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  1. Book ; Online: Natural and Synthetic Bioactives for Skin Health, Disease and Management

    Chamcheu, Jean Christopher / Walker, Anthony L / Noubissi-Kamdem, Felicite

    2022  

    Keywords Research & information: general ; Biology, life sciences ; keratinocytes ; rutin ; ascorbic acid ; UV radiation ; proteomics ; 3D cell culture ; borage oil ; triacylglycerol metabolism ; acyl-ceramide ; corneocyte lipid envelope ; epidermis ; anti-melanogenesis ; B16/F10 melanoma cell ; hydroxyoctadecadienoic acid ; Sorghum bicolor ; 3-isobutyl-1-methylxanthine ; mycosis fungoides ; atopic dermatitis ; cutaneous lymphomas ; cornified envelope proteins ; FLG ; microalgae ; Planktochlorella nurekis ; skin cells ; proliferation ; senescence ; holothuroids ; glycosaminoglycans ; inflammation ; ear-inflammation ; whey ; Lactobacillus helveticus ; melanin ; α-melanocyte-stimulating hormone ; tyrosinase ; tyrosinase-related protein 1 ; dopachrome tautomerase ; microphthalmia-associated transcription factor ; cosmetics ; black cumin ; Nigella sativa ; Thymocid® ; skin aging ; glycation ; collagen ; collagenase ; elastase ; melanogenesis ; cosmeceutical ; konjac glucomannan ; ultraviolet B ; human epidermal primary melanocytes ; human embryonic fibroblasts ; anti-inflammatory activity ; antioxidant activity ; Cornus officinalis ; molecular docking ; human high-affinity IgE receptors ; α-MSH ; UVB irradiation ; lotus seedpod extract ; epigallocatechin ; propolis ; skin ; matrix metalloproteinase-1 ; UV ; phosphoinositide 3-kinase ; skin care ; skin health ; bioactive substances ; phytonutrients ; antioxidants ; nutraceuticals ; Perilla frutescens ; cell proliferation ; ultraviolet radiation ; DNA repair ; Lactobacillus plantarum CJLP55 ; acne vulgaris ; sebum ; hydration ; urine bacterial extracellular vesicles ; fungal infections ; nanohydrogel ; polysaccharide ; essential oils ; eggshell membrane ; keratinocyte differentiation ; TRPV ; skin thickness ; Lithospermum erythrorhizon ; NC/Nga ; Th1 ; Th2 ; Th17 ; Th22 ; immune balance ; skin barrier function ; n/a
    Language English
    Size 1 electronic resource (314 pages)
    Publisher MDPI - Multidisciplinary Digital Publishing Institute
    Publishing place Basel
    Document type Book ; Online
    Note English
    HBZ-ID HT030379618
    ISBN 9783036560687 ; 3036560688
    Database ZB MED Catalogue: Medicine, Health, Nutrition, Environment, Agriculture

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  2. Article ; Online: The PI3K-Akt-mTOR and Associated Signaling Pathways as Molecular Drivers of Immune-Mediated Inflammatory Skin Diseases: Update on Therapeutic Strategy Using Natural and Synthetic Compounds.

    Roy, Tithi / Boateng, Samuel T / Uddin, Mohammad B / Banang-Mbeumi, Sergette / Yadav, Rajesh K / Bock, Chelsea R / Folahan, Joy T / Siwe-Noundou, Xavier / Walker, Anthony L / King, Judy A / Buerger, Claudia / Huang, Shile / Chamcheu, Jean Christopher

    Cells

    2023  Volume 12, Issue 12

    Abstract: The dysregulated phosphatidylinositol-3-kinase (PI3K)-Akt-mammalian target of rapamycin (mTOR) signaling pathway has been implicated in various immune-mediated inflammatory and hyperproliferative dermatoses such as acne, atopic dermatitis, alopecia, ... ...

