- |||||||||| griseofulvin / Generic mfg.
Journal: Synthesis of Indofulvin Pseudo-Natural Products Yields a New Autophagy Inhibitor Chemotype. (Pubmed Central) - Feb 12, 2022 Cheminformatic analysis indicates that the indofulvins reside in an area of chemical space sparsely covered by NPs, drugs, and drug-like compounds and they may combine favorable properties of these compound classes. Biological evaluation of the compound collection in different cell-based assays and the unbiased high content cell painting assay reveal that the indofulvins define a new autophagy inhibitor chemotype that targets mitochondrial respiration.
- |||||||||| Journal: Seriniquinones as Therapeutic Leads for Treatment of BRAF and NRAS Mutant Melanomas. (Pubmed Central) - Feb 11, 2022
To explore this rather as a survival or death mechanism, autophagy inhibition sensibilized BRAF mutants to SQ1 and SQ2, whereas the opposite happened to NRAS mutants. These data suggest that the seriniquinones remain active, independently of the melanoma mutation, and suggest the future combination of their application with inhibitors of autophagy to treat BRAF-mutated tumors.
- |||||||||| Review, Journal: Engineering Nanoplatform for Combined Cancer Therapeutics via Complementary Autophagy Inhibition. (Pubmed Central) - Feb 11, 2022
The multistep autophagic pathway provides potentially druggable targets to inhibit pro-survival autophagy under various therapeutic stimuli. In this review, we focus on autophagy inhibition based on functional nanoplatforms, which may be a potential strategy to increase therapeutic sensitivity in combinational cancer therapies, including chemotherapy, radiotherapy, phototherapy, sonodynamic therapy, and immunotherapy.
- |||||||||| Review, Journal: Autophagy in vascular dementia and natural products with autophagy regulating activity. (Pubmed Central) - Feb 10, 2022
Some autophagy regulators have been tested, suggesting that both activation and inhibition of autophagy can improve the cognitive function. This article reviews the role of autophagy in CCH-induced VD to discuss whether autophagy has the potential to become a target for drug development and provides several potential compounds for treating vascular dementia.
- |||||||||| Review, Journal: Autophagy is a major metabolic regulator involved in cancer therapy resistance. (Pubmed Central) - Feb 10, 2022
Moreover, autophagy is induced in numerous tumor types as a resistance mechanism following therapy, highlighting autophagy inhibition as a promising target for anti-cancer therapy. Thus, better understanding the mechanisms involved in tumor growth and resistance regulation through autophagy, which are not fully understood, will provide insights into patient treatment.
- |||||||||| sirolimus / Generic mfg.
Preclinical, Journal: 1,3-dichloro-2-propanol induced hepatic lipid accumulation by inhibiting autophagy via AKT/mTOR/FOXO1 pathway in mice. (Pubmed Central) - Feb 10, 2022 On the contrary, the autophagy inhibitor (chloroquine or 3-methyladenine) further exacerbated hepatic lipid accumulation caused by 1,3-DCP...We detected the changes in autophagy marker protein LC3-II and lipid accumulation using an AKT inhibitor ARQ-092 or a mTOR inhibitor rapamycin in HepG2 cells...Taken together, these data revealed that the effects of 1,3-DCP on lipid accumulation by inhibiting autophagy were dependent on AKT/mTOR/FOXO1 signaling pathway. Our study not only supplied the mechanism of 1,3-DCP toxicity, but also provided experimental basis for effective intervention measures of 1,3-DCP toxicity.
- |||||||||| Journal: Curcumin induces autophagic cell death in human thyroid cancer cells. (Pubmed Central) - Feb 10, 2022
Hyperactivation of the AKT/mTOR axis was observed in the majority of PTC samples we tested, and thyroid cancer cell lines along with cancer tissue specimens sustained a low basal autophagic activity. Taken together, our results provide new evidence that inducing autophagic cell death may serve as a potential anti-cancer strategy to handle thyroid cancer.
- |||||||||| Journal: Strain induced mechanoresponse depends on cell contractility and BAG3-mediated autophagy. (Pubmed Central) - Feb 9, 2022
Furthermore, we demonstrate that strain-induced cell reorientation is clearly delayed upon inhibition of autophagy, suggesting a bidirectional crosstalk between mechanotransduction and autophagic degradation. The strength of the observed delay depends on stable adhesion structures and stress fiber formation in a RhoA-dependent manner.
- |||||||||| sirolimus / Generic mfg.
Journal: miR221 regulates TGF-β1-induced HSC activation through inhibiting autophagy by directly targeting LAMP2. (Pubmed Central) - Feb 9, 2022 The results showed that the expression levels of collagen‑I (COL‑I) and α‑smooth muscle actin (α‑SMA) were increased in miR221‑overexpressing LX2 cells, while the autophagy inducer rapamycin reversed the inhibition of autophagic flux induced by miR221...These results indicated that miR221 may regulate TGF‑β1‑induced HSC activation through inhibiting autolysosome function by directly targeting LAMP2. The molecular mechanism of miR221 in regulating TGF‑β1‑induced HSC activation may provide novel insight into therapies to ameliorate the pathological progression of liver fibrosis.
- |||||||||| doxorubicin hydrochloride / Generic mfg.
