- |||||||||| quercetin (LY294002) / Eli Lilly
Preclinical, Journal: Peperomin E Induces Apoptosis and Cytoprotective Autophagy in Human Prostate Cancer DU145 Cells In Vitro and In Vivo. (Pubmed Central) - Jul 17, 2021 In summary, our finding showed that peperomin E had an effect on DU145 cells in vitro and in a nude mouse DU145 cell xenograft model in vivo, demonstrated that peperomin E could significantly induce apoptosis and the autophagic response in DU145 cells and that autophagy played a cytoprotective role in peperomin E-treated DU145 cells. These results suggest that the combination of peperomin E treatment and autophagic inhibition has potential for the treatment of prostate cancer.
- |||||||||| sirolimus / Generic mfg.
Journal: TCDD induced lipid accumulation by impairment of autophagic flux in THP-1 macrophages. (Pubmed Central) - Jul 17, 2021 On the contrary, pretreatment with autophagy inhibitor (Chloroquine, CQ) promoted TCDD-induced lipid accumulation...These results indicated that TCDD promoted lipid accumulation in THP-1 macrophages by inhibiting autophagic flux. Our findings revealed new insights into the toxicity mechanisms of TCDD.
- |||||||||| sirolimus / Generic mfg.
Journal: Autophagy contributes to angiotensin II induced dysfunction of HUVECs. (Pubmed Central) - Jul 17, 2021 Silence Atg5 completely reverses Ang II-activated autophagy levels. Our results demonstrate that Ang II stimulation increases autophagy levels via AT1 receptor, NADPH oxidase, mitochondrial K channel, eNOS, Atg5 signal pathway in HUVECs, and activation of autophagy contributes to Ang II induced dysfunction of HUVECs.
- |||||||||| Journal: 6-Shogaol from ginger shows anti-tumor effect in cervical carcinoma via PI3K/Akt/mTOR pathway. (Pubmed Central) - Jul 16, 2021
On the whole, the results of the present study demonstrated that RSV initiates the apoptosis and autophagic death of A549 cells via the activation of the p53 signaling pathway, further highlighting the potential of RSV for the treatment of NSCLC. These findings suggested that 6-shogaol could be developed as a functional food ingredient, which is potentially used as therapeutic agents for patients with cervical cancer.
- |||||||||| chloroquine phosphate / Generic mfg.
Journal: Propionate alleviates palmitic acid-induced endoplasmic reticulum stress by enhancing autophagy in calf hepatic cells. (Pubmed Central) - Jul 15, 2021 However, inhibition of autophagic activity by chloroquine or bafilomycin A1 impede the beneficial effects of propionate on ER stress and cell viability. These results demonstrated that propionate alleviates ER stress and elevates cell viability in PA-treated calf hepatic cells by enhancing autophagy, which implies that autophagy may be a promising target in improving liver injury of dairy cows during transition period.
- |||||||||| PLX4720 / Daiichi Sankyo
Journal: BRAF Inhibition Induces Cytoprotective Autophagy through AMPK in Thyroid Cancer Cells. (Pubmed Central) - Jul 15, 2021 We reveal that the inhibition of BRAF activity with its specific inhibitor PLX4720 or the depletion of its expression by siRNA induces autophagy in thyroid tumour cells...Collectively, we uncover a new role of AMPK in mediating the induction of cytoprotective autophagy by BRAF inhibition. In addition, these data establish a rationale for designing an integrated therapy targeting BRAF and the LKB1-AMPK-ULK1-autophagy axis for the treatment of BRAF-positive thyroid tumours.
- |||||||||| Journal: Cytotoxic Monoterpenoid Indole Alkaloids from Tabernaemontana corymbosa as Potent Autophagy Inhibitors by the Attenuation of Lysosomal Acidification. (Pubmed Central) - Jul 14, 2021
Alkaloids 1-4 are new vobasinyl-ibogan alkaloids, and 1 is characterized by an unusual 1,3-oxazinane moiety. Alkaloids 4 and 16 exhibited moderate cytotoxic potency against various human cancer cell lines, while 4, 10, 11, 13, 14, and 16 showed attenuation of lysosomal acidification activity (EC: 12.9-29.8 μM), thereby inhibiting autophagic flux.
- |||||||||| Journal: The role of activating transcription factor 6 in hydroxycamptothecin-induced fibroblast autophagy and apoptosis. (Pubmed Central) - Jul 14, 2021
Our experiments preliminarily revealed that YAP/TAZ and autophagy play important roles in the migration and invasion of RA-FLS, which might provide novel targets for the treatment of RA. Our results demonstrate that HCPT acts as a facilitator of fibroblast apoptosis and inhibitor of fibroblast proliferation for curbing the postoperative scar adhesion, in which the ATF6-mediated ERS pathway and autophagy are involved.