    Abstract The dysregulated phosphatidylinositol-3-kinase (PI3K)-Akt-mammalian target of rapamycin (mTOR) signaling pathway has been implicated in various immune-mediated inflammatory and hyperproliferative dermatoses such as acne, atopic dermatitis, alopecia, psoriasis, wounds, and vitiligo, and is associated with poor treatment outcomes. Improved comprehension of the consequences of the dysregulated PI3K/Akt/mTOR pathway in patients with inflammatory dermatoses has resulted in the development of novel therapeutic approaches. Nonetheless, more studies are necessary to validate the regulatory role of this pathway and to create more effective preventive and treatment methods for a wide range of inflammatory skin diseases. Several studies have revealed that certain natural products and synthetic compounds can obstruct the expression/activity of PI3K/Akt/mTOR, underscoring their potential in managing common and persistent skin inflammatory disorders. This review summarizes recent advances in understanding the role of the activated PI3K/Akt/mTOR pathway and associated components in immune-mediated inflammatory dermatoses and discusses the potential of bioactive natural products, synthetic scaffolds, and biologic agents in their prevention and treatment. However, further research is necessary to validate the regulatory role of this pathway and develop more effective therapies for inflammatory skin disorders.
    MeSH term(s) Humans ; Phosphatidylinositol 3-Kinase/metabolism ; Proto-Oncogene Proteins c-akt/metabolism ; Phosphatidylinositol 3-Kinases/metabolism ; Signal Transduction ; TOR Serine-Threonine Kinases/metabolism ; Psoriasis/drug therapy ; Dermatitis ; Sirolimus ; Biological Products/pharmacology ; Biological Products/therapeutic use
    Chemical Substances Phosphatidylinositol 3-Kinase (EC 2.7.1.137) ; Proto-Oncogene Proteins c-akt (EC 2.7.11.1) ; Phosphatidylinositol 3-Kinases (EC 2.7.1.-) ; TOR Serine-Threonine Kinases (EC 2.7.11.1) ; Sirolimus (W36ZG6FT64) ; Biological Products
    Language English
    Publishing date 2023-06-20
    Publishing country Switzerland
    Document type Journal Article ; Review ; Research Support, Non-U.S. Gov't ; Research Support, N.I.H., Extramural
    ZDB-ID 2661518-6
    ISSN 2073-4409 ; 2073-4409
    ISSN (online) 2073-4409
    ISSN 2073-4409
    DOI 10.3390/cells12121671
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Dual targeting of mTOR/IL-17A and autophagy by fisetin alleviates psoriasis-like skin inflammation.

    Roy, Tithi / Banang-Mbeumi, Sergette / Boateng, Samuel T / Ruiz, Emmanuelle M / Chamcheu, Roxane-Cherille N / Kang, Lin / King, Judy A / Walker, Anthony L / Nagalo, Bolni Marius / Kousoulas, Konstantin G / Esnault, Stephane / Huang, Shile / Chamcheu, Jean Christopher

    Frontiers in immunology

    2023  Volume 13, Page(s) 1075804

    Abstract: Psoriasis is a chronic autoimmune inflammatory skin disorder characterized by epidermal hyperplasia and aberrant immune response. In addition to aberrant cytokine production, psoriasis is associated with activation of the Akt/mTOR pathway. mTOR/S6K1 ... ...

