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  1. AU="Mukherjee, Suravi"
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  1. Article ; Online: Exploring the Structural Attributes of Yoda1 for the Development of New-Generation Piezo1 Agonist Yaddle1 as a Vaccine Adjuvant Targeting Optimal T Cell Activation.

    Goon, Sunny / Shiu Chen Liu, Chinky / Ghosh Dastidar, Uddipta / Paul, Barnali / Mukherjee, Suravi / Sarkar, Himadri Sekhar / Desai, Milie / Jana, Rituparna / Pal, Sourav / Sreedevi, Namala Venkata / Ganguly, Dipyaman / Talukdar, Arindam

    Journal of medicinal chemistry

    2024  

    Abstract: Piezo1, a mechano-activated ion channel, has wide-ranging physiological and therapeutic implications, with the ongoing development of specific agonists unveiling cellular responses to mechanical stimuli. In our study, we systematically analyzed the ... ...

    Abstract Piezo1, a mechano-activated ion channel, has wide-ranging physiological and therapeutic implications, with the ongoing development of specific agonists unveiling cellular responses to mechanical stimuli. In our study, we systematically analyzed the chemical subunits in Piezo1 protein agonist Yoda1 to comprehend the structure-activity relationship and push forward next-generation agonist development. Preliminary screening assays for Piezo1 agonism were performed using the Piezo1-mCherry-transfected HEK293A cell line, keeping Yoda1 as a positive control. We introduce a novel Piezo1 agonist Yaddle1 (
    Language English
    Publishing date 2024-05-08
    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.4c00322
    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)
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  2. Article ; Online: Hit-to-lead optimization of 2-aminoquinazolines as anti-microbial agents against Leishmania donovani.

    Das, Nirmal / Roy, Jayasree / Patra, Binita / Saunders, Eleanor / Sarkar, Dipika / Goon, Sunny / Sinha, Bishnu Prasad / Roy, Shreya / Roy, Swarnali / Sarif, Jafar / Bandopadhyay, Purbita / Barik, Subhasis / Mukherjee, Suravi / McNamara, Nicole / Varghese, Swapna / Simpson, Kaylene / Baell, Jonathan / McConville, Malcolm / Ganguly, Dipyaman /
    Talukdar, Arindam

    European journal of medicinal chemistry

    2024  Volume 269, Page(s) 116256

    Abstract: Visceral leishmaniasis is a potentially fatal disease caused by infection by the intracellular protist pathogens Leishmania donovani or Leishmania infantum. Present therapies are ineffective because of high costs, variable efficacy against different ... ...

    Abstract Visceral leishmaniasis is a potentially fatal disease caused by infection by the intracellular protist pathogens Leishmania donovani or Leishmania infantum. Present therapies are ineffective because of high costs, variable efficacy against different species, the requirement for hospitalization, toxicity and drug resistance. Detailed analysis of previously published hit molecules suggested a crucial role of 'guanidine' linkage for their efficacy against L. donovani. Here we report the design of 2-aminoquinazoline heterocycle as a basic pharmacophore-bearing guanidine linkage. The introduction of various groups and functionality at different positions of the quinazoline scaffold results in enhanced antiparasitic potency with modest host cell cytotoxicity using a physiologically relevant THP-1 transformed macrophage infection model. In terms of the ADME profile, the C7 position of quinazoline was identified as a guiding tool for designing better molecules. The good ADME profile of the compounds suggests that they merit further consideration as lead compounds for treating visceral leishmaniasis.
    MeSH term(s) Humans ; Leishmania donovani ; Leishmaniasis, Visceral/drug therapy ; Antiparasitic Agents/pharmacology ; Leishmania infantum ; Quinazolines/pharmacology ; Quinazolines/therapeutic use
    Chemical Substances Antiparasitic Agents ; Quinazolines
    Language English
    Publishing date 2024-02-27
    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.2024.116256
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.B 784: Show issues Location:
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