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  • ||||||||||  cisplatin / Generic mfg., paclitaxel / Generic mfg.
    Journal:  Hederagenin potentiated cisplatin- and paclitaxel-mediated cytotoxicity by impairing autophagy in lung cancer cells. (Pubmed Central) -  Mar 26, 2021   
    The aberrant acidic environment then impaired the function of lysosome, which was evidenced by the decrease of mature cathepsin B and cathepsin D. Lastly, hederagenin, in agree with our hypothesis, promoted pro-apoptotic effect of cisplatin and paclitaxel with the accumulation of reactive oxygen species (ROS); while the synergistic effect could be abolished by the ROS scavenger, N-acetyl-L-cysteine. These data summarily demonstrated hederagenin-induced accumulation of ROS by blocking autophagic flux potentiated the cytotoxicity of cisplatin and paclitaxel in lung cancer cells.
  • ||||||||||  Clinical, Journal:  Exploitation of DHODH and p53 activation as therapeutic targets - a case study in polypharmacology. (Pubmed Central) -  Mar 26, 2021   
    These mechanisms are the inhibition of a key enzyme of the de novo pyrimidine synthesis pathway, DHODH, and the blockage of uridine transport into cells. These findings hold a three-fold significance; firstly, we demonstrate that tenovins, and perhaps other compounds that activate p53, may activate p53 by more than one mechanism; secondly, that work previously conducted with certain tenovins as SirT1 inhibitors should additionally be viewed through the lens of DHODH inhibition as this is a major contributor to the mechanism of action of the most widely used tenovins; and finally, that small changes in the structure of a small molecule can lead to a dramatic change in the target profile of the molecule even when the phenotypic readout remains static.
  • ||||||||||  Journal:  Autophagy Mediates Leptin-Induced Migration and ERK Activation in Breast Cancer Cells. (Pubmed Central) -  Mar 26, 2021   
    Although leptin differentially induced autophagy in the breast cancer cell lines tested, autophagy inhibition reduced leptin-induced cell proliferation in MCF7 cells and decreased cell migration, ERK activation, and impaired morphological changes in both cell lines. Our data demonstrates an important role for basal autophagy or leptin-induced autophagy in leptin-induced migration and ERK phosphorylation in breast cancer cell lines, suggesting a potential use for the inhibition of autophagy in breast cancer associated with obesity.
  • ||||||||||  pimozide / Generic mfg.
    Journal, IO biomarker:  Pimozide Suppresses the Growth of Brain Tumors by Targeting STAT3-Mediated Autophagy. (Pubmed Central) -  Mar 25, 2021   
    The chronic administration of pimozide showed no general signs of toxicity, and the behavioral activity of the mice remained unchanged. Taken together, these results indicate that pimozide inhibits the growth of brain cancer by autophagy-mediated apoptosis.
  • ||||||||||  sirolimus / Generic mfg.
    Preclinical, Journal:  TNFα enhances trovafloxacin-induced in vitro hepatotoxicity by inhibiting protective autophagy. (Pubmed Central) -  Mar 23, 2021   
    These results indicate that TVX activates protective autophagy in HepG2 cells exposed to toxicity and an imbalance in negative feedback regulation of autophagy by TNFα synergistically enhanced the toxicity. The finding from this study may contribute to a better understanding of the mechanisms underlying iDILI associated with inflammatory stress.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Preclinical, Journal:  Graphene oxide induces dose-dependent lung injury in rats by regulating autophagy. (Pubmed Central) -  Mar 23, 2021   
    The autophagy inhibitors 3-methyladenine (3-MA) and chloroquine (CLQ) inhibited autophagy in the lung and attenuated GO-induced lung injury, as demonstrated by a reduced lung wet-to-dry weight ratio, lower levels of protein in the bronchoalveolar lavage fluid, and a reduced lung injury score...The results revealed that ATG5 knockdown-induced autophagic inhibition significantly decreased cellular injury and oxidative stress, suggesting that autophagy induction is a key event that leads to lung injury during exposure to GO. In conclusion, the findings of the present study indicated that GO causes lung injury in a dose-dependent manner by inducing autophagy.
  • ||||||||||  Tasigna (nilotinib) / Novartis, Inhibikase
    Journal:  α-Synucleinopathy associated c-Abl activation causes p53-dependent autophagy impairment. (Pubmed Central) -  Mar 20, 2021   
    The TSA effect may be mediated by inhibition of HDAC1/2 involved in autophagy and pyroptosis process. Collectively, our data show that c-Abl activation by α-synucleinopathy causes p53 dependent autophagy deficits and both c-Abl and p53 represent therapeutic target for PD.
  • ||||||||||  Review, Journal:  Extracellular Vesicles as a Novel Therapeutic Option in Liver Transplantation. (Pubmed Central) -  Mar 20, 2021   
    Once generated, the efficient delivery of EVs to the donor organ prior to transplantation remains an issue which could be resolved through the novel organ storage method ex vivo machine perfusion (EVMP). In this review, we summarize studies which have used tolerogenic cell derived EVs to ameliorate hepatic IRI and promote liver allograft acceptance, discuss the steps toward generation of clinical-grade EVs, and introduce EVMP as a novel method to efficiently deliver EVs.
  • ||||||||||  Journal:  LncRNA CCAT1 functions as apoptosis inhibitor in podocytes via autophagy inhibition. (Pubmed Central) -  Mar 19, 2021   
    Taken together, our results suggested that CCAT1 induction critically participated in apoptosis inhibition in podocytes through autophagy inhibition via increasing PI3K/Akt signaling. This might act as a promising therapeutic intervention for renal diseases associated with podocyte apoptosis.
