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  1. Article: Natural products as LSD1 inhibitors for cancer therapy.

    Fang, Yuan / Yang, Chao / Yu, Zhiqiang / Li, Xiaochuan / Mu, Qingchun / Liao, Guochao / Yu, Bin

    Acta pharmaceutica Sinica. B

    2020  

    Abstract: ... of natural LSD1 inhibitors, analysis of the co-crystal structures of LSD1/natural product complex, antitumor ... this review will provide a landscape of natural LSD1 inhibitors. ... polyphenols, and cyclic peptides have shown effectiveness against LSD1. These natural products provide novel ...

    Abstract Natural products generally fall into the biologically relevant chemical space and always possess novel biological activities, thus making them a rich source of lead compounds for new drug discovery. With the recent technological advances, natural product-based drug discovery is now reaching a new era. Natural products have also shown promise in epigenetic drug discovery, some of them have advanced into clinical trials or are presently being used in clinic. The histone lysine specific demethylase 1 (LSD1), an important class of histone demethylases, has fundamental roles in the development of various pathological conditions. Targeting LSD1 has been recognized as a promising therapeutic option for cancer treatment. Notably, some natural products with different chemotypes including protoberberine alkaloids, flavones, polyphenols, and cyclic peptides have shown effectiveness against LSD1. These natural products provide novel scaffolds for developing new LSD1 inhibitors. In this review, we mainly discuss the identification of natural LSD1 inhibitors, analysis of the co-crystal structures of LSD1/natural product complex, antitumor activity and their modes of action. We also briefly discuss the challenges faced in this field. We believe this review will provide a landscape of natural LSD1 inhibitors.
    Keywords covid19
    Language English
    Publishing date 2020-06-20
    Publishing country Netherlands
    Document type Journal Article ; Review
    ISSN 2211-3835
    ISSN 2211-3835
    DOI 10.1016/j.apsb.2020.06.007
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Natural products as LSD1 inhibitors for cancer therapy

    Fang, Yuan / Yang, Chao / Yu, Zhiqiang / Li, Xiaochuan / Mu, Qingchun / Liao, Guochao / Yu, Bin

    Abstract: ... of natural LSD1 inhibitors, analysis of the co-crystal structures of LSD1/natural product complex, antitumor ... this review will provide a landscape of natural LSD1 inhibitors. ... polyphenols, and cyclic peptides have shown effectiveness against LSD1. These natural products provide novel ...

    Abstract Natural products generally fall into the biologically relevant chemical space and always possess novel biological activities, thus making them a rich source of lead compounds for new drug discovery. With the recent technological advances, natural product-based drug discovery is now reaching a new era. Natural products have also shown promise in epigenetic drug discovery, some of them have advanced into clinical trials or are presently being used in clinic. The histone lysine specific demethylase 1 (LSD1), an important class of histone demethylases, has fundamental roles in the development of various pathological conditions. Targeting LSD1 has been recognized as a promising therapeutic option for cancer treatment. Notably, some natural products with different chemotypes including protoberberine alkaloids, flavones, polyphenols, and cyclic peptides have shown effectiveness against LSD1. These natural products provide novel scaffolds for developing new LSD1 inhibitors. In this review, we mainly discuss the identification of natural LSD1 inhibitors, analysis of the co-crystal structures of LSD1/natural product complex, antitumor activity and their modes of action. We also briefly discuss the challenges faced in this field. We believe this review will provide a landscape of natural LSD1 inhibitors.
    Keywords covid19
    Publisher WHO
    Document type Article
    Note WHO #Covidence: #824859
    Database COVID19

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  3. Article ; Online: Identification and biological evaluation of natural product Biochanin A.