    Abstract Psoriasis is a chronic autoimmune inflammatory skin disorder characterized by epidermal hyperplasia and aberrant immune response. In addition to aberrant cytokine production, psoriasis is associated with activation of the Akt/mTOR pathway. mTOR/S6K1 regulates T-lymphocyte activation and migration, keratinocytes proliferation and is upregulated in psoriatic lesions. Several drugs that target Th1/Th17 cytokines or their receptors have been approved for treating psoriasis in humans with variable results necessitating improved therapies. Fisetin, a natural dietary polyphenol with anti-oxidant and anti-proliferative properties, covalently binds mTOR/S6K1. The effects of fisetin on psoriasis and its underlying mechanisms have not been clearly defined. Here, we evaluated the immunomodulatory effects of fisetin on Th1/Th17-cytokine-activated adult human epidermal keratinocytes (HEKa) and anti-CD3/CD28-stimulated inflammatory CD4
    MeSH term(s) Humans ; Animals ; Mice ; Interleukin-17/metabolism ; Proto-Oncogene Proteins c-akt/metabolism ; Phosphatidylinositol 3-Kinases/metabolism ; Psoriasis ; Dermatitis ; TOR Serine-Threonine Kinases/metabolism ; Inflammation/metabolism ; Imiquimod/adverse effects ; Cytokines/metabolism ; Disease Models, Animal ; Autophagy ; Sirolimus/therapeutic use
    Chemical Substances fisetin (OO2ABO9578) ; Interleukin-17 ; Proto-Oncogene Proteins c-akt (EC 2.7.11.1) ; Phosphatidylinositol 3-Kinases (EC 2.7.1.-) ; TOR Serine-Threonine Kinases (EC 2.7.11.1) ; Imiquimod (P1QW714R7M) ; Cytokines ; Sirolimus (W36ZG6FT64) ; MTOR protein, human (EC 2.7.1.1)
    Language English
    Publishing date 2023-01-18
    Publishing country Switzerland
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, U.S. Gov't, Non-P.H.S.
    ZDB-ID 2606827-8
    ISSN 1664-3224 ; 1664-3224
    ISSN (online) 1664-3224
    ISSN 1664-3224
    DOI 10.3389/fimmu.2022.1075804
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Role and Therapeutic Targeting of the PI3K/Akt/mTOR Signaling Pathway in Skin Cancer: A Review of Current Status and Future Trends on Natural and Synthetic Agents Therapy.

    Chamcheu, Jean Christopher / Roy, Tithi / Uddin, Mohammad Burhan / Banang-Mbeumi, Sergette / Chamcheu, Roxane-Cherille N / Walker, Anthony L / Liu, Yong-Yu / Huang, Shile

    Cells

    2019  Volume 8, Issue 8

    Abstract: The mammalian or mechanistic target of rapamycin (mTOR) and associated phosphatidyl-inositiol 3-kinase (PI3K)/protein kinase B (Akt) pathways regulate cell growth, differentiation, migration, and survival, as well as angiogenesis and metabolism. ... ...

    Abstract The mammalian or mechanistic target of rapamycin (mTOR) and associated phosphatidyl-inositiol 3-kinase (PI3K)/protein kinase B (Akt) pathways regulate cell growth, differentiation, migration, and survival, as well as angiogenesis and metabolism. Dysregulation of these pathways is frequently associated with genetic/epigenetic alterations and predicts poor treatment outcomes in a variety of human cancers including cutaneous malignancies like melanoma and non-melanoma skin cancers. Recently, the enhanced understanding of the molecular and genetic basis of skin dysfunction in patients with skin cancers has provided a strong basis for the development of novel therapeutic strategies for these obdurate groups of skin cancers. This review summarizes recent advances in the roles of PI3K/Akt/mTOR and their targets in the development and progression of a broad spectrum of cutaneous cancers and discusses the current progress in preclinical and clinical studies for the development of PI3K/Akt/mTOR targeted therapies with nutraceuticals and synthetic small molecule inhibitors.
    MeSH term(s) Animals ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Biological Products/pharmacology ; Biological Products/therapeutic use ; Clinical Trials as Topic ; Humans ; Molecular Targeted Therapy ; Phosphatidylinositol 3-Kinases/metabolism ; Proto-Oncogene Proteins c-akt/metabolism ; Signal Transduction/drug effects ; Skin Neoplasms/drug therapy ; Skin Neoplasms/metabolism ; TOR Serine-Threonine Kinases/metabolism
    Chemical Substances Antineoplastic Agents ; Biological Products ; MTOR protein, human (EC 2.7.1.1) ; TOR Serine-Threonine Kinases (EC 2.7.1.1) ; Proto-Oncogene Proteins c-akt (EC 2.7.11.1)
    Language English
    Publishing date 2019-07-31
    Publishing country Switzerland
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 2661518-6
    ISSN 2073-4409 ; 2073-4409
    ISSN (online) 2073-4409
    ISSN 2073-4409
    DOI 10.3390/cells8080803
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Identification of new fisetin analogs as kinase inhibitors: Data on synthesis and anti-skin cancer activities evaluation.