- |||||||||| Preclinical, Journal: Melatonin induces the rejuvenation of long-term ex vivo expanded periodontal ligament stem cells by modulating the autophagic process. (Pubmed Central) - Jul 14, 2021
The present study suggests that MLT may attenuate long-term expansion-caused cellular senescence by restoring autophagy, most likely via the PI3K/AKT/mTOR signaling pathway in an MT-dependent manner. This is the first report identifying the involvement of MT-dependent PI3K/AKT/mTOR signaling in MLT-induced autophagy alteration, indicating a potential of autophagy-restoring agents such as MLT to be used in the development of optimized clinical-scale cell production protocols.
- |||||||||| Journal: IL-6 regulates autophagy and chemotherapy resistance by promoting BECN1 phosphorylation. (Pubmed Central) - Jul 13, 2021
Furthermore, we investigate BECN1 Y333 phosphorylation as a predictive marker for poor CRC prognosis and chemotherapy resistance. Combination treatment with autophagy inhibitors or pharmacological agents targeting the IL-6/JAK2/BECN1 signaling pathway may represent a potential strategy for CRC cancer therapy.
- |||||||||| Journal: Amino Acids in Autophagy: Regulation and Function. (Pubmed Central) - Jul 13, 2021
In particular, insulin activates mTORC1 via the PI3K class I-AKT pathway; while amino acids activate mTORC1 either through the PI3K class III (hVps34) pathway or through a variety of amino acid sensors located in the cytosol or lysosomal membrane. These amino acid sensors control the translocation of mTORC1 from the cytosol to the lysosomal surface where mTORC1 is activated by Rheb GTPase, therefore regulating autophagy and the lysosomal protein degradation.
- |||||||||| Journal: Role of L-Arginine in Nitric Oxide Synthesis and Health in Humans. (Pubmed Central) - Jul 13, 2021
NO is a vasodilator, a neurotransmitter, a regulator of nutrient metabolism, and a killer of bacteria, fungi, parasites, and viruses [including coronaviruses, such as SARS-CoV and SARS-CoV-2 (the virus causing COVID-19). Thus, Arg supplementation can enhance immunity, anti-infectious, and anti-oxidative responses, fertility, wound healing, ammonia detoxification, nutrient digestion and absorption, lean tissue mass, and brown adipose tissue development; ameliorate metabolic syndromes (including dyslipidemia, obesity, diabetes, and hypertension); and treat individuals with erectile dysfunction, sickle cell disease, muscular dystrophy, and pre-eclampsia.
- |||||||||| Ibrance (palbociclib) / Pfizer
Trial completion date, Trial primary completion date, Surgery: NCI-2018-01050: Hydroxychloroquine, Palbociclib, and Letrozole Before Surgery in Treating Patients With Estrogen Receptor Positive, HER2 Negative Breast Cancer (clinicaltrials.gov) - Jul 8, 2021 P1/2, N=54, Recruiting, The combination of apatinib and CQ sensitized ESCC cells to paclitaxel to induce apoptosis through the IRE-1α-AKT-mTOR signaling pathway, thus providing the basis for its use in innovative anticancer therapeutic strategies. Trial completion date: Dec 2020 --> Dec 2024 | Trial primary completion date: Dec 2020 --> Dec 2023
- |||||||||| Journal: Stapled peptide inhibitors of autophagy adapter LC3B. (Pubmed Central) - Jul 8, 2021
Based on these data, we used artificial amino acids and diversity-oriented stapling to improve affinity and resistance to biological degradation while maintaining or improving LC3B affinity and selectivity. These peptides represent the highest-affinity LC3B-selective ligands reported to date, and they will be useful tools for further elucidation of LC3B's role in autophagy and in cancer.
- |||||||||| chloroquine phosphate / Generic mfg.
Journal: (Pro)renin receptor/ATP6AP2 is required for autophagy and regulates proliferation in lung adenocarcinoma cells. (Pubmed Central) - Jul 8, 2021 Autophagy inhibitors, bafilomycin A1 and chloroquine, were used as positive controls...Western blot and immunocytochemistry showed that (P)RR-specific siRNA, as well as the autophagy inhibitors, induced p62 and LC3 accumulation in cytoplasmic granules. These results suggest that (P)RR is involved in cell proliferation and progression of lung adenocarcinoma via regulating autophagy.
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