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  1. Article: Inhibitory effect of phytochemicals towards SARS-CoV-2 papain like protease (PLpro) proteolytic and deubiquitinase activity.

    Kawall, Anasha / Lewis, Devin S M / Sharma, Avini / Chavada, Krishna / Deshmukh, Rahul / Rayalam, Srujana / Mody, Vicky / Taval, Shashidharamurthy

    Frontiers in chemistry

    2023  Volume 10, Page(s) 1100460

    Abstract: Recent studies have shown that RNA-dependent RNA polymerase (RdRp), 3-chymotrypsin-like protease (3CLpro), and papain-like protease (PLpro) are necessary for SARS-CoV-2 replication. Among these three enzymes, PLpro exhibits both proteolytic and ... ...

    Abstract Recent studies have shown that RNA-dependent RNA polymerase (RdRp), 3-chymotrypsin-like protease (3CLpro), and papain-like protease (PLpro) are necessary for SARS-CoV-2 replication. Among these three enzymes, PLpro exhibits both proteolytic and deubiquitinase (DUB) activity and is responsible for disrupting the host's innate immune response against SARS-CoV-2. Because of this unique property of PLpro, we investigated the inhibitory effects of phytochemicals on the SARS-CoV-2 PLpro enzyme. Our data indicates that the phytochemicals such as catechin, epigallocatechin gallate (EGCG), mangiferin, myricetin, rutin, and theaflavin exhibited inhibitory activity with IC
    Language English
    Publishing date 2023-01-12
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2711776-5
    ISSN 2296-2646
    ISSN 2296-2646
    DOI 10.3389/fchem.2022.1100460
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Pharmacological antagonism of EP2 receptor does not modify basal cardiovascular and respiratory function, blood cell counts, and bone morphology in animal models.

    Rawat, Varun / Banik, Avijit / Amaradhi, Radhika / Rojas, Asheebo / Taval, Shashidharamurthy / Nagy, Tamas / Dingledine, Raymond / Ganesh, Thota

    Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

    2022  Volume 147, Page(s) 112646

    Abstract: The EP2 receptor has emerged as a therapeutic target with exacerbating role in disease pathology for a variety of peripheral and central nervous system disorders. We and others have recently demonstrated beneficial effects of EP2 antagonists in ... ...

    Abstract The EP2 receptor has emerged as a therapeutic target with exacerbating role in disease pathology for a variety of peripheral and central nervous system disorders. We and others have recently demonstrated beneficial effects of EP2 antagonists in preclinical models of neuroinflammation and peripheral inflammation. However, it was earlier reported that mice with global EP2 knockout (KO) display adverse phenotypes on fertility and blood pressure. Other studies indicated that EP2 activation with an agonist has a beneficial effect of healing fractured bone in animal models. These results impeded the development of EP2 antagonists, and EP2 antagonism as therapeutic strategy. To determine whether treatment with EP2 antagonist mimics the adverse phenotypes of the EP2 global KO mouse, we tested two EP2 antagonists TG11-77. HCl and TG6-10-1 in mice and rats while they are on normal or high-salt diet, and by two different administration protocols (acute and chronic). There were no adverse effects of the antagonists on systolic and diastolic blood pressure, heart rate, respiratory function in mice and rats regardless of rodents being on a regular or high salt diet. Furthermore, chronic exposure to TG11-77. HCl produced no adverse effects on blood cell counts, bone-volume and bone-mineral density in mice. Our findings argue against adverse effects on cardiovascular and respiratory systems, blood counts and bone structure in healthy rodents from the use of small molecule reversible antagonists for EP2, in contrast to the genetic ablation model. This study paves the way for advancing therapeutic applications of EP2 antagonists against diseases involving EP2 dysfunction.
    MeSH term(s) Animals ; Blood Cell Count ; Bone Density/drug effects ; Bone and Bones/drug effects ; Cardiovascular Diseases/pathology ; Disease Models, Animal ; Female ; Hemodynamics/drug effects ; Indoles/pharmacology ; Male ; Mice ; Mice, Inbred C57BL ; Mice, Knockout ; Phenotype ; Rats ; Rats, Sprague-Dawley ; Receptors, Prostaglandin E, EP2 Subtype/antagonists & inhibitors ; Respiratory Rate/drug effects
    Chemical Substances Indoles ; Receptors, Prostaglandin E, EP2 Subtype ; TG6-10-1
    Language English
    Publishing date 2022-01-26
    Publishing country France
    Document type Journal Article
    ZDB-ID 392415-4
    ISSN 1950-6007 ; 0753-3322 ; 0300-0893
    ISSN (online) 1950-6007
    ISSN 0753-3322 ; 0300-0893
    DOI 10.1016/j.biopha.2022.112646
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Ud II Zs.198: Show issues Location:
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  3. Article ; Online: Lipocalin-2 deficiency may predispose to the progression of spontaneous age-related adiposity in mice.

