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  • ||||||||||  LY294002 / Eli Lilly
    Preclinical, Journal:  1-Monopalmitin promotes lung cancer cells apoptosis through PI3K/Akt pathway in vitro. (Pubmed Central) -  Jul 19, 2023   
    1-Mono induced cytoprotective autophagy since autophagy inhibitor Chloroquine dramatically enhanced 1-Mono-induced cytotoxicity. In summary, our results showed 1-Mono kills lung cancer through PI3K/Akt pathway, providing novel options for lung cancer administration.
  • ||||||||||  Journal:  Potent New Targets for Autophagy Enhancement to Delay Neuronal Ageing. (Pubmed Central) -  Jul 18, 2023   
    Molecules that specifically inhibit Rab2 or Arl8 serve as potent drug candidates to modulate the activity of the autophagic process in treating neurodegenerative pathologies. In the future, it would be reasonable to investigate which GAP enzyme can inhibit Rab2 or Arl8 specifically, but not affect Rab7, with similar medical purposes.
  • ||||||||||  ezurpimtrostat (GNS561) / Genoscience Pharma, Genfit, Avastin (bevacizumab) / Roche, Tecentriq (atezolizumab) / Roche
    Review, Journal, Checkpoint inhibition:  Update on Autophagy Inhibitors in Cancer: Opening up to a Therapeutic Combination with Immune Checkpoint Inhibitors. (Pubmed Central) -  Jul 18, 2023   
    GNS561, a PPT1 inhibitor, is a promising autophagy modulator as it has started a phase 2 clinical trial in liver cancer indication, combined with atezolizumab and bevacizumab, an assessment without precedent in the field. This approach paves a new road, leading to the resurgence of anticancer autophagy inhibitors as an attractive therapeutic target in cancer.
  • ||||||||||  sirolimus / Generic mfg.
    Journal, IO biomarker:  DR1-CSE/HS pathway upregulates autophagy and inhibits H9C2 cells damage induced by high glucose. (Pubmed Central) -  Jul 18, 2023   
    In addition, AICAR (an agonist of AMPK) and Rapamycin (an inhibitor of mTOR) increased the production of autophagosomes but decreased the p-mTOR/t-mTOR ratio, which was similar to the effects of SKF38393 and 3MA. Our findings suggest that DR1 reduces the HG-induced cardiomyocyte damage via up-regulating the CSE/HS pathway, which increases cell autophagy by inhibiting the activation of mTOR.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Journal:  Identifying a selective inhibitor of autophagy that targets ATG12-ATG3 protein-protein interaction. (Pubmed Central) -  Jul 17, 2023   
    Compound 189 has the potential to be developed into a therapeutic drug and its discovery documents the power of targeting PPIs for acquiring specific and selective compound inhibitors of autophagy.Abbreviations: ANOVA: analysis of variance; ATG: autophagy related; CQ: chloroquine; GFP: green fluorescent protein; GLuc: Gaussia Luciferase; HEK: human embryonic kidney; IL1B: interleukin 1 beta; LPS: lipopolysaccharide; MAP1LC3B/LC3B: microtubule associated protein 1 light chain 3 beta; PCA: protein-fragment complementation assay; PDAC: pancreatic ductal adenocarcinoma; PMA: phorbol 12-myristate 13-acetate; PPI: protein-protein interaction. VCL: vinculin.
  • ||||||||||  Verzenio (abemaciclib) / Eli Lilly
    Journal:  CDK4/6 and autophagy inhibitors synergize to suppress the growth of human head and neck squamous cell carcinomas. (Pubmed Central) -  Jul 17, 2023   
    Our results show that the specific CDK4/6 inhibitor, abemaciclib, inhibited cell growth, and induced apoptosis in HNSCC cell lines...Coinhibition of CDK4/6 and autophagy synergistically decreased cell viability, induced apoptosis, and inhibited tumor growth in both in vitro and in vivo preclinical HNSCC models. These results reveal a potential therapeutic strategy that supports the rationale for further clinical development of a combination of CDK4/6 and autophagy inhibitors in HNSCC.
  • ||||||||||  Targretin oral (bexarotene oral) / ReXceptor
    Preclinical, Journal:  Bexarotene improves motor function after spinal cord injury in mice. (Pubmed Central) -  Jul 15, 2023   
    Intravenous injection of transcription factor E3 shRNA or intraperitoneal injection of compound C, an AMP-activated protein kinase blocker, inhibited the effects of bexarotene. These findings suggest that bexarotene regulates nuclear translocation of transcription factor E3 through the AMP-activated protein kinase-S-phase kinase-associated protein 2-coactivator-associated arginine methyltransferase 1 and AMP-activated protein kinase-mammalian target of rapamycin signal pathways, promotes autophagy, decreases reactive oxygen species level, inhibits pyroptosis, and improves motor function after spinal cord injury.
  • ||||||||||  Journal:  IL-22 promotes occludin expression by activating autophagy and treats ulcerative colitis. (Pubmed Central) -  Jul 13, 2023   
    Importantly, inhibiting autophagy in vitro by 3-Methyladenine (3-MA) attenuated the occludin protective effects of IL-22. In summary, our findings demonstrate that IL-22 ameliorates DSS-induced ulcerative colitis, which may be attributable to activating autophagy and then promoting occludin expression.
  • ||||||||||  MG132 / Jilin University, Dorothy M. Davis Heart and Lung Research Institute
    Preclinical, Journal:  Development of KEAP1-targeting PROTAC and its antioxidant properties: In vitro and in vivo. (Pubmed Central) -  Jul 12, 2023   
    Summarizing, we described the synthesis of a KEAP1-targeting PROTAC (SD2267) and its efficacy and mode of action in vitro and in vivo. The results obtained suggest that SD2267 could be used to treat hepatic diseases related to oxidative stress.