    Roy, Tithi / Boateng, Samuel T / Banang-Mbeumi, Sergette / Singh, Pankaj K / Basnet, Pratik / Chamcheu, Roxane-Cherille N / Ladu, Federico / Chauvin, Isabel / Spiegelman, Vladimir S / Hill, Ronald A / Kousoulas, Konstantin G / Nagalo, Bolni Marius / Walker, Anthony L / Fotie, Jean / Murru, Siva / Sechi, Mario / Chamcheu, Jean Christopher

    Data in brief

    2021  Volume 35, Page(s) 106858

    Abstract: This article contains supplemental datasets of the recently published related research ... ...

    Abstract This article contains supplemental datasets of the recently published related research article
    Language English
    Publishing date 2021-02-10
    Publishing country Netherlands
    Document type Journal Article
    ZDB-ID 2786545-9
    ISSN 2352-3409 ; 2352-3409
    ISSN (online) 2352-3409
    ISSN 2352-3409
    DOI 10.1016/j.dib.2021.106858
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article: Identification of new fisetin analogs as kinase inhibitors: Data on synthesis and anti-skin cancer activities evaluation

    Roy, Tithi / Boateng, Samuel T. / Banang-Mbeumi, Sergette / Singh, Pankaj K. / Basnet, Pratik / Chamcheu, Roxane-Cherille N. / Ladu, Federico / Chauvin, Isabel / Spiegelman, Vladimir S. / Hill, Ronald A. / Kousoulas, Konstantin G. / Nagalo, Bolni Marius / Walker, Anthony L. / Fotie, Jean / Murru, Siva / Sechi, Mario / Chamcheu, Jean Christopher

    Data in Brief. 2021 Apr., v. 35

    2021  

    Abstract: This article contains supplemental datasets of the recently published related research article “Synthesis, Inverse Docking-Assisted Identification and in vitro Biological Characterization of Flavonol-based Analogs of Fisetin as c-Kit, CDK2 and mTOR ... ...

    Abstract This article contains supplemental datasets of the recently published related research article “Synthesis, Inverse Docking-Assisted Identification and in vitro Biological Characterization of Flavonol-based Analogs of Fisetin as c-Kit, CDK2 and mTOR Inhibitors against Melanoma and Non-melanoma Skin Cancers” by Roy et al., [1]. It provides in-depth data not included in the original co-submission on the biophysical, molecular docking, and biological characterization of newly synthesized flavonol-based analogs of fisetin, a natural dietary small molecule with anticancer and anti-inflammatory properties. These synthetic small molecules were investigated as new, potential single and/or multi-kinase inhibitors of the cyclin-dependent kinase-2 (CDK2), receptor tyrosine kinases (c-KITs), and mammalian targets of rapamycin (mTOR) targets, potentially active against melanoma or non-melanoma skin cancers. Furthermore, this data-in-brief article comprises additional sets of results on several aspects of the properties of the dual and multiple kinase inhibitor compounds’ effects that were not presented in the associated article, including the activated targets that are dysregulated in skin cancers; the effects on markers of apoptosis; on colony formation; and in scratch wound healing assays. The study has identified a panel of novel fisetin analogs that are either single- or multi-kinase inhibitors, which may be further developed as active for the treatment of melanoma and non-melanoma skin cancers. The dataset presented herein will be utilized for additional studies aiming to establish a biological platform to steer for predictive and experimental screening of novel flavonoids and analogs in relevant organoids, humanized animal models and in vivo disease models. The present results should also serve as a key stepping-stone towards enabling target-structure-based design, synthesis and initial testing of novel analogs or derivatives of fisetin. The current study may eventually lead to the development of safe, promising and preclinical candidate entities for treatment of skin and other forms of cancers as well as various other human diseases, which can possibly add to the general armamentarium of promising and safe drugs for health promotion.
    Keywords apoptosis ; cyclin-dependent kinase ; data collection ; flavonoids ; health promotion ; humans ; melanoma ; organoids ; rapamycin ; receptor protein-tyrosine kinase
    Language English
    Dates of publication 2021-04
    Publishing place Elsevier Inc.
    Document type Article
    ZDB-ID 2786545-9
    ISSN 2352-3409
    ISSN 2352-3409
    DOI 10.1016/j.dib.2021.106858
    Database NAL-Catalogue (AGRICOLA)