    Meyers, Keya / López, María / Ho, Joanna / Wills, Savannah / Rayalam, Srujana / Taval, Shashidharamurthy

    Scientific reports

    2020  Volume 10, Issue 1, Page(s) 14589

    Abstract: Lipocalin-2 (Lcn2) is an innate immune protein elevated by several orders of magnitude in various inflammatory conditions including aging and obesity. Recent studies have shown that Lcn2 is secreted by adipocytes in response to inflammation and is ... ...

    Abstract Lipocalin-2 (Lcn2) is an innate immune protein elevated by several orders of magnitude in various inflammatory conditions including aging and obesity. Recent studies have shown that Lcn2 is secreted by adipocytes in response to inflammation and is categorized as a new adipokine cross-linking innate immunity and metabolic disorders including obesity. However, the involvement of Lcn2 and its function during the progression of obesity is largely unknown. Recently, browning of white adipose tissue (WAT) has gained attention as a therapeutic strategy to combat obesity. Herein, we have shown that treatment of mature 3T3-L1 adipocytes with recombinant Lcn2 (rec-Lcn2) resulted in the up-regulation of thermogenic and beige/brown markers (UCP1, PRDM16, ZIC-1 and TBX1) and increased mitochondrial activity. Additionally, global Lcn2 genetic knockout (Lcn2KO) mice exhibited accelerated weight gain and visceral fat deposition with age, when compared to wild type (WT) mice. Taken together, both in vitro and in vivo studies suggest that Lcn2 is a naturally occurring adipokine, and may serve as an anti-obesity agent by upregulating the thermogenic markers resulting in the browning of WAT. Therefore, Lcn2 and its downstream signaling pathways could be a potential therapeutic target for obesity.
    MeSH term(s) 3T3-L1 Cells ; Adipose Tissue/metabolism ; Adipose Tissue/pathology ; Aging ; Animals ; Female ; Intra-Abdominal Fat/metabolism ; Intra-Abdominal Fat/pathology ; Lipocalin-2/physiology ; Male ; Mice ; Mice, Inbred C57BL ; Mice, Knockout ; Obesity/physiopathology ; Thermogenesis ; Weight Gain
    Chemical Substances Lipocalin-2 ; Lcn2 protein, mouse (126469-30-5)
    Language English
    Publishing date 2020-09-03
    Publishing country England
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 2615211-3
    ISSN 2045-2322 ; 2045-2322
    ISSN (online) 2045-2322
    ISSN 2045-2322
    DOI 10.1038/s41598-020-71249-7
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Aloin isoforms (A and B) selectively inhibits proteolytic and deubiquitinating activity of papain like protease (PLpro) of SARS-CoV-2 in vitro.

    Lewis, Devin S M / Ho, Joanna / Wills, Savannah / Kawall, Anasha / Sharma, Avini / Chavada, Krishna / Ebert, Maximilian C C J C / Evoli, Stefania / Singh, Ajay / Rayalam, Srujana / Mody, Vicky / Taval, Shashidharamurthy

    Scientific reports

    2022  Volume 12, Issue 1, Page(s) 2145

    Abstract: The most common host entry point of human adapted coronaviruses (CoV) including SARS-CoV-2 is through the initial colonization in the nostril and mouth region which is responsible for spread of the infection. Most recent studies suggest that the ... ...

