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  • ||||||||||  MRT68921 / University of Dundee
    Journal:  Inhibition of autophagy initiation: A novel strategy for oral squamous cell carcinomas. (Pubmed Central) -  Jan 15, 2024   
    In conclusion, this study identified a combination of novel autophagy inhibitors which can potently inhibit proliferation of both chemosensitive as well as chemoresistant OSCC cells and could be developed as a novel therapy against advanced OSCC tumors.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Journal:  Comprehensive Analysis of MICALL2 Reveals Its Potential Roles in EGFR Stabilization and Ovarian Cancer Cell Invasion. (Pubmed Central) -  Jan 15, 2024   
    Furthermore, MICALL2 silencing promoted EGFR degradation; however, this effect was abrogated by treatment with the autophagy inhibitors acadesine and chloroquine diphosphate...Collectively, our results indicated that MICALL2 participated in the process of immune infiltration and invasion by ovarian cancer cells. Moreover, MICALL2 prevented EGFR degradation in a Rac1-dependent manner, consequently leading to EGFR-AKT-mTOR-MMP9 signaling activation and invadopodia-mediated matrix degradation.
  • ||||||||||  Journal:  COPI Vesicle Disruption Inhibits Mineralization via mTORC1-Mediated Autophagy. (Pubmed Central) -  Jan 15, 2024   
    Inhibition of mTOR1 rescues the impaired osteogenesis by activating autophagy. Collectively, our study highlights the functional importance of COPI in mineralization and identifies COPI as a potential therapeutic target for treating bone-related diseases.
  • ||||||||||  AZD0156 / AstraZeneca
    Journal:  Antioxidants and azd0156 Rescue Inflammatory Response in Autophagy-Impaired Macrophages. (Pubmed Central) -  Jan 15, 2024   
    Importantly, the chemical activation of autophagy or ATM inhibition during M1 polarization reduced the M1 phenotype and inflammation, whereas inhibiting autophagy during M2 polarization also reduced the M2 phenotype. Thus, our findings highlight the importance of the autophagy-ATM pathway in driving macrophage inflammation.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  Capsaicin Attenuates LPS-Induced Acute Lung Injury by Inhibiting Inflammation and Autophagy Through Regulation of the TRPV1/AKT Pathway. (Pubmed Central) -  Jan 15, 2024   
    The autophagy agonist rapamycin (Rapa) and the autophagy inhibitors 3-methyladenine (3-MA) and bafilomycin A1 (Baf-A1) were used to clarify the characteristics of LPS-induced autophagy...Furthermore, prior administration of CAP provided substantial protection to mice against ALI induced by LPS, reduced the lung wet/dry ratio, decreased proinflammatory cytokine expression, and downregulated LC3 expression. Taken together, our results indicate that CAP protects against LPS-induced ALI by inhibiting inflammatory responses and autophagic death through the TRPV1/AKT signaling pathway, presenting a novel strategy for ALI therapy.
  • ||||||||||  Journal:  LKB1 depletion-mediated epithelial-mesenchymal transition induces fibroblast activation in lung fibrosis. (Pubmed Central) -  Jan 15, 2024   
    3D co-cultures of ATII cells and MRC5 lung fibroblasts coupled with RNA sequencing (RNA-seq) confirmed that paracrine signalling between LKB1-depleted ATII cells and fibroblasts augmented myofibroblast differentiation. Together these data suggest that reduced autophagy caused by LKB1 inhibition can induce EMT in ATII cells and contribute to fibrosis via aberrant epithelial-fibroblast crosstalk.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Preclinical, Journal:  Role of autophagy in betaine-promoted hepatoprotection against non-alcoholic fatty liver disease in mice. (Pubmed Central) -  Jan 15, 2024   
    To determine the role of autophagy in the improvement of NAFLD, chloroquine (CQ), an autophagy inhibitor, was injected into the mice fed a CDAHFD and betaine (0.5 % in drinking water)...Notably, the betaine-induced improvements in lipid metabolism determined by protein levels of p-AMPK, p-ACC, PPAR?, and ACS1, were reversed by CQ. Thus, the results of this study suggest that the activation of autophagy is an important upstream mechanism for the inhibition of steatosis, ER stress, and apoptosis by betaine in NAFLD.
