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  1. Article ; Online: Proteasome as a Drug Target in Trypanosomatid Diseases.

    Silva, Mariana Luiza / de Santiago-Silva, Kaio Maciel / Fabris, Marciéli / Camargo, Priscila Goes / de Lima Ferreira Bispo, Marcelle

    Current drug targets

    2023  Volume 24, Issue 10, Page(s) 781–789

    Abstract: Some diseases caused by trypanosomatid parasites, like Leishmaniasis, Chagas Disease, and Human African Trypanosomiasis (HTA), are challenging to manage, mainly concerning pharmacological therapy because they are associated with vulnerable populations. ... ...

    Abstract Some diseases caused by trypanosomatid parasites, like Leishmaniasis, Chagas Disease, and Human African Trypanosomiasis (HTA), are challenging to manage, mainly concerning pharmacological therapy because they are associated with vulnerable populations. Unfortunately, there is a lack of significant investments in the search for new drugs. Therefore, one of the strategies to aid the discovery of new drugs is to identify and inhibit molecular targets essential to the parasite's survival, such as the proteasome, which degrades most proteins in the parasite cells. Our study has presented several proteasome inhibitors with various pharmacophoric cores, and two of them, 5, and 13, have stood out in the clinical phase of treatment for leishmaniasis.
    MeSH term(s) Animals ; Humans ; Proteasome Endopeptidase Complex ; Trypanosomiasis, African/drug therapy ; Chagas Disease/drug therapy ; Leishmaniasis/drug therapy ; Proteasome Inhibitors/pharmacology ; Proteasome Inhibitors/therapeutic use
    Chemical Substances Proteasome Endopeptidase Complex (EC 3.4.25.1) ; Proteasome Inhibitors
    Language English
    Publishing date 2023-07-19
    Publishing country United Arab Emirates
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2064859-5
    ISSN 1873-5592 ; 1389-4501
    ISSN (online) 1873-5592
    ISSN 1389-4501
    DOI 10.2174/1389450124666230719104147
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 5578: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
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  2. Article ; Online: CYP1B1: A Promising Target in Cancer Drug Discovery.

    Fabris, Marciéli / Luiza Silva, Mariana / de Santiago-Silva, Kaio Maciel / de Lima Ferreira Bispo, Marcelle / Goes Camargo, Priscila

    Anti-cancer agents in medicinal chemistry

    2023  Volume 23, Issue 9, Page(s) 981–988

    Abstract: CYP1B1 plays an essential role in cancer's pathogenesis since it activates procarcinogens. Significantly, this enzyme catalyzes the hydroxylation of 17β-estradiol, leading to carcinogenic metabolites involved in carcinogenesis and cancer progression. ... ...

    Abstract CYP1B1 plays an essential role in cancer's pathogenesis since it activates procarcinogens. Significantly, this enzyme catalyzes the hydroxylation of 17β-estradiol, leading to carcinogenic metabolites involved in carcinogenesis and cancer progression. Therefore, the inhibition of CYP1B1 activity is considered a therapeutic target for chemotherapy. In addition, CYP1B1 is overexpressed in hormone-dependent cancer cells and could be related to resistance to anticancer drugs. However, the activity of CYP1B1 in the tumor microenvironment can metabolize and activate prodrugs in cancer cells, providing more selectivity and being useful for chemoprevention or chemotherapy strategies. Furthermore, due to its importance in anticancer drug design, recent studies have reported using computational methods to understand the intermolecular interactions between possible ligands and CYP1B1. Therefore, in this perspective, we highlight recent findings in developing CYP1B1 inhibitors (flavonoids, trans-stilbenes, estradiol derivatives, and carbazoles) and CYP1B1-activated prodrugs (a chalcone DMU-135 and an oxime DMAKO-20). Finally, we have analyzed their possible molecular interactions with this enzymatic target by molecular docking, which can help to design new active substances.
    MeSH term(s) Humans ; Cytochrome P-450 CYP1A1/metabolism ; Molecular Docking Simulation ; Prodrugs/pharmacology ; Cytochrome P-450 CYP1B1 ; Antineoplastic Agents/pharmacology ; Neoplasms/drug therapy ; Carcinogenesis ; Drug Discovery ; Estradiol ; Tumor Microenvironment
    Chemical Substances Cytochrome P-450 CYP1A1 (EC 1.14.14.1) ; Prodrugs ; Cytochrome P-450 CYP1B1 (EC 1.14.14.1) ; Antineoplastic Agents ; Estradiol (4TI98Z838E) ; CYP1B1 protein, human (EC 1.14.14.1)
    Language English
    Publishing date 2023-01-09
    Publishing country Netherlands
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2217610-X
    ISSN 1875-5992 ; 1871-5206
    ISSN (online) 1875-5992
    ISSN 1871-5206
    DOI 10.2174/1871520623666230119103914
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 5583: Show issues Location:
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  3. Article ; Online: Thiohydantoins and hydantoins derived from amino acids as potent urease inhibitors: Inhibitory activity and ligand-target interactions.

