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  • ||||||||||  danusertib (PHA-739358) / Nerviano Medical Sciences
    Journal:  Augmentation of danusertib's anticancer activity against melanoma by blockage of autophagy. (Pubmed Central) -  Oct 7, 2020   
    Thus, the induction of autophagy by danusertib appears to be a survival mechanism in melanoma cells that may counteract its anticancer effects. These findings suggest a novel strategy to enhance the anticancer efficacy of danusertib in melanoma by blocking autophagy.
  • ||||||||||  Journal:  Effects of evodiamine on PI3K/Akt and MAPK/ERK signaling pathways in pancreatic cancer cells. (Pubmed Central) -  Oct 7, 2020   
    The tumor expression of phosphorylated AKT, detected using immunohistochemistry, decreased with increasing EVO doses in vivo. EVO induced PC cell apoptosis by inhibiting phosphoinositide 3‑kinase/AKT and mitogen‑activated protein kinase/ERK and inhibiting the phosphorylation of signal transducer and activator of transcription activator 3 in PC cells to inhibit autophagy, suggesting that EVO may be considered as a novel PC treatment.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Journal:  Prostaglandin F2α Induces Goat Corpus Luteum Regression via Endoplasmic Reticulum Stress and Autophagy. (Pubmed Central) -  Oct 7, 2020   
    To reveal the function of ER stress and autophagy in the CL regression process induced by PGF2α, we used 4-phenyl butyric acid (4-PBA) and chloroquine (CQ) for inhibiting ER stress and autophagy, respectively...In addition, knockdown of EIF2S1, which blocked the PERK pathway activation, promoted apoptosis by reducing autophagy in goat luteal cells treated with PGF2α. In conclusion, our study indicates that ER stress promotes goat luteal cell apoptosis to regulate the regression of CL and activates autophagy to inhibit the goat luteal cell apoptosis via PERK signaling pathway.
  • ||||||||||  Journal:  Dysregulation of autophagy and stress granule-related proteins in stress-driven Tau pathology. (Pubmed Central) -  Oct 3, 2020   
    Interestingly, an mTOR-driven pharmacological stimulation of autophagy attenuates the GC-driven accumulation of Tau and SG-related proteins as well as the related cell death, suggesting a critical interface between autophagy and the response of the SG-related protein in the neurodegenerative potential of chronic stress and GC. These studies provide novel insights into the RNA-protein intracellular signaling regulating the precipitating role of environmental stress and GC on Tau-driven brain pathology.
  • ||||||||||  bortezomib / Generic mfg.
    Journal:  Cdc37 Contributes to bortezomib resistance in multiple myeloma via autophagy (Pubmed Central) -  Oct 3, 2020   
    Suppressing Cdc37 expression in MM cell line NCI-H929 induced BTZ resistance and autophagy activation, while CQ could rescue BTZ resistance caused by Cdc37 inhibition. Cdc37 may participate in BTZ resistance in MM via the regulation of autophagy activity.
  • ||||||||||  Journal:  Cationic gold nanoparticles elicit mitochondrial dysfunction: a multi-omics study. (Pubmed Central) -  Oct 2, 2020   
    Moreover, the cationic Au-NPs triggered autophagy in macrophage-like RFP-GFP-LC3 reporter cells, and cell death was aggravated upon inhibition of autophagy. Taken together, these studies have disclosed mitochondria-dependent effects of cationic Au-NPs resulting in the rapid demise of the cells.
  • ||||||||||  bleomycin / Generic mfg., BMS
    Journal:  PGC-1α regulates autophagy to promote fibroblast activation and tissue fibrosis. (Pubmed Central) -  Oct 2, 2020   
    PGC-1α is upregulated in SSc and promotes autophagy to foster TGFβ-induced fibroblast activation. Targeting of PGC-1α prevents aberrant autophagy, inhibits fibroblast activation and tissue fibrosis and may over therapeutic potential.
  • ||||||||||  hydroxychloroquine / Generic mfg.
