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  • ||||||||||  Preclinical, Journal:  Autophagy core protein BECN1 is vital for spermatogenesis and male fertility in mice. (Pubmed Central) -  Nov 17, 2023   
    Furthermore, inhibition of autophagy was observed in the testes of germ cell-specific Becn1 knockout mice, which may contribute to impaired spermiogenesis and reduced fertility. Collectively, our results reveal that Becn1 is essential for fertility and spermiogenesis in mice.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Journal:  Hollow CuSe-based nanocatalysts for combined photothermal and chemodynamic therapy in the second near-infrared window. (Pubmed Central) -  Nov 17, 2023   
    In particular, the hollow octahedral CuSe nanoparticles exhibited higher photothermal and chemodynamic performance than that of spherical or cubic CuSe nanoparticles in the second near-infrared (NIR-II) window. In addition, the octahedral CuSe nanoparticles were further loaded with the autophagy inhibitor chloroquine (CQ) and connected with the targeting neuropeptide Y ligand, and shown to work as a novel therapeutic platform (CuSe@CQ@NPY), holding an immense potential to achieve synergetic enhancement of CDT/PTT with a positive therapeutic outcome for breast cancer.
  • ||||||||||  hydroxychloroquine / Generic mfg.
    Preclinical, Journal:  Sensitivity of osteosarcoma cell lines to autophagy inhibition as determined by pharmacologic and genetic manipulation. (Pubmed Central) -  Nov 17, 2023   
    Pharmacologic inhibition of autophagy can be achieved using lysosomotropic agents such as hydroxychloroquine (HCQ) that interfere with fusion of the autophagosome to the lysosome thus preventing completion of the recycling process...A relationship was observed between antiproliferative responses to HCQ and Lys05 and VPS34 CRISPR score with D values correlating with VPS34 response (r?=?0.968 and 0.887) in a species independent manner. The results show that a subset of cOSA and hOSA cell lines are autophagy-dependent and sensitive to HCQ at pharmacologically-relevant exposures.
  • ||||||||||  Journal:  APOL1-G2 accelerates nephrocyte cell death by inhibiting the autophagy pathway. (Pubmed Central) -  Nov 16, 2023   
    We found that G2 and G1G2-expressing nephrocytes developed more severe changes in autophagic pathways, acidification of organelles, and the structure of the slit diaphragms, compared to G1 nephrocytes, leading to their premature death. We conclude that both RA affect similar key cell trafficking pathways, leading to reduced autophagy, and suggesting new therapeutic targets to prevent APOL1-kidney diseases.
  • ||||||||||  LY294002 / Eli Lilly, Erivedge (vismodegib) / Roche
    Journal:  Inhibition of Hedgehog signaling ameliorates foam cell formation by promoting autophagy in early atherosclerosis. (Pubmed Central) -  Nov 14, 2023   
    Therefore, our result demonstrated that inhibition of the Hh signaling pathway increases cholesterol efflux and ameliorates macrophage-derived foam cell formation by promoting autophagy in vitro. Our data thus suggested a novel therapeutic target of atherosclerosis and indicated the potential of vismodegib to treat atherosclerosis.
  • ||||||||||  Review, Journal:  Pharmacotherapy developments in Autophagy inhibitors for bladder cancer. (Pubmed Central) -  Nov 14, 2023   
    This paper is a review of the literature, which selected randomized trials, cohort studies, case-control studies documenting the relationship between autophagy inhibitors and bladder cancer treatment. Autophagy is a promising pathway for cancer cell targeting that opens the horizons for a potential new therapeutic area in particular the multidisciplinary management of bladder cancer.
  • ||||||||||  Review, Journal:  The mechanisms of action of mitochondrial targeting agents in cancer: inhibiting oxidative phosphorylation and inducing apoptosis. (Pubmed Central) -  Nov 13, 2023   
    Mitochondrial targeting agents typically rely on small molecule medications (such as synthetic small molecules agents, active ingredients of plants, mitochondrial inhibitors or autophagy inhibitors, and others), modified mitochondrial delivery system agents (such as lipophilic cation modification or combining other molecules to form targeted mitochondrial agents), and a few mitochondrial complex inhibitors. This article will review these compounds in three main areas: oxidative phosphorylation (OXPHOS), changes in ROS levels, and endogenous oxidative and apoptotic processes.
  • ||||||||||  Preclinical, Journal, IO biomarker:  MEX3C induces cognitive impairment in mice through autophagy inhibition. (Pubmed Central) -  Nov 13, 2023   
    The KO of the MEX3C gene reduces the plasticity of synapses in various regions of the hippocampus, thereby affecting the function of the hippocampus and eventually causing the decline of cognitive function. On the other hand, compared with WT mice, MEX3C-KO mice showed increased anxiety-like behaviors in minefield and elevated plus maze tests.
