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  • ||||||||||  cisplatin / Generic mfg.
    Review, Journal:  Autophagy modulating agents as chemosensitizers for cisplatin therapy in cancer. (Pubmed Central) -  Feb 3, 2022   
    Such a strategy encompasses not only simple autophagy inhibition but also harnessing the process to induce autophagy-dependent cell death. In this paper, we briefly describe the mechanism of cisplatin resistance with a special emphasis on autophagy and we give an extensive literature review of potential substances with cisplatin chemosensitising properties related to autophagy modulation.
  • ||||||||||  Byetta (exenatide) / AstraZeneca
    Preclinical, Journal:  Neuroprotection of Exendin-4 by Enhanced Autophagy in a Parkinsonian Rat Model of α-Synucleinopathy. (Pubmed Central) -  Feb 3, 2022   
    Taken together, our results demonstrate that exendin-4 treatment relieved behavioral deficits, dopaminergic degeneration, and pathological α-synuclein aggregation in a parkinsonian rat model of α-synucleinopathy and that these effects were mediated by enhanced autophagy via inhibiting the PI3K/Akt/mTOR pathway. In light of the safety and tolerance of exendin-4 administration, our results suggest that exendin-4 may represent a promising disease-modifying treatment for Parkinson's disease.
  • ||||||||||  sirolimus / Generic mfg., doxorubicin hydrochloride / Generic mfg.
    Journal:  PLAC8 promotes adriamycin resistance via blocking autophagy in breast cancer. (Pubmed Central) -  Feb 3, 2022   
    Thus, our findings suggest that PLAC8, through the participation of p62, inhibits autophagy and consequently results in ADM resistance in breast cancer. PLAC8/p62 pathway may act as novel therapeutic targets in breast cancer treatment and has potential clinical application in overcoming ADM resistance.
  • ||||||||||  Review, Journal:  Alantolactone: a sesquiterpene lactone with diverse pharmacological effects. (Pubmed Central) -  Feb 3, 2022   
    This review summarizes the recent advances of the pharmacological effects of Ala, including anti-inflammatory, antitumor, antimicrobial, neuroprotective activities, as well as the underlying mechanisms. Ala might be employed as a potential lead to develop drugs for multiple diseases.
  • ||||||||||  Preclinical, Journal:  Collagen type I enhance cell growth and insulin biosynthesis in rat pancreatic cells. (Pubmed Central) -  Feb 2, 2022   
    That is, autophagy negatively regulates nuclear translocation of β-catenin that leads to insulin biosynthesis and cell proliferation. In conclusion, IGF-1R/down regulation of autophagy/nuclear translocation of β-catenin is involved in collagen I-induced INS-1 cell proliferation and insulin synthesis.
  • ||||||||||  Review, Journal:  Post-Ischemic Brain Neurodegeneration in the Form of Alzheimer's Disease Proteinopathy: Possible Therapeutic Role of Curcumin. (Pubmed Central) -  Feb 2, 2022   
    Studies in animal models of cerebral ischemia have shown that curcumin reduces infarct volume, brain edema, blood-brain barrier permeability, apoptosis, neuroinflammation, glutamate neurotoxicity, inhibits autophagy and oxidative stress, and improves neurological and behavioral deficits. The available data suggest that curcumin may be a new therapeutic substance in both regenerative medicine and the treatment of neurodegenerative disorders such as post-ischemic neurodegeneration.
  • ||||||||||  Review, Journal:  The Onco-immunological Implications of F nucleatum in Breast Cancer. (Pubmed Central) -  Feb 1, 2022   
    This results in cell growth and treatment resistance through autophagy as well as immune evasion. Targeted treatment directed at F. nucleatum combined with immunotherapy and autophagy inhibitors might therefore be a feasible treatment strategy for breast cancer patients.
  • ||||||||||  Preclinical, Journal:  Features of the Population of Mouse Peritoneal Macrophages Isolated after Stimulation with Concanavalin A and Thioglycolate. (Pubmed Central) -  Feb 1, 2022   
    Macrophages obtained after administration of concanavalin A have reduced mitochondrial potential, which reflects a tendency to apoptosis. Autophagy activation and inhibition neutralize the differences in pro- and anti-inflammatory properties of polarized macrophages obtained after thioglycolate administration, but have less pronounced effect on macrophages obtained after administration concanavalin A. Autophagy inhibitor increases mitochondrial potential in non-polarized macrophages obtained after administration of concanavalin A. These results demonstrate divergent properties of macrophages obtained after administration of glycolate and concanavalin A due to the difference in the mechanisms of experimental peritonitis.