    Journal:  Pharmacophore hybridisation and nanoscale assembly to discover self-delivering lysosomotropic new-chemical entities for cancer therapy. (Pubmed Central) -  Oct 2, 2020   
    The selected BAQ12 and BAQ13 ONNs are highly effective in inducing lysosomal disruption, lysosomal dysfunction and autophagy blockade and exhibit 30-fold higher antiproliferative activity than hydroxychloroquine used in clinical trials...In addition, they are able to encapsulate and deliver additional drugs to tumour sites and are thus promising agents for autophagy inhibition-based combination therapy. Given their transdisciplinary advantages, these BAQ ONNs have enormous potential to improve cancer therapy.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Journal:  Salidroside induces apoptosis and protective autophagy in human gastric cancer AGS cells through the PI3K/Akt/mTOR pathway. (Pubmed Central) -  Oct 1, 2020   
    Furthermore, treatment with the autophagy inhibitor chloroquine enhanced salidroside-induced cell apoptosis, indicating that the autophagy mediated by salidroside may protect AGS cells from death...The above findings indicate that salidroside inhibited the growth of gastric cancer and induced apoptosis and protective autophagy through the PI3K/Akt/mTOR pathway. In summary, our study provides novel insights regarding the activity of salidroside against gastric cancer and contributes to the clinical application of salidroside combined with autophagy inhibitors as a chemotherapeutic strategy for human gastric cancer.
  • ||||||||||  Journal:  Membrane and synaptic defects leading to neurodegeneration in Adar mutant Drosophila are rescued by increased autophagy. (Pubmed Central) -  Oct 1, 2020   
    In summary, our study provides novel insights regarding the activity of salidroside against gastric cancer and contributes to the clinical application of salidroside combined with autophagy inhibitors as a chemotherapeutic strategy for human gastric cancer. These findings link Drosophila Adar mutant synaptic and neurotransmission defects to more general cellular defects in autophagy; presumably, edited isoforms of CNS proteins are required for optimum synaptic response capabilities in the brain during the behaviorally complex adult life stage.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Journal:  Bismuth embedded silica nanoparticles loaded with autophagy suppressant to promote photothermal therapy. (Pubmed Central) -  Sep 30, 2020   
    Here, we investigated bismuth crystals embedded silica (Bi@SiO) nanoparticles, loaded with an autophagy inhibitor (chloroquine, CQ)...Both in vitro and in vivo anti-tumor effects were consequently promoted owing to the combined effects enabled by Bi@SiO-CQ nanoparticles under mild NIR irradiation conditions. This study demonstrates a potential new PTT platform with superior therapeutic efficacy.
  • ||||||||||  sirolimus / Generic mfg.
    Preclinical, Journal:  Autophagy Promotes Porcine Parvovirus Replication and Induces Non-Apoptotic Cell Death in Porcine Placental Trophoblasts. (Pubmed Central) -  Sep 30, 2020   
    Induction of autophagy by rapamycin (RAPA) inhibited the occurrence of apoptotic cell death, yet promoted viral replication in PPV-infected cells; inhibition of autophagy by 3-MA or ATG5 knockdown increased cellular apoptosis and reduced PPV replication...Meanwhile, induction of complete autophagy with RAPA increased lysosomal damage and non-apoptotic cell death in the later phase of PPV infection. Therefore, our data suggest that autophagy can enhance PPV replication and promote the occurrence of lysosomal-damage-associated non-apoptotic cell death in PPV-infected porcine placental trophoblasts.
  • ||||||||||  JQ-1 / Roche
    Journal:  Inhibition of Brd4 by JQ1 Promotes Functional Recovery From Spinal Cord Injury by Activating Autophagy. (Pubmed Central) -  Sep 30, 2020   
    In the mechanistic analysis, we observed that modulation of the AMPK-mTOR-ULK1 pathway is involved in the activation of autophagy mediated by Brd4 inhibition. Taken together, the results of our investigation provides compelling evidence that Brd4 inhibition by JQ1 promotes functional recovery after SCI and that Brd4 may serve as a potential target for SCI treatment.