  • ||||||||||  Journal:  Synergistic interplay of UV radiation and urban particulate matter induces impairment of autophagy and alters cellular fate in senescence-prone human dermal fibroblasts. (Pubmed Central) -  Jan 13, 2024   
    Whereas UPM treatment in isolation did not affect proliferation or survival of HDF, of note, simultaneous UPM treatment of UV-irradiated cells selectively inhibited autophagic flux, thereby changing cell fate of a fraction of the cell population from senescence to apoptotic cell death. Our findings highlight the synergistic effects of UV radiation and UPM on skin aging, emphasizing the need to consider these factors in assessing the impact of environmental stressors on human health and opening opportunities for developing comprehensive approaches to protect and preserve skin integrity in the face of growing environmental challenges.
  • ||||||||||  hydroquinone / Generic mfg.
    Journal:  MicroRNA-204-5p Ameliorates Renal Injury via Regulating Keap1/Nrf2 Pathway in Diabetic Kidney Disease. (Pubmed Central) -  Jan 10, 2024   
    In vitro, high glucose-induced HK-2 cells were treated with miR-204-5p inhibitor, miR-204-5p mimics, ATG5 siRNA, tertiary butyl hydroquinone (TBHQ), ML385, or 3-Methyladenine (3-MA)...Furthermore, the binding of miR-204-5p with Keap1 was confirmed by luciferase reporter assay and miR-204-5p negatively regulated Keap1 expression, resulting in the activation of Nrf2 pathway. MicroRNA-204-5p protects against the progression of diabetic renal fibrosis by restoring autophagy via regulating Keap1/Nrf2 pathway.
  • ||||||||||  Journal:  Puerarin reduces cell damage from cerebral ischemia-reperfusion by inhibiting ferroptosis. (Pubmed Central) -  Jan 10, 2024   
    Further, the use of 3-Methyladenine, an autophagy inhibitor, underscores the significance of autophagy in managing OGD/R-induced stress. These findings suggest Puerarin's potential as a therapeutic agent for conditions characterized by ischemic cellular damage, highlighting the need for further clinical exploration.
  • ||||||||||  dexmedetomidine / Generic mfg.
    Biomarker, Journal:  Dexmedetomidine Alleviates Ischemia/Reperfusion-Associated Acute Kidney Injury by Enhancing Autophagic Activity via the ?2-AR/AMPK/mTOR Pathway. (Pubmed Central) -  Jan 9, 2024   
    Furthermore, we identified the FDA-approved small molecule STING inhibitor, Pabocilib, as an effective attenuator of LIRI during lung transplant in rats.Conclusion Our study not only illuminates the pivotal role of the cGAS/STING pathway through the non-canonical PRK signaling in LIRI, but also identifies a promising molecular drug for PGD. These analyses provide strong evidence for the ability of DEX to protect against I/R-associated AKI via the ?2-AR/AMPK/mTOR pathway-mediated enhancement of autophagic activity.
  • ||||||||||  Journal:  Hyperglycemia exacerbates cerebral ischemia/reperfusion injury by up-regulating autophagy through p53-Sesn2-AMPK pathway. (Pubmed Central) -  Jan 9, 2024   
    Finally, experiments with autophagy inhibitors 3-MA and aldose reductase inhibitor (ARI) revealed that while both inhibitors reduced the number of TUNEL positive neurons and reversed the effects of hyperglycemic ischemia on LC3 and p62, only ARI decreased the levels of p53, P-p53. These results suggested that hyperglycemia might induce excessive autophagy to aggravate the brain injury resulted from I/R and that hyperglycemia might activate the p53-Sesn2-AMPK signaling pathway, in addition to the classical PI3K/AKT/mTOR autophagy pathway.