  • ||||||||||  SHP099 / Novartis
    Journal:  Polygala saponins inhibit NLRP3 inflammasome-mediated neuroinflammation via SHP2-Mediated mitophagy. (Pubmed Central) -  Feb 1, 2022   
    In Aβ(1-42)-, A53T-α-synuclein-, or Q74-induced BV-2 cells, PSS significantly inhibited NLRP3 inflammasome activation, which was attenuated by bafilomycin A1 (an autophagy inhibitor) and SHP099 (an SHP-2 inhibitor)...In APP/PS1 mice, PSS improved cognitive function, ameliorated Aβ pathology, and inhibited neuronal death. Collectively, the present study, for the first time, shows that PSS inhibit the NLRP3 inflammasome via SHP-2-mediated mitophagy in vitro and in vivo, which strongly suggests the therapeutic potential of PSS in various neurodegenerative diseases.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  Macroautophagy involved in testosterone synthesis in Leydig cells of male dairy goat (Capra hircus). (Pubmed Central) -  Feb 1, 2022   
    In contrast, treatment with rapamycin (an autophagy activator), enhanced steroidogenesis in LCs. Collectively, these in vivo and in vitro results suggested that autophagy activity is related to steroidogenesis in LCs of dairy goats, which may ultimately influence the spermatogenesis and fertility of these animals.
  • ||||||||||  LY294002 / Eli Lilly
    Journal:  CWHM-1008 Induces Apoptosis and Protective Autophagy through the Akt/mTOR Axis in LUAD Cells. (Pubmed Central) -  Feb 1, 2022   
    Potential effects of an autophagy inhibitor (LY294002) and constitutively active Akt plasmid (CA-Akt) on CWHM-1008-induced apoptosis were also examined...Moreover, CWHM-1008 significantly inhibited the growth and induced apoptosis of A549 cell in nude mice in vivo. The present findings provide new insights into anticancer properties of CWHM-1008, suggesting that it may be an adjuvant treatment for LUAD treatment, warranting further study.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  Oridonin Alleviates LPS-Induced Depression by Inhibiting NLRP3 Inflammasome via Activation of Autophagy. (Pubmed Central) -  Feb 1, 2022   
    Lipopolysaccharide (LPS)-induced depression models were established both in C57BL/6 mice and primary astrocytes, which were treated with Ori, autophagy agonist Rapamycin (Rap) and autophagy inhibitor 3-Methyladenine (3-MA)...The therapeutic effect of Ori was enhanced by Rap and weakened by 3-MA. Collectively, our findings provided a promising antidepressant drug and uncovered that Ori alleviated LPS-induced depression by inhibiting NLRP3 inflammasome through activation of autophagy.
  • ||||||||||  hydroxychloroquine / Generic mfg., cisplatin / Generic mfg.
    Autophagy as a therapeutic target in head and neck squamous cell carcinoma () -  Feb 1, 2022 - Abstract #ECHNOICHNO2022ECHNO_ICHNO_161;    
    Furthermore, chemotherapy - comprised of autophagy inhibition and Cisplatin - and radiotherapy combined showed a significant decrease in cell viability in 2D and 3D cell culture. Conclusion Chemically targeting autophagy with specific inhibitors in established HNSCC cell lines shows significant reduction of cell viability and impairment of cancer cell migration.