    Abstract The most common host entry point of human adapted coronaviruses (CoV) including SARS-CoV-2 is through the initial colonization in the nostril and mouth region which is responsible for spread of the infection. Most recent studies suggest that the commercially available oral and nasal rinse products are effective in inhibiting the viral replication. However, the anti-viral mechanism of the active ingredients present in the oral rinses have not been studied. In the present study, we have assessed in vitro enzymatic inhibitory activity of active ingredients in the oral mouth rinse products: aloin A and B, chlorhexidine, eucalyptol, hexetidine, menthol, triclosan, methyl salicylate, sodium fluoride and povidone, against two important proteases of SARS-CoV-2 PLpro and 3CLpro. Our results indicate only aloin A and B effectively inhibited proteolytic activity of PLpro with an IC
    MeSH term(s) Animals ; Binding Sites ; COVID-19/pathology ; COVID-19/virology ; Cell Survival/drug effects ; Chlorocebus aethiops ; Coronavirus 3C Proteases/antagonists & inhibitors ; Coronavirus 3C Proteases/metabolism ; Coronavirus Papain-Like Proteases/antagonists & inhibitors ; Coronavirus Papain-Like Proteases/metabolism ; Emodin/analogs & derivatives ; Emodin/chemistry ; Emodin/metabolism ; Emodin/pharmacology ; Humans ; Molecular Dynamics Simulation ; Protein Isoforms/chemistry ; Protein Isoforms/metabolism ; Protein Isoforms/pharmacology ; SARS-CoV-2/enzymology ; SARS-CoV-2/isolation & purification ; Vero Cells
    Chemical Substances Protein Isoforms ; 3C-like proteinase, SARS-CoV-2 (EC 3.4.22.-) ; Coronavirus Papain-Like Proteases (EC 3.4.22.2) ; papain-like protease, SARS-CoV-2 (EC 3.4.22.2) ; Coronavirus 3C Proteases (EC 3.4.22.28) ; Emodin (KA46RNI6HN) ; alloin (W41H6S09F4)
    Language English
    Publishing date 2022-02-09
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2615211-3
    ISSN 2045-2322 ; 2045-2322
    ISSN (online) 2045-2322
    ISSN 2045-2322
    DOI 10.1038/s41598-022-06104-y
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Identification of 3-chymotrypsin like protease (3CLPro) inhibitors as potential anti-SARS-CoV-2 agents.

    Mody, Vicky / Ho, Joanna / Wills, Savannah / Mawri, Ahmed / Lawson, Latasha / Ebert, Maximilian C C J C / Fortin, Guillaume M / Rayalam, Srujana / Taval, Shashidharamurthy

    Communications biology

    2021  Volume 4, Issue 1, Page(s) 93

    Abstract: Emerging outbreak of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) infection is a major threat to public health. The morbidity is increasing due to lack of SARS-CoV-2 specific drugs. Herein, we have identified potential drugs that target ... ...

    Abstract Emerging outbreak of severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) infection is a major threat to public health. The morbidity is increasing due to lack of SARS-CoV-2 specific drugs. Herein, we have identified potential drugs that target the 3-chymotrypsin like protease (3CLpro), the main protease that is pivotal for the replication of SARS-CoV-2. Computational molecular modeling was used to screen 3987 FDA approved drugs, and 47 drugs were selected to study their inhibitory effects on SARS-CoV-2 specific 3CLpro enzyme in vitro. Our results indicate that boceprevir, ombitasvir, paritaprevir, tipranavir, ivermectin, and micafungin exhibited inhibitory effect towards 3CLpro enzymatic activity. The 100 ns molecular dynamics simulation studies showed that ivermectin may require homodimeric form of 3CLpro enzyme for its inhibitory activity. In summary, these molecules could be useful to develop highly specific therapeutically viable drugs to inhibit the SARS-CoV-2 replication either alone or in combination with drugs specific for other SARS-CoV-2 viral targets.
    MeSH term(s) Antiviral Agents/chemistry ; Antiviral Agents/pharmacology ; COVID-19/drug therapy ; COVID-19/virology ; Coronavirus 3C Proteases/antagonists & inhibitors ; Coronavirus 3C Proteases/chemistry ; Coronavirus 3C Proteases/metabolism ; Cysteine Proteinase Inhibitors/chemistry ; Cysteine Proteinase Inhibitors/pharmacology ; Drug Discovery ; Humans ; Ligands ; Molecular Docking Simulation ; Molecular Dynamics Simulation ; Protein Binding ; Protein Conformation ; SARS-CoV-2/drug effects ; SARS-CoV-2/enzymology ; Structure-Activity Relationship ; Virus Replication/drug effects
    Chemical Substances Antiviral Agents ; Cysteine Proteinase Inhibitors ; Ligands ; Coronavirus 3C Proteases (EC 3.4.22.28)
    Language English
    Publishing date 2021-01-20
    Publishing country England
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ISSN 2399-3642
    ISSN (online) 2399-3642
    DOI 10.1038/s42003-020-01577-x
    Database MEDical Literature Analysis and Retrieval System OnLINE

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