  • ||||||||||  SB202190 / Amgen
    Journal:  Origanum majorana Essential Oil Triggers p38 MAPK-Mediated Protective Autophagy, Apoptosis, and Caspase-Dependent Cleavage of P70S6K in Colorectal Cancer Cells. (Pubmed Central) -  Mar 19, 2021   
    Blockade of autophagy with 3-methyladenine (3-MA) and chloroquine (CQ), two autophagy inhibitors, potentiated the OMEO-induced apoptotic cell death...Pharmacological inhibition of p38 MAPK by the p38 inhibitors SB 202190 and SB 203580 not only significantly decreased apoptotic cell death, but also reduced the autophagy level in OMEO treated HT-29 cells...Our findings suggest that OMEO inhibits colon cancer through p38 MAPK-mediated protective autophagy and apoptosis associated with caspase-dependent cleavage of p70S6K. To the best of our knowledge, this study is the first to report on the implications of the p38 MAPK signaling pathway in targeting p70S6K to caspase cleavage.
  • ||||||||||  Isentress (raltegravir) / Merck (MSD)
    Journal:  HIV Nef and Antiretroviral Therapy Have an Inhibitory Effect on Autophagy in Human Astrocytes that May Contribute to HIV-Associated Neurocognitive Disorders. (Pubmed Central) -  Mar 19, 2021   
    We studied in-bulk and selective autophagic flux in primary human astrocytes treated with extracellular Nef and/or a combination of tenofovir+emtricitabine+raltegravir (ART) using Western blotting, a tandem fluorescent LC3 reporter, and transmission electron microscopy/morphometry...Dysregulation of both autophagic processes is maintained after 7 days of Nef and/or ART treatment. Persistent autophagy dysregulation due to chronic Nef and/or ART exposure may ultimately result in astrocyte and neuronal dysfunction, contributing to HAND.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Journal:  Effects of the autophagy modulators d-limonene and chloroquine on vimentin levels in SH-SY5Y cells. (Pubmed Central) -  Mar 19, 2021   
    Our findings suggest an inverse relationship between vimentin reduction and LC3-II accumulation, whose causal link needs to be examined. Further experiments are needed to dissect the role of vimentin reduction in the mechanisms through which CQ impairs fusion of autophagosome with lysosomes as well as in other effects of this drug.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Journal:  Chloroquine: autophagy inhibitor, antimalarial, bitter taste receptor agonist in fight against COVID-19, a reality check? (Pubmed Central) -  Mar 19, 2021   
    Further, we also highlight some of cell-based mechanism(s) that CQ and its derivatives affect in mediating variety of physiological responses in the cell. We believe, data emanating from the clinical studies and continual understanding of the fundamental mechanisms may potentially help in designing effective therapeutic strategies that meets both efficacy and safety criteria for COVID-19.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  Macrophage autophagy regulates mitochondria-mediated apoptosis and inhibits necrotic core formation in vulnerable plaques. (Pubmed Central) -  Mar 18, 2021   
    Application of ApoE mice with rapamycin (an autophagy inducer) inhibited necrotic core formation in vulnerable plaques by decreasing macrophage apoptosis...Finally, we found that MAPK-NF-κB signalling pathway was involved in autophagy modulation of 7-KC-induced macrophage apoptosis. So, we provide strong evidence for the potential therapeutic benefit of macrophage autophagy in regulating mitochondria-mediated apoptosis and inhibiting necrotic core formation in vulnerable plaques.
  • ||||||||||  [VIRTUAL] IDENTIFICATION OF A NOVEL ANTI-HIV miRNA IN INTERLEUKIN-27– DIFFERENTIATED MACROPHAGES () -  Mar 18, 2021 - Abstract #CROI2021CROI_389;    
    Collectively, CRNDE silencing alleviates HIBD, at least partially, through promoting autophagy. We discovered a total of 38 novel microRNAs in AB mac and characterized that, dual-function miRNA, miRAB40, may provide novel insights into the miRNA-mediated regulation of autophagy induction and HIV inhibition via IFN expression.
  • ||||||||||  Journal:  Sirt1 coordinates with ERα to regulate autophagy and adiposity. (Pubmed Central) -  Mar 17, 2021   
    Moreover, Sirt1 deacetylated ERα, which constituted a positive feedback loop in the regulation of autophagy and adiposity. Our results revealed a new mechanism of Sirt1 regulating autophagy in adipocytes and shed light on sex difference in adiposity.
  • ||||||||||  Journal:  Targeting Autophagy Augments BBR-Mediated Cell Death in Human Hepatoma Cells Harboring Hepatitis C Virus RNA. (Pubmed Central) -  Mar 17, 2021   
    Finally, BBR inhibited the growth of Huh-7 cells that were persistently infected with the full-length genome HCV particles, and concomitant pharmacological inhibition of autophagy potentiated the killing of these cells by BBR. Our findings suggest that combining BBR with the inhibition of autophagy could be an attractive treatment strategy against HCC, irrespective of the presence of the HCV genome.
  • ||||||||||  erastin - Whitehead Institute for Biomedical Research, Dana / Farber Cancer Institute, Columbia University, Prolexys
    Journal:  SIRT3 deficiency is resistant to autophagy-dependent ferroptosis by inhibiting the AMPK/mTOR pathway and promoting GPX4 levels. (Pubmed Central) -  Mar 17, 2021   
    We concluded that upregulated SIRT3-enhanced autophagy activation by promoting AMPK-mTOR pathway and decreasing GPX4 level to induce ferroptosis in trophoblastic cells. SIRT3 deficiency was resistant to high glucose- and erastin-induced autophagy-dependent ferroptosis and is, therefore, a potential therapeutic approach for treating GDM.