  • ||||||||||  Journal, IO Biomarker:  Cucurbitacin E Induces Autophagy-Involved Apoptosis in Intestinal Epithelial Cells. (Pubmed Central) -  Sep 30, 2020   
    An autophagy inhibitor, 3-methyladenine, reduced CuE-induced apoptosis. These results suggest that CuE may induce apoptosis and autophagy in IECs via the PI3K/AKT/mTOR signaling pathway and that autophagy following endoplasmic reticulum stress participates in the pro-apoptotic process induced by CuE.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Journal:  The SIRT6-Autophagy-Warburg Effect Axis in Papillary Thyroid Cancer. (Pubmed Central) -  Sep 30, 2020   
    Treatment with the ROS scavenger N-acetyl-L-cysteine (NAC, 5 mM) or the autophagy inhibitor chloroquine (CQ) both rescued the inhibition of the Warburg effect...In conclusion, we identified a SIRT6-ROS-ER stress-autophagy-GLUT1-Warburg effect axis in PTC, which may provide a new therapeutic target. In addition, NAC (low concentration) and CQ, previously considered to be tumor inhibitors, were shown to promote tumorigenesis in PTC with high SIRT6 expression by inducing the Warburg effect.
  • ||||||||||  Journal:  Voltage-switchable HCl transport enabled by lipid headgroup-transporter interactions. (Pubmed Central) -  Sep 27, 2020   
    By studying anion binding affinity and transport mechanisms of four other anion transporters, we show that the lack of uniport and the voltage-dependent H+/Cl- symport originate from strong binding to lipid phosphate headgroup that hampers the diffusion of the free transporters through the membranes, leading to an unusual H+/Cl- symport mechanism that involves only charged species. Our work provides important mechanistic insights into different classes of anion transporters and a new approach to achieve voltage-switchability in artificial membrane transport systems.
  • ||||||||||  Journal:  Corosolic Acid Ameliorates Cardiac Hypertrophy via Regulating Autophagy. (Pubmed Central) -  Sep 27, 2020   
    Therefore, miR-21-5p could be a new therapeutic target, to replace EB irradiation, and control keloid relapse. These results suggest that CRA may protect against cardiac hypertrophy through regulating AMPK-dependent autophagy.
  • ||||||||||  Review, Journal:  Glioblastoma: targeting the autophagy in tumorigenesis. (Pubmed Central) -  Sep 26, 2020   
    In this review, we highlight the molecular links between GBM and autophagy with the focus on the effects of autophagy on the stemness maintenance, metabolism and proteostasis in GBM tumorigenesis. Understanding the molecular pathways involved in autophagy target is critical for GBM therapy.
  • ||||||||||  Journal:  Mitochondrial Perturbations Couple mTORC2 to Autophagy in C. elegans. (Pubmed Central) -  Sep 26, 2020   
    Importantly, we find that inactivation of mTORC2-SGK-1 signaling impairs mitochondrial homeostasis and triggers an increased release of mitochondria-derived reactive oxygen species (mtROS) to induce autophagy. Thus, mitochondrial stress couples reduced mTORC2 activity to enhanced autophagic turnover.
  • ||||||||||  Journal:  FGF21 augments autophagy in random-pattern skin flaps via AMPK signaling pathways and improves tissue survival. (Pubmed Central) -  Sep 26, 2020   
    In our mechanistic investigation, we found that FGF21-induced autophagy enhancement is mediated by the dephosphorylation and nuclear translocation of TFEB; this effect was due to activation of AMPK-FoxO3a-SPK2-CARM1 and AMPK-mTOR signaling pathways. Together, our data provides novel evidence that FGF21 is a potent modulator of autophagy capable of significantly increasing random skin flap viability, and thus may serve as a promising therapy for clinical use.
  • ||||||||||  Review, Journal:  Autophagy-related MicroRNAs in chronic lung diseases and lung cancer. (Pubmed Central) -  Sep 26, 2020   
    Herein, we documented that up/down regulation of miRNAs can activate or inhibit autophagy in chronic lung diseases including lung cancer. Therefore, theses miRNAs could be a promising therapeutic tool for lung cancer specially in drug-resistance lung cancer cells.
  • ||||||||||  Journal:  Autophagy regulates levels of tumor suppressor enzyme protein phosphatase 6. (Pubmed Central) -  Sep 26, 2020   
    Accordingly, protein levels of PP6 and p62 fluctuate in concert under different physiological and pathophysiological conditions. Our data reveal that PP6 is regulated by p62-dependent autophagy and suggest that accumulation of PP6 protein in tumor tissues is caused at least partially by deficiency in autophagy.