Preclinical, Journal: LCN2 deficiency ameliorates doxorubicin-induced cardiomyopathy in mice. (Pubmed Central) - Feb 9, 2022 LCN2 co-localized with LC3B-stained cells in the DOX-treated WT mouse heart, but not in the DOX-treated LCN2KO mouse heart. These findings indicate that the cardiotoxic effect of DOX is due to autophagosome accumulation mediated by LCN2 upregulation and that LCN2 may inhibit autophagic flux, leading to DOX-induced cardiomyopathy.
- |||||||||| Journal: Autophagy, not apoptosis, plays a role in lumen formation of eccrine gland organoids. (Pubmed Central) - Feb 9, 2022
These findings indicate that the cardiotoxic effect of DOX is due to autophagosome accumulation mediated by LCN2 upregulation and that LCN2 may inhibit autophagic flux, leading to DOX-induced cardiomyopathy. Using our model of eccrine gland 3D-reconstruction in Matrigel, we determined that autophagy rather than apoptosis plays a role in the lumen formation of EGOs.
- |||||||||| ByFavo (remimazolam) / PAION, Cosmo Pharma, Mundipharma, Pharmascience, Acacia Pharma
Journal: Remimazolam alleviates neuropathic pain via regulating bradykinin receptor B1 and autophagy. (Pubmed Central) - Feb 8, 2022 In conclusion, Dex upregulated the phosphorylation of Beclin1 at S295 site by activating the PI3K/Akt pathway and reduced the interactions of Atg14L-Beclin1-Vps34 complex, thus inhibiting autophagy and protecting against myocardial I/R injury. Remimazolam downregulated BDKRB1, inhibited BDKRB1/RAS/MEK signalling pathway and regulated the autophagic lysosome induction, exhibiting a better outcome in the NP.
- |||||||||| Journal: MicroRNA-17-5p Promotes Cardiac Hypertrophy by Targeting Mfn2 to Inhibit Autophagy. (Pubmed Central) - Feb 8, 2022
Mfn2 overexpression attenuated miR-17-5p-induced cell hypertrophy, and in rat myocardial tissue, miR-17-5p induced autophagy inhibition. In summary, the results of the present study demonstrated that miR-17-5p inhibits Mfn2 expression, activates the PI3K/AKT/mTOR pathway and suppresses autophagy to promote cardiac hypertrophy.
- |||||||||| Review, Journal: Emerging quinoline and quinolone based antibiotics in the light of epidemics. (Pubmed Central) - Feb 8, 2022
Therefore, quinoline and quinolone derivatives attain significance in area of research and treatment of various life-threatening epidemics such as SARS, Zika virus, Ebola virus, Dengue and COVID-19 (currently). In this chapter, the research and advancements of quinoline and quinolone-based antibiotics in epidemic management is briefly discussed.
- |||||||||| Journal: Thiopurines correct the effects of autophagy impairment on intestinal healing - a potential role for ARHGAP18/RhoA. (Pubmed Central) - Feb 5, 2022
RhoA dysregulation appeared mediated through accumulation of the upstream regulator ARHGAP18, which was observed in cell lines, human foetal organoids and primary colonic tissue. Our results indicate that the ATG16L1 T300A Crohn's disease-associated SNP causes a decrease in migration capacity in epithelial cells, mediated by an increase in SQSTM1 and ARHGAP18 protein and subsequent reduced RhoA activation.
- |||||||||| GNS561 / Genoscience Pharma
Journal: GNS561 Exhibits Potent Antiviral Activity against SARS-CoV-2 through Autophagy Inhibition. (Pubmed Central) - Feb 5, 2022 To confirm our findings, we used the K18-hACE2 mouse model and highlighted that GNS561 treatment led to a decline in SARS-CoV-2 virions in the lungs associated with a disruption of the autophagy pathway. Overall, our study highlights GNS561 as a powerful drug in the treatment of SARS-CoV-2 infection and supports the hypothesis that autophagy blockers could be an alternative strategy for COVID-19.
- |||||||||| Journal: Vitamin D promotes autophagy in AML cells by inhibiting miR-17-5p-induced Beclin-1 overexpression. (Pubmed Central) - Feb 4, 2022
Vitamin D was found to diminish cell proliferation and enhance autophagy. Finally, through rescue assays, miR-17-5p facilitated the ability of cell proliferation, inhibited autophagy and apoptosis by modulating Beclin-1 in HL-60 cells following the treatment of 4 μM vitamin D. Vitamin D promoted autophagy in AML cells by modulating miR-17-5p and Beclin-1.
- |||||||||| doxycycline / Generic mfg.
Journal, PD(L)-1 Biomarker, IO biomarker: Engineering Chameleon Prodrug Nanovesicles to Increase Antigen Presentation and Inhibit PD-L1 Expression for Circumventing Immune Resistance of Cancer. (Pubmed Central) - Feb 4, 2022 It is first sorted out that doxycycline (Doxy) efficiently inhibits autophagy of the tumor cells, and increases the surface level of major histocompatibility complex class I (MHC-I)...After a proof of concept for overcoming intrinsic and inducible immune evasion, the prodrug nanovesicles are applied to validate the efficacy of cancer immunotherapy in two tumor-bearing mouse models. This research thus provides a novel targeting strategy for reducing tumor immune resistance and potentiating tumor immunotherapy.
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