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  1. AU="Mansoor, Farheen"
  2. AU="Stanton, Clive"
  3. AU=Herholz K AU=Herholz K
  4. AU="Marichal, Axel"
  5. AU="Camon, Ana M"
  6. AU="Randall, Michael D"

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  1. Artikel ; Online: Exploring bi-carbazole-linked triazoles as inhibitors of prolyl endo peptidase via integrated in vitro and in silico study.

    Ullah, Saeed / Mansoor, Farheen / Khan, Salman Ali / Jabeen, Uzma / Almars, Amany I / Almohaimeed, Hailah M / Basri, Ahmed M / Alshabrmi, Fahad M

    Scientific reports

    2024  Band 14, Heft 1, Seite(n) 7675

    Abstract: A serine protease called prolyl endopeptidase (PEP) hydrolyses the peptide bonds on the carboxy side of the proline ring. The excessive PEP expression in brain results in neurodegenerative illnesses like dementia, Alzheimer's disease, and Parkinson's ... ...

    Abstract A serine protease called prolyl endopeptidase (PEP) hydrolyses the peptide bonds on the carboxy side of the proline ring. The excessive PEP expression in brain results in neurodegenerative illnesses like dementia, Alzheimer's disease, and Parkinson's disease. Results of the prior studies on antioxidant activity, and the non-cytotoxic effect of bi-carbazole-linked triazoles, encouraged us to extend our studies towards its anti-diabetic potential. Hence, for this purpose all compounds 1-9 were evaluated to reveal their anti-prolyl endo peptidase activity. Fortunately, seven compounds resulted into significant inhibitory capability ranging from 26 to 63 µM. Among them six compounds 4-9 exhibited more potent inhibitory activity with IC
    Mesh-Begriff(e) Peptide Hydrolases ; Triazoles/pharmacology ; Triazoles/chemistry ; Prolyl Oligopeptidases ; Serine Endopeptidases ; Carbazoles ; Structure-Activity Relationship ; Molecular Docking Simulation
    Chemische Substanzen Peptide Hydrolases (EC 3.4.-) ; Triazoles ; Prolyl Oligopeptidases (EC 3.4.21.26) ; Serine Endopeptidases (EC 3.4.21.-) ; Carbazoles
    Sprache Englisch
    Erscheinungsdatum 2024-04-01
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 2615211-3
    ISSN 2045-2322 ; 2045-2322
    ISSN (online) 2045-2322
    ISSN 2045-2322
    DOI 10.1038/s41598-024-58428-6
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  2. Artikel ; Online: In-vitro inhibition of NLRP3 inflammasome by 3,6-dihydroxyflavone (3,6-DHF): a therapeutic strategy for the treatment of chronic inflammatory and autoimmune diseases.

    Mansoor, Farheen / Jabeen, Almas / Shah, Syeda Farah / Simjee, Shabana U / Bano, Samina / Faizi, Shaheen

    Molecular and cellular biochemistry

    2022  Band 478, Heft 3, Seite(n) 555–570

    Abstract: Nucleotide-binding oligomerization domain (NOD)-like receptor family pyrin domain containing 3 (NLRP3) inflammasome complex has an important role in immune system and its abnormal activation is associated with the pathogenesis of various inflammatory and ...

    Abstract Nucleotide-binding oligomerization domain (NOD)-like receptor family pyrin domain containing 3 (NLRP3) inflammasome complex has an important role in immune system and its abnormal activation is associated with the pathogenesis of various inflammatory and auto-immune diseases. The study reveals the anti-inflammatory effects of 3,6-dihydroxyflavone (3,6-DHF). Here, we aimed to determine the inhibitory effects of 3,6-DHF on NLRP3 inflammasome and its associated components, thereby determining the signaling pathways involved in the inhibition. Reactive oxygen species (ROS) and nitric oxide (NO) were quantified by chemiluminescence and Griess methods, respectively. Inflammatory cell model was induced in human leukemic monocytes (THP-1). mRNA levels were estimated through real-time RT-PCR, protein expressions were evaluated by protein slot blot and immunocytochemistry, MTT and alamar blue assays were employed for toxicity studies. The compound 3,6-DHF was found to be the potent inhibitor of NLRP3 inflammasome by targeting the molecules involve in its activation pathway. Anti-inflammatory effects were revealed by inhibition of ROS and NO, reduction in the transcription of caspase-1, ASC, IL-1β and TLR-4 was observed along with the marked inhibition of NLRP3, IL-18, NF-κB and pNF-κB at translational level. 3,6-DHF was non-toxic on normal human fibroblast (BJ) and THP-1 cells and, could be a potential therapeutic agent in NLRP3 inflammasome driven diseases.
    Mesh-Begriff(e) Humans ; Inflammasomes/metabolism ; NLR Family, Pyrin Domain-Containing 3 Protein/metabolism ; Reactive Oxygen Species/metabolism ; NF-kappa B/metabolism ; Inflammation ; Caspase 1/metabolism ; Autoimmune Diseases ; Anti-Inflammatory Agents ; Interleukin-1beta/metabolism
    Chemische Substanzen Inflammasomes ; NLR Family, Pyrin Domain-Containing 3 Protein ; Reactive Oxygen Species ; 3,6-dihydroxyflavone ; NF-kappa B ; Caspase 1 (EC 3.4.22.36) ; Anti-Inflammatory Agents ; Interleukin-1beta
    Sprache Englisch
    Erscheinungsdatum 2022-08-11
    Erscheinungsland Netherlands
    Dokumenttyp Journal Article
    ZDB-ID 184833-1
    ISSN 1573-4919 ; 0300-8177
    ISSN (online) 1573-4919
    ISSN 0300-8177
    DOI 10.1007/s11010-022-04527-9
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  3. Artikel ; Online: Biochemical and computational inhibition of α-glucosidase by novel metronidazole-linked 1

    Ullah, Saeed / Halim, Sobia Ahsan / Waqas, Muhammad / Mansoor, Farheen / Avula, Satya Kumar / Khan, Farhan A / Perviaz, Muhammad / Ogaly, Hanan A / Khan, Ajmal / Al-Harrasi, Ahmed

    Journal of biomolecular structure & dynamics

    2024  , Seite(n) 1–21

    Abstract: In the current study, metronidazole derivatives containing ... ...

    Abstract In the current study, metronidazole derivatives containing 1
    Sprache Englisch
    Erscheinungsdatum 2024-03-03
    Erscheinungsland England
    Dokumenttyp Journal Article
    ZDB-ID 49157-3
    ISSN 1538-0254 ; 0739-1102
    ISSN (online) 1538-0254
    ISSN 0739-1102
    DOI 10.1080/07391102.2024.2322622
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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    Verfügbar in ZB MED Köln/Königswinter

    Zs.A 2093: Hefte anzeigen Standort:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

    Über subito bestellen

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