    Camargo, Priscila Goes / Fabris, Marciéli / Nakamae, Matheus Yoshimitsu Tatsuta / de Freitas Oliveira, Breno Germano / da Silva Lima, Camilo Henrique / de Fátima, Ângelo / de Lima Ferreira Bispo, Marcelle / Macedo, Fernando

    Chemico-biological interactions

    2022  Volume 365, Page(s) 110045

    Abstract: We report the investigation of hydantoins and thiohydantoins derived from L and d-amino acids as inhibitors against the Canavalia ensiformis urease (CEU). The biochemical in vitro assay against CEU revealed a promising inhibitory potential for most ... ...

    Abstract We report the investigation of hydantoins and thiohydantoins derived from L and d-amino acids as inhibitors against the Canavalia ensiformis urease (CEU). The biochemical in vitro assay against CEU revealed a promising inhibitory potential for most thiohydantoins with six of them showing %I higher than the reference inhibitor thiourea (56.5%). In addition, thiohydantoin derived from l-valine, 1b, as well as the hydantoin 2d, derived from l-methionine, were identified as the most potent inhibitors with %I = 90.5 and 85.9 respectively. Enzyme kinetic studies demonstrated a mixed and uncompetitive inhibition profile for these compounds with K
    MeSH term(s) Amino Acids ; Canavalia/metabolism ; Enzyme Inhibitors/chemistry ; Hydantoins/pharmacology ; Kinetics ; Ligands ; Molecular Docking Simulation ; Thiohydantoins ; Urease/chemistry ; Urease/metabolism
    Chemical Substances Amino Acids ; Enzyme Inhibitors ; Hydantoins ; Ligands ; Thiohydantoins ; Urease (EC 3.5.1.5)
    Language English
    Publishing date 2022-07-16
    Publishing country Ireland
    Document type Journal Article
    ZDB-ID 218799-1
    ISSN 1872-7786 ; 0009-2797
    ISSN (online) 1872-7786
    ISSN 0009-2797
    DOI 10.1016/j.cbi.2022.110045
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 686: Show issues Location:
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  4. Article: Antiprotozoal Activity of Benzoylthiourea Derivatives against

    Pereira, Patrícia Morais Lopes / Fernandes, Bruna Terci / Dos Santos, Vitória Ribeiro / Cabral, Weslei Roberto Correia / Lovo-Martins, Maria Isabel / Alonso, Lais / Lancheros, César Armando Contreras / de Paula, Jéssica Carreira / Camargo, Priscila Goes / Suzukawa, Helena Tiemi / Alonso, Antônio / Macedo, Fernando / Nakamura, Celso Vataru / Tavares, Eliandro Reis / de Lima Ferreira Bispo, Marcelle / Yamauchi, Lucy Megumi / Pinge-Filho, Phileno / Yamada-Ogatta, Sueli Fumie

    Pathogens (Basel, Switzerland)

    2023  Volume 12, Issue 8

    Abstract: For decades, only two nitroheterocyclic drugs have been used as therapeutic agents for Chagas disease. However, these drugs present limited effectiveness during the chronic phase, possess unfavorable pharmacokinetic properties, and induce severe adverse ... ...