    Wang, Lei / Li, Lingzhao / Han, Quanxiang / Wang, Xiaofang / Zhao, Di / Liu, Junqi

    Bioorganic chemistry

    2020  Volume 97, Page(s) 103674

    Abstract: ... Biochanin A as a new LSD1 inhibitor and further biological evaluation in gastric MGC-803 cells. Biochanin ... Natural products have shown promise for epigenetic modulations and thus are therapeutically ... A effectively and reversibly inhibited LSD1 (IC ...

    Abstract Natural products have shown promise for epigenetic modulations and thus are therapeutically potential for cancer prevention and treatment. In this work, we report the identification of natural product Biochanin A as a new LSD1 inhibitor and further biological evaluation in gastric MGC-803 cells. Biochanin A effectively and reversibly inhibited LSD1 (IC
    MeSH term(s) Antineoplastic Agents/pharmacology ; Apoptosis/drug effects ; Biological Products/pharmacology ; Cell Line ; Cell Line, Tumor ; Cell Movement/drug effects ; Cell Proliferation/drug effects ; Genistein/pharmacology ; Histone Demethylases/antagonists & inhibitors ; Histone Demethylases/metabolism ; Humans ; Stomach Neoplasms/drug therapy ; Stomach Neoplasms/metabolism
    Chemical Substances Antineoplastic Agents ; Biological Products ; Genistein (DH2M523P0H) ; Histone Demethylases (EC 1.14.11.-) ; KDM1A protein, human (EC 1.5.-) ; biochanin A (U13J6U390T)
    Language English
    Publishing date 2020-02-17
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2020.103674
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4207: 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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  4. Article ; Online: Promising natural lysine specific demethylase 1 inhibitors for cancer treatment: advances and outlooks.

    Li, Zhong-Rui / Gu, Meng-Zhen / Xu, Xiao / Zhang, Jing-Han / Zhang, Hai-Li / Han, Chao

    Chinese journal of natural medicines

    2022  Volume 20, Issue 4, Page(s) 241–257

    Abstract: ... on the development of novel natural LSD1 inhibitors for cancer therapy. ... we briefly highlight recent advances in natural LSD1 inhibitors over the past decade. We present ... as a demethylase of histone 3 lysine 4 and 9, has become a potential therapeutic target for cancer therapy. LSD1 mediates ...

    Abstract Lysine specific demethylase 1 (LSD1), a transcriptional corepressor or coactivator that serves as a demethylase of histone 3 lysine 4 and 9, has become a potential therapeutic target for cancer therapy. LSD1 mediates many cellular signaling pathways and regulates cancer cell proliferation, invasion, migration, and differentiation. Recent research has focused on the exploration of its pharmacological inhibitors. Natural products are a major source of compounds with abundant scaffold diversity and structural complexity, which have made a major contribution to drug discovery, particularly anticancer agents. In this review, we briefly highlight recent advances in natural LSD1 inhibitors over the past decade. We present a comprehensive review on their discovery and identification process, natural plant sources, chemical structures, anticancer effects, and structure-activity relationships, and finally provide our perspective on the development of novel natural LSD1 inhibitors for cancer therapy.
    MeSH term(s) Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/therapeutic use ; Histone Demethylases/chemistry ; Histone Demethylases/metabolism ; Humans ; Lysine/therapeutic use ; Neoplasms/drug therapy
    Chemical Substances Antineoplastic Agents ; Enzyme Inhibitors ; Histone Demethylases (EC 1.14.11.-) ; Lysine (K3Z4F929H6)
    Language English
    Publishing date 2022-04-29
    Publishing country China
    Document type Journal Article ; Review
    ZDB-ID 2192577-X
    ISSN 1875-5364 ; 2095-6975 ; 1672-3651
    ISSN (online) 1875-5364
    ISSN 2095-6975 ; 1672-3651
    DOI 10.1016/S1875-5364(22)60141-9
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 6113: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
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  5. Article ; Online: Discovery of natural product-like spirooxindole derivatives as highly potent and selective LSD1/KDM1A inhibitors for AML treatment.