  • ||||||||||  LY294002 / Eli Lilly, dorsomorphin (Compound C) / EMD Serono
    Journal, PARP Biomarker:  Arsenic induces autophagy-dependent apoptosis via Akt inactivation and AMPK activation signaling pathways leading to neuronal cell death. (Pubmed Central) -  Jan 29, 2022   
    Expectedly, inhibition of Akt signaling with LY294002 obviously enhanced As-triggered autophagy and apoptosis...Taken together, these results indicated that As exerted its cytotoxicity in neuronal cells via the Akt inactivation/AMPK activation downstream-regulated autophagy-dependent apoptosis pathways, which ultimately lead to cell death. Our findings suggest that the regulation of Akt/AMPK signals may be a promising intervention to against As-induced neurotoxicity and NDs.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Preclinical, Journal:  Food-derived cyanidin-3-O-glucoside alleviates oxidative stress: evidence from the islet cell line and diabetic db/db mice. (Pubmed Central) -  Jan 29, 2022   
    More importantly, an autophagy inhibitor chloroquine (CQ) was added to verify our findings at the protein level, and we observed the co-localization of mitochondria and lysosomes, which may form autophagolysosomes to clean damaged mitochondria...This was demonstrated by increased levels of ROS, and the impaired activities of anti-oxidative enzymes superoxide dismutase (SOD) and catalase (CAT) were partly reversed by C3G intervention. Our study has provided evidence for the alleviation effect of C3G against oxidative stress in pancreas islets, which may provide enlightenment for improving the health situation of diabetic patients in the future.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Journal:  DJ-1 deficiency in hepatocytes improves liver ischemia-reperfusion injury by enhancing mitophagy. (Pubmed Central) -  Jan 28, 2022   
    We demonstrate that DJ-1 down-regulation in both human and mouse liver tissues in response to I/R injury, and Dj-1 deficiency in hepatocytes but not in myeloid cells could significantly ameliorate I/R induced liver injury and inflammatory responses. This hepatoprotective effects was dependent on enhanced autophagy in Dj-1 knockout mice, because inhibition of autophagy by 3-Methyladenine (3-MA) and chloroquine (CQ) could reverse the protective effect on hepatic I/R injury in Dj-1 knockout mice Dj-1 deficiency in hepatocytes significantly enhanced mitochondrial accumulation and protein stability of PARKIN, which in turn promotes the onset of mitophagy resulting in elevated clearance of damaged mitochondria during I/R injury.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Journal:  Hypoxia via ERK signaling inhibits hepatic PPARα to promote fatty liver. (Pubmed Central) -  Jan 28, 2022   
    This hepatoprotective effects was dependent on enhanced autophagy in Dj-1 knockout mice, because inhibition of autophagy by 3-Methyladenine (3-MA) and chloroquine (CQ) could reverse the protective effect on hepatic I/R injury in Dj-1 knockout mice Dj-1 deficiency in hepatocytes significantly enhanced mitochondrial accumulation and protein stability of PARKIN, which in turn promotes the onset of mitophagy resulting in elevated clearance of damaged mitochondria during I/R injury. Overall, our results demonstrate that ERK activated by hypoxia signaling plays a crucial role in fatty acid β-oxidation genes by repressing hepatocyte PPARα signaling.
  • ||||||||||  Farydak (panobinostat) / Secura Bio
    Journal:  Modulation of pancreatic neuroendocrine neoplastic cell fate by autophagy mediated death. (Pubmed Central) -  Jan 27, 2022   
    2D and 3D human pNEN and pancreatic stellate cells were treated with panobinostat and bafilomycin...Discussion/Conclusion Our study highlights that the autophagy functional restoration and prolongation of this catabolic process, mediated by inhibition of deacetylase, is responsible for the reduction of pNEN cells. Prompting of autophagy cell death could be a promising strategy for the therapy of pNEN.
  • ||||||||||  Gilotrif (afatinib) / Boehringer Ingelheim
    Journal:  Afatinib induces pro-survival autophagy and increases sensitivity to apoptosis in stem-like HNSCC cells. (Pubmed Central) -  Jan 27, 2022   
    This suggested that blocking autophagy has the potential to serve as a promising strategy to target HNSCC stem cells. In conclusion, our findings suggested that the combination treatment with afatinib and autophagy inhibitors has the potential to eradicate HNSCC cells, especially cancer stem cells in clinical therapy.
  • ||||||||||  Journal:  IRF1 inhibits autophagy-mediated proliferation of colorectal cancer via targeting ATG13. (Pubmed Central) -  Jan 27, 2022   
    ATG13, an important factors of autophagy complex, was confirmed as a target of IRF1. These findings indicated that IRF1 function as a tumor suppressor in CRC and inhibit autophagy through ATG13, targeting this pathway may provide new insights into the molecular mechanisms of CRC progression.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Journal:  Ouabain and chloroquine trigger senolysis of BRAF-V600E-induced senescent cells by targeting autophagy. (Pubmed Central) -  Jan 27, 2022   
    Consequently, we identified autophagy inhibitor chloroquine as a novel senolytic in BRAF senescence based on the mode of action of cardioglycosides. Our work underlies the interest of characterizing the mechanisms of senolytics to discover novel compounds and identifies the endoplasmic reticulum stress-autophagy tandem as a new vulnerability in BRAF senescence that can be exploited for the development of further senolytic strategies.