  • ||||||||||  5-fluorouracil / Generic mfg.
    Journal:  KLF4 targets RAB26 and decreases 5-FU resistance through inhibiting autophagy in colon cancer. (Pubmed Central) -  Jul 11, 2023   
    Accumulating studies demonstrated that resistance of colon cancer (CC) to 5-fluorouracil (5-FU) contributes to adverse prognosis...Autophagy activator Rapamycin or sh-RAB26 treatment reversed the impact of KLF4 overexpression on 5-FU resistance...Rescue experiments revealed that KLF4 targeted RAB26 to inhibit CC cell autophagy, resulting in decreasing the resistance to 5-FU. KLF4 strengthened the sensitivity of CC cells to 5-FU by targeting RAB26 to restrain autophagy pathway.
  • ||||||||||  Selzentry (maraviroc) / ViiV Healthcare
    Journal:  Microglial-to-neuronal CCR5 signaling regulates autophagy in neurodegeneration. (Pubmed Central) -  Jul 10, 2023   
    CCR5 upregulation is self-sustaining, as CCL5-CCR5 autophagy inhibition impairs CCR5 degradation itself. Finally, pharmacological or genetic inhibition of CCR5 rescues mTORC1 hyperactivation and autophagy dysfunction, which ameliorates HD and tau pathologies in mouse models.
  • ||||||||||  doxorubicin hydrochloride / Generic mfg.
    Preclinical, Journal:  Antitumor Activity of Berberine by Activating Autophagy and Apoptosis in CAL-62 and BHT-101 Anaplastic Thyroid Carcinoma Cell Lines. (Pubmed Central) -  Jul 7, 2023   
    Doxorubicin (DOX) is the only drug approved for anaplastic thyroid cancer treatment, but its clinical use is restricted due to irreversible tissue toxicity...Furthermore, BER and DOX cooperated to promote apoptosis and autophagy in ATC cells. Taken together, the present findings indicated that BER induces apoptosis and autophagic cell death by activating ROS and regulating the PI3K/AKT/mTOR signaling pathway.
  • ||||||||||  sirolimus / Generic mfg.
    Journal:  Peroxinredoxin 6 reduction accelerates cigarette smoke extract?induced senescence by regulating autophagy in BEAS?2B cells. (Pubmed Central) -  Jul 7, 2023   
    Furthermore, autophagy inhibition by 3-Methyladenine increased P16 and P21 expression levels, while autophagy activation by rapamycin reduced P16 and P21 expression levels in CSE-treated BEAS-2B cells...In conclusion, the present study demonstrated a novel protective role for PRDX6 in COPD. Furthermore, a reduction in PRDX6 could accelerate senescence by inducing autophagy impairment in CSE-treated BEAS-2B cells.
  • ||||||||||  A study on the cell death mode of ? cells under hypoxia and the protective effect of huc-MSC-CM (Indigo H) -  Jul 7, 2023 - Abstract #IPITAIXACTRMS2023IPITA_IXA_CTRMS_67;    
    cells from hypoxia-induced apoptosis and pyroptosis by inducing autophagy, and enhance cell survival. This result shows that pyroptosis can also be used as a target for ?-cell protection, and huc-MSCs-CM can simultaneously target multiple cell death pathways to protect ?-cells and may improve the effect of islet transplantation.
  • ||||||||||  Deficiency of methylmalonyl-CoA mutase correlates with higher autophagy in HEK cells (Pincus (ICC)) -  Jul 6, 2023 - Abstract #SSIEM2023SSIEM_262;    
    An involvement of autophagy is also underlined by elevated LC3 levels in MMUT KO cells, both under basal and starvation conditions, and that higher MMUT protein levels are detected upon treatment with the autophagy inhibitor Bafilomycin A1. Conclusion The reduced expression of MMUT variants indicates a decreased stability and potentially faster degradation, while inhibition of autophagy yields higher MMUT protein levels.
  • ||||||||||  gabapentin / Generic mfg.
    Tau as the missing link between persistent pain and increased risk for dementia- preclinical evidence (In-Person) -  Jul 6, 2023 - Abstract #AAIC2023AAIC_8333;    
    Molecular understanding experiments also included the analgesic drug, gabapentin or virus-driven overexpression of Rab35, a regulator of Tau degradation... Our findings reveal that exposure to chronic pain triggers Tau-related neuronal pathology in hippocampus and may be relevant for understanding how chronic pain precipitates memory loss leading to dementia as recently suggested by clinical studies.
  • ||||||||||  Evaluating dynamic autophagic responses to tau inclusions (In-Person) -  Jul 6, 2023 - Abstract #AAIC2023AAIC_8315;    
    With this tool we can now dynamically assess autophagy in ex vivo BSCs and characterize changes in response to tau and other pathologies. Overall, understanding the mechanisms that enable tau turnover may guide therapies for Alzheimer
  • ||||||||||  Preclinical, Journal:  In vivo measurement of autophagic flux by fluorescence correlation spectroscopy. (Pubmed Central) -  Jul 6, 2023   
    This new method was able to evaluate autophagy inducers, early-stage autophagy inhibitors, and late-stage autophagy inhibitors. Compared with current methods, our method shows high spatiotemporal resolution and very high sensitivity for autophagosomes in low EGFP-LC3B expressing cells and will become an attractive and alternative method for biological and medical studies, some drug screening, and disease treatment.