    Yang, Chao / Fang, Yuan / Luo, Xiang / Teng, Dehong / Liu, Zhongqiu / Zhou, Yingtang / Liao, Guochao

    Bioorganic chemistry

    2022  Volume 120, Page(s) 105596

    Abstract: ... therapy. Following the work on the discovery of natural LSD1 inhibitor higenamine, we herein performed ... Histone lysine specific demethylase 1 (LSD1) is a promising new therapeutic target for cancer ... potent LSD1 inhibitor (IC ...

    Abstract Histone lysine specific demethylase 1 (LSD1) is a promising new therapeutic target for cancer therapy. Following the work on the discovery of natural LSD1 inhibitor higenamine, we herein performed further structure-based design, synthesis, and extensive structure-activity relationship (SAR) studies, affording structurally new spirooxindole derivatives. Particularly, FY-56 was identified to be a highly potent LSD1 inhibitor (IC
    MeSH term(s) Animals ; Biological Products/therapeutic use ; Enzyme Inhibitors ; Histone Demethylases ; Leukemia, Myeloid, Acute/drug therapy ; Mice ; Structure-Activity Relationship
    Chemical Substances Biological Products ; Enzyme Inhibitors ; Histone Demethylases (EC 1.14.11.-)
    Language English
    Publishing date 2022-01-06
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2022.105596
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4207: 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)

    Order via subito

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  6. Article: Promising natural lysine specific demethylase 1 inhibitors for cancer treatment: advances and outlooks

    LI, Zhong-Rui / GU, Meng-Zhen / XU, Xiao / ZHANG, Jing-Han / ZHANG, Hai-Li / HAN, Chao

    Chinese journal of natural medicines. 2022 Apr., v. 20, no. 4

    2022  

    Abstract: ... on the development of novel natural LSD1 inhibitors for cancer therapy. ... we briefly highlight recent advances in natural LSD1 inhibitors over the past decade. We present ... as a demethylase of histone 3 lysine 4 and 9, has become a potential therapeutic target for cancer therapy. LSD1 mediates ...

    Abstract Lysine specific demethylase 1 (LSD1), a transcriptional corepressor or coactivator that serves as a demethylase of histone 3 lysine 4 and 9, has become a potential therapeutic target for cancer therapy. LSD1 mediates many cellular signaling pathways and regulates cancer cell proliferation, invasion, migration, and differentiation. Recent research has focused on the exploration of its pharmacological inhibitors. Natural products are a major source of compounds with abundant scaffold diversity and structural complexity, which have made a major contribution to drug discovery, particularly anticancer agents. In this review, we briefly highlight recent advances in natural LSD1 inhibitors over the past decade. We present a comprehensive review on their discovery and identification process, natural plant sources, chemical structures, anticancer effects, and structure–activity relationships, and finally provide our perspective on the development of novel natural LSD1 inhibitors for cancer therapy.
    Keywords cancer therapy ; cell proliferation ; histones ; lysine ; neoplasm cells ; transcription (genetics)
    Language English
    Dates of publication 2022-04
    Size p. 241-257.
    Publishing place Elsevier B.V.
    Document type Article
    ZDB-ID 2192577-X
    ISSN 1875-5364 ; 2095-6975 ; 1672-3651
    ISSN (online) 1875-5364
    ISSN 2095-6975 ; 1672-3651
    DOI 10.1016/S1875-5364(22)60141-9
    Database NAL-Catalogue (AGRICOLA)

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 6113: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

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  7. Article ; Online: Flavone-based natural product agents as new lysine-specific demethylase 1 inhibitors exhibiting cytotoxicity against breast cancer cells in vitro.

    Xu, Xiao / Peng, Wenhui / Liu, Cuiyun / Li, Sixuan / Lei, Jiali / Wang, Zhen / Kong, Lingyi / Han, Chao

    Bioorganic & medicinal chemistry

    2018  Volume 27, Issue 2, Page(s) 370–374

    Abstract: ... These findings suggest that natural LSD1 inhibitors, and particularly isoquercitrin, are promising for cancer ... However, almost all LSD1 inhibitors developed to date are chemo-synthesised molecules. In this study, the LSD1 ... Lysine-specific demethylase 1 (LSD1) has recently emerged as a therapeutic target for cancer ...

    Abstract Lysine-specific demethylase 1 (LSD1) has recently emerged as a therapeutic target for cancer. However, almost all LSD1 inhibitors developed to date are chemo-synthesised molecules. In this study, the LSD1 inhibitory activity of 12 natural flavones, including four aglycones and their corresponding monoglycosides and diglucosides, was evaluated. Based on the structure-activity relationships, LSD1 inhibition activity was greater for flavonoid monoglycosides than their aglycones lacking the sugar moiety. The effects of isoquercitrin, which exhibited optimal LSD1 inhibitory activity, on cancer cell properties were evaluated. Isoquercitrin induced the expression of key proteins in the mitochondrial-mediated apoptosis pathway and caused apoptosis in LSD1-overexpressing MDA-MB-231 cells via the inhibition of LSD1. These findings suggest that natural LSD1 inhibitors, and particularly isoquercitrin, are promising for cancer treatment.
    MeSH term(s) Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Apoptosis/drug effects ; Biological Products/chemistry ; Biological Products/pharmacology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; Flavones/chemistry ; Flavones/pharmacology ; Histone Demethylases/metabolism ; Humans ; Membrane Potential, Mitochondrial/drug effects ; Mitochondria/metabolism ; Molecular Structure ; Structure-Activity Relationship
    Chemical Substances Antineoplastic Agents ; Biological Products ; Enzyme Inhibitors ; Flavones ; Histone Demethylases (EC 1.14.11.-) ; KDM1A protein, human (EC 1.5.-)
    Language English
    Publishing date 2018-12-07
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1161284-8
    ISSN 1464-3391 ; 0968-0896
    ISSN (online) 1464-3391
    ISSN 0968-0896
    DOI 10.1016/j.bmc.2018.12.013
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 3815: 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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  8. Article ; Online: Bioactivity evaluation of natural product α-mangostin as a novel xanthone-based lysine-specific demethylase 1 inhibitor to against tumor metastasis.

    Han, Chao / Li, Zhongrui / Hou, Jiqin / Wang, Zhen / Xu, Dingqiao / Xue, Guimin / Kong, Lingyi

    Bioorganic chemistry

    2017  Volume 76, Page(s) 415–419

    Abstract: ... all the developed LSD1 inhibitors are chemo-synthesized molecules, while α-mangostin is first characterized ... as xanthone-based natural inhibitor in the current study with IC ... Lysine-specific demethylase 1 (LSD1), which has been reported to be overexpressed in several human ...

    Abstract Lysine-specific demethylase 1 (LSD1), which has been reported to be overexpressed in several human cancers, has recently emerged as an attractive therapeutic target for treating cancer. To date, almost all the developed LSD1 inhibitors are chemo-synthesized molecules, while α-mangostin is first characterized as xanthone-based natural inhibitor in the current study with IC
    MeSH term(s) Biological Products/chemistry ; Biological Products/pharmacology ; Catalytic Domain ; Cell Line, Tumor ; Cell Movement/drug effects ; Histone Demethylases/antagonists & inhibitors ; Histone Demethylases/chemistry ; Humans ; Molecular Docking Simulation ; Neoplasm Metastasis/drug therapy ; Xanthones/chemistry ; Xanthones/pharmacology
    Chemical Substances Biological Products ; Xanthones ; Histone Demethylases (EC 1.14.11.-) ; KDM1A protein, human (EC 1.5.-) ; mangostin (U6RIV93RU1)
    Language English
    Publishing date 2017-12-08
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2017.12.004
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4207: 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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