    Abstract For decades, only two nitroheterocyclic drugs have been used as therapeutic agents for Chagas disease. However, these drugs present limited effectiveness during the chronic phase, possess unfavorable pharmacokinetic properties, and induce severe adverse effects, resulting in low treatment adherence. A previous study reported that
    Language English
    Publishing date 2023-08-03
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2695572-6
    ISSN 2076-0817
    ISSN 2076-0817
    DOI 10.3390/pathogens12081012
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Molecular Targets for Chalcones in Antileishmanial Drug Discovery.

    de Santiago-Silva, Kaio Maciel / da Silva Gomes, Gabriel Felix / Perez, Carla Cristina / da Silva Lima, Camilo Henrique / de Lima Ferreira Bispo, Marcelle

    Mini reviews in medicinal chemistry

    2020  Volume 23, Issue 14, Page(s) 1414–1434

    Abstract: Leishmaniases are infectious diseases caused by flagellated protozoan parasites belonging to the ... ...

    Abstract Leishmaniases are infectious diseases caused by flagellated protozoan parasites belonging to the genus
    MeSH term(s) Female ; Humans ; Chalcones/pharmacology ; Chalcones/chemistry ; Chalcone/chemistry ; Molecular Docking Simulation ; Antiprotozoal Agents/pharmacology ; Antiprotozoal Agents/therapeutic use ; Antiprotozoal Agents/chemistry ; Leishmania ; Leishmaniasis/drug therapy ; Drug Discovery
    Chemical Substances Chalcones ; Chalcone (5S5A2Q39HX) ; Antiprotozoal Agents
    Language English
    Publishing date 2020-09-08
    Publishing country Netherlands
    Document type Review ; Journal Article
    ZDB-ID 2104081-3
    ISSN 1875-5607 ; 1389-5575
    ISSN (online) 1875-5607
    ISSN 1389-5575
    DOI 10.2174/1389557523666230127125058
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 5891: Show issues Location:
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  6. Article ; Online: In silico

    Felix da Silva Gomes, Gabriel / Goes Camargo, Priscila / de Santiago-Silva, Kaio Maciel / Suzukawa, Helena Tiemi / Sotero da Silva Ribeiro, Ana Paula / Orsato, Alexandre / Nakazato, Gerson / Yamada-Ogatta, Sueli Fumie / Faccin-Galhardi, Ligia Carla / da Silva Lima, Camilo Henrique / de Lima Ferreira Bispo, Marcelle / Perez, Carla Cristina

    Journal of biomolecular structure & dynamics

    2022  Volume 41, Issue 18, Page(s) 8978–8991

    Abstract: COVID-19, a disease caused by SARS-CoV-2, was declared a pandemic in 2020 and created a global crisis in health systems, with more than 545 million confirmed cases and 6.33 million deaths. In this sense, this work aims to identify possible inhibitors of ... ...

    Abstract COVID-19, a disease caused by SARS-CoV-2, was declared a pandemic in 2020 and created a global crisis in health systems, with more than 545 million confirmed cases and 6.33 million deaths. In this sense, this work aims to identify possible inhibitors of the SARS-CoV-2 RdRp enzyme using
    Language English
    Publishing date 2022-11-03
    Publishing country England
    Document type Journal Article
    ZDB-ID 49157-3
    ISSN 1538-0254 ; 0739-1102
    ISSN (online) 1538-0254
    ISSN 0739-1102
    DOI 10.1080/07391102.2022.2140203
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 2093: Show issues Location:
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