
    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:
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    Jg. 1995 - 2021: Lesesall (2.OG)
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  2. Article ; Online: Drug development and potential targets for Cushing's syndrome.

    Wei, Wei / Xu, Qianqian / Wu, Liuyi / Gong, Guangyue / Tian, Yucheng / Huang, Huidan / Li, Zhiyu

    European journal of medicinal chemistry

    2024  Volume 270, Page(s) 116333

    Abstract: Cushing's syndrome (CS) is a complex disorder characterized by the excessive secretion of cortisol, with Cushing's disease (CD), particularly associated with pituitary tumors, exhibiting heightened morbidity and mortality. Although transsphenoidal ... ...

    Abstract Cushing's syndrome (CS) is a complex disorder characterized by the excessive secretion of cortisol, with Cushing's disease (CD), particularly associated with pituitary tumors, exhibiting heightened morbidity and mortality. Although transsphenoidal pituitary surgery (TSS) stands as the primary treatment for CD, there is a crucial need to optimize patient prognosis. Current medical therapy serves as an adjunctive measure due to its unsatisfactory efficacy and unpredictable side effects. In this comprehensive review, we delve into recent advances in understanding the pathogenesis of CS and explore therapeutic options by conducting a critical analysis of potential drug targets and candidates. Additionally, we provide an overview of the design strategy employed in previously reported candidates, along with a summary of structure-activity relationship (SAR) analyses and their biological efficacy. This review aims to contribute valuable insights to the evolving landscape of CS research, shedding light on potential avenues for therapeutic development.
    MeSH term(s) Humans ; Cushing Syndrome/drug therapy ; Cushing Syndrome/etiology ; Pituitary ACTH Hypersecretion/complications ; Pituitary ACTH Hypersecretion/drug therapy ; Drug Delivery Systems ; Drug Development ; Hydrocortisone/therapeutic use
    Chemical Substances Hydrocortisone (WI4X0X7BPJ)
    Language English
    Publishing date 2024-03-22
    Publishing country France
    Document type Journal Article ; Review
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2024.116333
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.B 784: Show issues Location:
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  3. Article ; Online: An updated patent review of glutaminase inhibitors (2019-2022).

    Wang, Danni / Li, Xiaohong / Gong, Guangyue / Lu, Yulong / Guo, Ziming / Chen, Rui / Huang, Huidan / Li, Zhiyu / Bian, Jinlei

    Expert opinion on therapeutic patents

    2023  Volume 33, Issue 1, Page(s) 17–28

    Abstract: Introduction: Kidney-type glutaminase (GLS1), a key enzyme controlling the hydrolysis of glutamine to glutamate to resolve the 'glutamine addiction' of cancer cells, has been shown to play a central role in supporting cancer growth and proliferation. ... ...

    Abstract Introduction: Kidney-type glutaminase (GLS1), a key enzyme controlling the hydrolysis of glutamine to glutamate to resolve the 'glutamine addiction' of cancer cells, has been shown to play a central role in supporting cancer growth and proliferation. Therefore, the inhibition of GLS1 as a novel cancer treating strategy is of great interest.
    Areas covered: This review covers recent patents (2019-present) involving GLS1 inhibitors, which are mostly focused on their chemical structures, molecular mechanisms of action, pharmacokinetic properties, and potential clinical applications.
    Expert opinion: Currently, despite significant efforts, the search for potent GLS1 inhibitors has not resulted in the development of compounds for therapeutic applications. Most recent patents and literature focus on GLS1 inhibitors IPN60090 and DRP104, which have entered clinical trials. While other patent disclosures during this period have not generated any drug candidates, the clinical update will inform the potential of these inhibitors as promising therapeutic agents either as single or as combination interventions.
    MeSH term(s) Humans ; Glutamine ; Glutaminase ; Patents as Topic ; Enzyme Inhibitors/pharmacology ; Neoplasms
    Chemical Substances Glutamine (0RH81L854J) ; Glutaminase (EC 3.5.1.2) ; Enzyme Inhibitors
    Language English
    Publishing date 2023-02-02
    Publishing country England
    Document type Review ; Journal Article
    ZDB-ID 1186201-4
    ISSN 1744-7674 ; 0962-2594 ; 1354-3776
    ISSN (online) 1744-7674
    ISSN 0962-2594 ; 1354-3776
    DOI 10.1080/13543776.2023.2173573
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 3962: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
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  4. Article ; Online: Discovery of Novel Aminobutanoic Acid-Based ASCT2 Inhibitors for the Treatment of Non-Small-Cell Lung Cancer.