  • ||||||||||  Journal:  TRPM2-dependent autophagy inhibition exacerbates oxidative stress-induced CXCL16 secretion by keratinocytes in vitiligo. (Pubmed Central) -  Jan 8, 2024   
    Taken together, our findings show that cell density is a significant contributor in shaping cancer chemosensitivity, that the ISDS (aka the Ujwal Punyamurtula/Wafik El-Deiry or Ujwal-WAF Index) can be used to effectively assess cell viability and that this phenomenon of density-dependent chemoresistance may be leveraged for a variety of biologic and cancer therapeutic applications. Inhibition of TRPM2 may serve as a potential target for the treatment of vitiligo.
  • ||||||||||  Truqap (capivasertib) / Otsuka, AstraZeneca
    Journal:  The role and mechanism of AZD5363 anti-leukemia activity in T-cell acute lymphoblastic leukemia. (Pubmed Central) -  Jan 8, 2024   
    Targeting the expression of miR-26a-5p, as well as inhibiting the activation of autophagy and the NLRP3 inflammasome pathway, could offer additional treatments for pathological cardiac hypertrophy. AZD5363 suppressed T-ALL progression and its anti-leukemia activity was enhanced by HCQ in T-ALL cells, which might provide a potential therapeutic strategy for human T-ALL.
  • ||||||||||  Victoza (liraglutide) / Novo Nordisk
    Glp-1Ras Regulate Lipid Metabolism and induce Autophagy Through Ampk/Sirt1 Pathway to Improve NAFLD (Room 15, J) -  Jan 6, 2024 - Abstract #APASL2024APASL_689;    
    We investigated whether the therapeutic effect of liraglutide (LRG, a representative drug of GLP-1RAs) on hepatic steatosis is related to regulating lipid metabolism and enhancing autophagy in the hepatocytes... GLP-1RAs may improve hepatic steatosis by regulating lipid metabolism and enhancing autophagy in an APMK/SIRT1- dependent manner, which providing a new target for the treatment of NAFLD.
  • ||||||||||  Journal:  Lipid and cholesterols modulate the dynamics of SARS-CoV-2 viral ion channel ORF3a and its pathogenic variants. (Pubmed Central) -  Jan 5, 2024   
    We also infer that loss of stability primarily grounds for pathogenicity in more than half of the pathogenic variants of ORF3a. Overall, the effect of mutation on alteration of ion permeability of ORF3a, proposed in this study brings mechanistic insights into variant consequences on viral membrane proteins of SARS-CoV-2, which can be utilized for the development of novel therapeutics to treat COVID-19 and other coronavirus diseases.
  • ||||||||||  Journal:  Network pharmacology mechanisms and experimental verification of licorice in the treatment of ulcerative colitis. (Pubmed Central) -  Jan 4, 2024   
    Overall, the effect of mutation on alteration of ion permeability of ORF3a, proposed in this study brings mechanistic insights into variant consequences on viral membrane proteins of SARS-CoV-2, which can be utilized for the development of novel therapeutics to treat COVID-19 and other coronavirus diseases. Licorice improves UC, which may be related to the activation of the Nrf2/PINK1 signaling pathway that regulates autophagy.
  • ||||||||||  Journal:  FUNDC1-induced mitophagy protects spinal cord neurons against ischemic injury. (Pubmed Central) -  Jan 4, 2024   
    The protective effects of FUNDC1 against apoptosis and mitochondrial dysfunction were reversed by 3-methyladenine (3-MA), an autophagy inhibitor. Taken together, our results confirm that FUNDC1 can protect against neuronal loss after SCI by inducing mitophagy, inhibiting mitochondria-dependent apoptosis, and improving mitochondrial function.