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  7. Article ; Online: Synthesis, inverse docking-assisted identification and in vitro biological characterization of Flavonol-based analogs of fisetin as c-Kit, CDK2 and mTOR inhibitors against melanoma and non-melanoma skin cancers.

    Roy, Tithi / Boateng, Samuel T / Banang-Mbeumi, Sergette / Singh, Pankaj K / Basnet, Pratik / Chamcheu, Roxane-Cherille N / Ladu, Federico / Chauvin, Isabel / Spiegelman, Vladimir S / Hill, Ronald A / Kousoulas, Konstantin G / Nagalo, Bolni Marius / Walker, Anthony L / Fotie, Jean / Murru, Siva / Sechi, Mario / Chamcheu, Jean Christopher

    Bioorganic chemistry

    2020  Volume 107, Page(s) 104595

    Abstract: Due to hurdles, including resistance, adverse effects, and poor bioavailability, among others linked with existing therapies, there is an urgent unmet need to devise new, safe, and more effective treatment modalities for skin cancers. Herein, a series of ...

    Abstract Due to hurdles, including resistance, adverse effects, and poor bioavailability, among others linked with existing therapies, there is an urgent unmet need to devise new, safe, and more effective treatment modalities for skin cancers. Herein, a series of flavonol-based derivatives of fisetin, a plant-based flavonoid identified as an anti-tumorigenic agent targeting the mammalian targets of rapamycin (mTOR)-regulated pathways, were synthesized and fully characterized. New potential inhibitors of receptor tyrosine kinases (c-KITs), cyclin-dependent kinase-2 (CDK2), and mTOR, representing attractive therapeutic targets for melanoma and non-melanoma skin cancers (NMSCs) treatment, were identified using inverse-docking, in vitro kinase activity and various cell-based anticancer screening assays. Eleven compounds exhibited significant inhibitory activities greater than the parent molecule against four human skin cancer cell lines, including melanoma (A375 and SK-Mel-28) and NMSCs (A431 and UWBCC1), with IC
    MeSH term(s) Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Apoptosis/drug effects ; Cell Proliferation/drug effects ; Cell Survival/drug effects ; Cyclin-Dependent Kinase 2/antagonists & inhibitors ; Cyclin-Dependent Kinase 2/metabolism ; Dose-Response Relationship, Drug ; Drug Screening Assays, Antitumor ; Flavonols/chemical synthesis ; Flavonols/chemistry ; Flavonols/pharmacology ; Humans ; Melanoma/drug therapy ; Melanoma/metabolism ; Melanoma/pathology ; Molecular Docking Simulation ; Molecular Structure ; Proto-Oncogene Proteins c-kit/antagonists & inhibitors ; Proto-Oncogene Proteins c-kit/metabolism ; Skin Neoplasms/drug therapy ; Skin Neoplasms/metabolism ; Skin Neoplasms/pathology ; Structure-Activity Relationship ; TOR Serine-Threonine Kinases/antagonists & inhibitors ; TOR Serine-Threonine Kinases/metabolism ; Tumor Cells, Cultured
    Chemical Substances Antineoplastic Agents ; Flavonols ; MTOR protein, human (EC 2.7.1.1) ; KIT protein, human (EC 2.7.10.1) ; Proto-Oncogene Proteins c-kit (EC 2.7.10.1) ; TOR Serine-Threonine Kinases (EC 2.7.11.1) ; CDK2 protein, human (EC 2.7.11.22) ; Cyclin-Dependent Kinase 2 (EC 2.7.11.22) ; fisetin (OO2ABO9578)
    Language English
    Publishing date 2020-12-30
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2020.104595
    Database MEDical Literature Analysis and Retrieval System OnLINE

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