    Qin, Lian / Cheng, Xinying / Wang, Shijiao / Gong, Guangyue / Su, Huiyan / Huang, Huidan / Chen, Tian / Damdinjav, Davaadagva / Dorjsuren, Buyankhishig / Li, Zhiyu / Qiu, Zhixia / Bian, Jinlei

    Journal of medicinal chemistry

    2024  Volume 67, Issue 2, Page(s) 988–1007

    Abstract: Alanine-serine-cysteine transporter 2 (ASCT2) is up-regulated in lung cancers, and inhibiting it could potentially lead to nutrient deprivation, making it a viable strategy for cancer treatment. In this study, we present a series of ASCT2 inhibitors ... ...

    Abstract Alanine-serine-cysteine transporter 2 (ASCT2) is up-regulated in lung cancers, and inhibiting it could potentially lead to nutrient deprivation, making it a viable strategy for cancer treatment. In this study, we present a series of ASCT2 inhibitors based on aminobutanoic acids, which exhibit potent inhibitory activity. Two compounds,
    MeSH term(s) Humans ; Carcinoma, Non-Small-Cell Lung/drug therapy ; Lung Neoplasms/drug therapy ; Lung Neoplasms/metabolism ; Cysteine ; Serine ; Alanine ; HEK293 Cells ; Glutamine ; Minor Histocompatibility Antigens/metabolism ; Cell Line, Tumor
    Chemical Substances Cysteine (K848JZ4886) ; Serine (452VLY9402) ; Alanine (OF5P57N2ZX) ; Glutamine (0RH81L854J) ; Minor Histocompatibility Antigens
    Language English
    Publishing date 2024-01-13
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.3c01093
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.MB 1: Show issues

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  5. Article ; Online: Discovery of novel flavonoid-based CDK9 degraders for prostate cancer treatment via a PROTAC strategy.

    Wu, Tizhi / Zhang, Zhiming / Gong, Guangyue / Du, Zekun / Xu, Yifan / Yu, Sixian / Ma, Feihai / Zhang, Xuan / Wang, Yuxiao / Chen, Haoming / Wu, Shiqi / Xu, Xi / Qiu, Zhixia / Li, Zhiyu / Wu, Hongxi / Bian, Jinlei / Wang, Jubo

    European journal of medicinal chemistry

    2023  Volume 260, Page(s) 115774

    Abstract: CDK9 plays a vital role in regulating RNA transcription and significantly impacts the expression of short-lived proteins such as Mcl-1 and c-Myc. Thus, targeting CDK9 holds great promise for the development of antitumor drugs. Natural flavonoid ... ...

    Abstract CDK9 plays a vital role in regulating RNA transcription and significantly impacts the expression of short-lived proteins such as Mcl-1 and c-Myc. Thus, targeting CDK9 holds great promise for the development of antitumor drugs. Natural flavonoid derivatives have recently gained considerable attention in the field of antitumor drug research due to their broad bioactivity and low toxicity. In this study, the PROTAC strategy was used to perform structural modifications of the flavonoid derivative LWT-111 to design a series of flavonoid-based CDK9 degraders. Notably, compound CP-07 emerged as a potent CDK9 degrader, effectively suppressing the proliferation and colony formation of 22RV1 cells by downregulating Mcl-1 and c-Myc. Moreover, CP-07 exhibited significant tumor growth inhibition with a TGI of 75.1% when administered at a dose of 20 mg/kg in the 22RV1 xenograft tumor model. These findings demonstrated the potential of CP-07 as a powerful flavonoid-based CDK9 degrader for prostate cancer therapy.
    MeSH term(s) Male ; Animals ; Humans ; Myeloid Cell Leukemia Sequence 1 Protein ; Prostatic Neoplasms/drug therapy ; Disease Models, Animal ; Flavonoids/pharmacology ; Heterografts ; Cyclin-Dependent Kinase 9
    Chemical Substances Myeloid Cell Leukemia Sequence 1 Protein ; Flavonoids ; CDK9 protein, human (EC 2.7.11.22) ; Cyclin-Dependent Kinase 9 (EC 2.7.11.22)
    Language English
    Publishing date 2023-09-01
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2023.115774
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

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