  • ||||||||||  Journal:  Orexin-A/OX1R is involved in regulation of autophagy to promote cortisol secretion in adrenocortical cell. (Pubmed Central) -  Nov 13, 2023   
    The findings suggest the mechanistic basis for disorders of cortisol secretion, providing the potential therapeutic targets for hypercortisolism treatment. FUND: This work was supported by National Natural Science Foundation of China (32170603, 31871286), the Doctoral Start-up Foundation of Liaoning Province (20180540008, 2019-BS-298), the Natural Science Foundation of Liaoning Province (2019-ZD-0779), and Shenyang Science and Technology Plan Fund Projects (21-173-9-28).
  • ||||||||||  hydroxychloroquine / Generic mfg.
    Review, Journal:  Hydroxychloroquine in nephrology: current status and future directions. (Pubmed Central) -  Nov 13, 2023   
    Created with Biorender.com. HCQ, hydroxychloroquine; GBM, glomerular basement membrane; mDC, myeloid dendritic cell; MHC, major histocompatibility complex; TLR, toll-like receptor.
  • ||||||||||  Journal:  FAT1 inhibits AML autophagy and proliferation via downregulating ATG4B expression. (Pubmed Central) -  Nov 12, 2023   
    HCQ, hydroxychloroquine; GBM, glomerular basement membrane; mDC, myeloid dendritic cell; MHC, major histocompatibility complex; TLR, toll-like receptor. Our study suggested that the "FAT1-TGF?-smad2/3-ATG4B-autophagy" pathway may be a novel target for developing new targeted drugs to AML treatment.
  • ||||||||||  Targeting amino acid metabolic vulnerabilities in IDH-mutant and IDH-wildtype gliomas (Exhibit Hall A/B) -  Nov 11, 2023 - Abstract #SNO2023SNO_1183;    
    In addition, GLUD1 inhibitor suppressed the growth of xenografted glioma cells with overexpressed mutant IDH1. In conclusion, L-asparaginase and Glud1 inhibitor will be new therapeutic option for IDH-wildtype glioma and IDH-mutant glioma, respectively.
  • ||||||||||  Journal:  PRPF19 promotes the proliferation, migration, and inhibits autophagy in prostate cancer by suppressing SLC40A1. (Pubmed Central) -  Nov 10, 2023   
    In the double knockdown of PRPF19 and SLC40A1, PRPF19 repressed the mRNA and reduced protein level of SLC40A1, and SLC40A1 antagonized effects of PRPF19 on proliferation, migration and autophagy of PCa cells. PRPF19 promoted proliferation and migration, and inhibited autophagy in PCa by attenuating SLC40A1 expression, indicating PRPF19 was a potential therapeutic target for PCa treatment.
  • ||||||||||  cisplatin / Generic mfg., paclitaxel / Generic mfg., fingolimod / Generic mfg.
    Journal:  FTY720 increases paclitaxel efficacy in cisplatin-resistant oral squamous cell carcinoma. (Pubmed Central) -  Nov 10, 2023   
    PRPF19 promoted proliferation and migration, and inhibited autophagy in PCa by attenuating SLC40A1 expression, indicating PRPF19 was a potential therapeutic target for PCa treatment. FTY720 sensitizes cisplatin-resistant oral squamous cell carcinoma cells for paclitaxel.
  • ||||||||||  temuterkib (LY3214996) / Eli Lilly
    Enrollment closed, Trial primary completion date, Combination therapy, Metastases:  LY3214996 +/- HCQ in Pancreatic Cancer (clinicaltrials.gov) -  Nov 8, 2023   
    P2,  N=52, Active, not recruiting, 
    Our data indicate that JSI-124 is a promising therapeutic agent for MPM treatment. Recruiting --> Active, not recruiting | Trial primary completion date: Nov 2023 --> Aug 2023
  • ||||||||||  Journal:  CSNK2 suppresses autophagy by activating FLN-NHL-containing TRIM proteins. (Pubmed Central) -  Nov 8, 2023   
    Thus, our results identify the CSNK2-TRIM2, -TRIM3, -TRIM71 axis as a key regulatory pathway that limits autophagy. Targeting this axis may allow for therapeutic induction of autophagy against viral infections and in diseases associated with dysregulated autophagy.
  • ||||||||||  chloroquine phosphate / Generic mfg.
    Preclinical, