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  1. Article ; Online: Human sirtuin 2 inhibitors, their mechanisms and binding modes.

    Penteado, André Berndt / Hassanie, Haifa / Gomes, Renan Augusto / Silva Emery, Flávio da / Goulart Trossini, Gustavo Henrique

    Future medicinal chemistry

    2023  Volume 15, Issue 3, Page(s) 291–311

    Abstract: The silent information regulator (sirtuin) is a family of enzymes involved in epigenetic processes with lysine deacetylase activity, having as substrates histones and other proteins. They participate in a wide range of cellular and pathologic processes, ... ...

    Abstract The silent information regulator (sirtuin) is a family of enzymes involved in epigenetic processes with lysine deacetylase activity, having as substrates histones and other proteins. They participate in a wide range of cellular and pathologic processes, such as gene expression, cell division and motility, oxidative-induced stress management, metabolic control and carcinogenesis, among others, thus presenting as interesting therapeutic targets. In this article, the authors describe the inhibitory mechanisms and binding modes of the human sirtuin 2 (hSIRT2) inhibitors, which had their complexes with the enzyme structurally characterized. The results help pave the way for the rational designing of new hSIRT2 inhibitors and the development of novel therapeutic agents targeting this epigenetic enzyme.
    MeSH term(s) Humans ; Sirtuin 2 ; Histone Deacetylase Inhibitors/chemistry ; Histones/metabolism
    Chemical Substances Sirtuin 2 (EC 3.5.1.-) ; Histone Deacetylase Inhibitors ; Histones
    Language English
    Publishing date 2023-03-09
    Publishing country England
    Document type Journal Article ; Review ; Research Support, Non-U.S. Gov't
    ISSN 1756-8927
    ISSN (online) 1756-8927
    DOI 10.4155/fmc-2022-0253
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Parasitic sirtuin 2 as an opportunity in drug discovery.

    Gomes, Renan Augusto / Fornari, Evelin / Silva Rocha, Ana Carolina / Tripodi, Gustavo Luis / Silva Emery, Flavio da / Goulart Trossini, Gustavo Henrique

    Future medicinal chemistry

    2021  Volume 13, Issue 16, Page(s) 1397–1409

    Abstract: Infections caused by protozoans remain a public health issue, especially in tropical countries. Serious adverse events, lack of efficacy at the different stages of the infection and routes of administration that have a negative impact on treatment ... ...

    Abstract Infections caused by protozoans remain a public health issue, especially in tropical countries. Serious adverse events, lack of efficacy at the different stages of the infection and routes of administration that have a negative impact on treatment adherence are some of the problems with currently available therapy against these diseases. Here we describe an epigenetic target, sirtuin 2 and its related proteins, that is promising given the results in phenotypic assays and
    MeSH term(s) Animals ; Antiprotozoal Agents/chemistry ; Antiprotozoal Agents/pharmacology ; Drug Discovery ; Humans ; Leishmania/drug effects ; Parasitic Sensitivity Tests ; Plasmodium falciparum/drug effects ; Schistosoma mansoni/drug effects ; Sirtuin 2/antagonists & inhibitors ; Sirtuin 2/metabolism ; Trypanosoma/drug effects
    Chemical Substances Antiprotozoal Agents ; Sirtuin 2 (EC 3.5.1.-)
    Language English
    Publishing date 2021-06-30
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ISSN 1756-8927
    ISSN (online) 1756-8927
    DOI 10.4155/fmc-2021-0091
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

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