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  1. Article ; Online: Discovery of Potent Antimalarial Type II Kinase Inhibitors with Selectivity over Human Kinases.

    Wang, Lushun / Bohmer, Monica J / Wang, Jinhua / Nardella, Flore / Calla, Jaeson / Laureano De Souza, Mariana / Schindler, Kyra A / Montejo, Lukas / Mittal, Nimisha / Rocamora, Frances / Treat, Mayland / Charlton, Jordan T / Tumwebaze, Patrick K / Rosenthal, Philip J / Cooper, Roland A / Chakrabarti, Ratna / Winzeler, Elizabeth A / Chakrabarti, Debopam / Gray, Nathanael S

    Journal of medicinal chemistry

    2024  Volume 67, Issue 2, Page(s) 1460–1480

    Abstract: While progress has been made in the effort to eradicate malaria, the disease remains a significant threat to global health. Acquired resistance to frontline treatments is emerging in Africa, urging a need for the development of novel antimalarial agents. ...

    Abstract While progress has been made in the effort to eradicate malaria, the disease remains a significant threat to global health. Acquired resistance to frontline treatments is emerging in Africa, urging a need for the development of novel antimalarial agents. Repurposing human kinase inhibitors provides a potential expedited route given the availability of a diverse array of kinase-targeting drugs that are approved or in clinical trials. Phenotypic screening of a library of type II human kinase inhibitors identified compound
    MeSH term(s) Humans ; Antimalarials/pharmacology ; Antimalarials/therapeutic use ; Malaria/drug therapy ; Structure-Activity Relationship ; Receptor, EphA2 ; Africa ; Plasmodium falciparum
    Chemical Substances Antimalarials ; Receptor, EphA2 (EC 2.7.10.1)
    Language English
    Publishing date 2024-01-12
    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.3c02046
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
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    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)
    Zs.MB 1: Show issues

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  2. Article ; Online: Molecular targets for Chagas disease: validation, challenges and lead compounds for widely exploited targets.

    Laureano de Souza, Mariana / Lapierre, Thibault Joseph William Jacques Dit / Vitor de Lima Marques, Gabriel / Ferraz, Witor Ribeiro / Penteado, André Berndt / Henrique Goulart Trossini, Gustavo / Murta, Silvane Maria Fonseca / de Oliveira, Renata Barbosa / de Oliveira Rezende, Celso / Ferreira, Rafaela Salgado

    Expert opinion on therapeutic targets

    2023  Volume 27, Issue 10, Page(s) 911–925

    Abstract: Introduction: Chagas disease (CD) imposes social and economic burdens, yet the available treatments have limited efficacy in the disease's chronic phase and cause serious adverse effects. To address this challenge, target-based approaches are a possible ...

    Abstract Introduction: Chagas disease (CD) imposes social and economic burdens, yet the available treatments have limited efficacy in the disease's chronic phase and cause serious adverse effects. To address this challenge, target-based approaches are a possible strategy to develop new, safe, and active treatments for both phases of the disease.
    Areas covered: This review delves into target-based approaches applied to CD drug discovery, emphasizing the studies from the last five years. We highlight the proteins cruzain (CZ), trypanothione reductase (TR), sterol 14 α-demethylase (CPY51), iron superoxide dismutase (Fe-SOD), proteasome, cytochrome
    Expert opinion: Target-based approaches toward developing potential CD therapeutics have yielded promising leads in recent years. We expect a significant advance in this field in the next decade, fueled by the new options for
    MeSH term(s) Humans ; Chagas Disease/drug therapy ; Trypanosoma cruzi/genetics ; Drug Discovery
    Language English
    Publishing date 2023-10-30
    Publishing country England
    Document type Journal Article ; Review ; Research Support, Non-U.S. Gov't
    ZDB-ID 2055208-7
    ISSN 1744-7631 ; 1472-8222
    ISSN (online) 1744-7631
    ISSN 1472-8222
    DOI 10.1080/14728222.2023.2264512
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 5244: 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: Characterization of Competitive Inhibitors of Plasmodium falciparum cGMP-Dependent Protein Kinase.

    Eck, Tyler / Laureano de Souza, Mariana / Delvillar, Melvin / Ashraf, Kutub / Yadav Bheemanaboina, Rammohan R / Chakrasali, Ramappa / Kreiss, Tamara / Siekierka, John J / Rotella, David P / Bhanot, Purnima / Goodey, Nina M

    Chembiochem : a European journal of chemical biology

    2022  Volume 23, Issue 7, Page(s) e202100704

    Abstract: Plasmodium falciparum cGMP-dependent protein kinase (PfPKG) is an enticing antimalarial drug target. Novel chemotypes are needed because existing inhibitors have safety issues that may prevent further development. This work demonstrates isoxazole-based ... ...

    Abstract Plasmodium falciparum cGMP-dependent protein kinase (PfPKG) is an enticing antimalarial drug target. Novel chemotypes are needed because existing inhibitors have safety issues that may prevent further development. This work demonstrates isoxazole-based compounds are potent ATP competitive inhibitors of PfPKG and discloses a new analogue in this series. Isoxazoles 3 and 5 had K
    MeSH term(s) Antimalarials/pharmacology ; Binding Sites ; Cyclic GMP-Dependent Protein Kinases/antagonists & inhibitors ; Cyclic GMP-Dependent Protein Kinases/chemistry ; Humans ; Plasmodium falciparum/drug effects ; Protein Domains ; Protein Kinase Inhibitors/pharmacology
    Chemical Substances Antimalarials ; Protein Kinase Inhibitors ; Cyclic GMP-Dependent Protein Kinases (EC 2.7.11.12)
    Language English
    Publishing date 2022-02-23
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2020469-3
    ISSN 1439-7633 ; 1439-4227
    ISSN (online) 1439-7633
    ISSN 1439-4227
    DOI 10.1002/cbic.202100704
    Database MEDical Literature Analysis and Retrieval System OnLINE

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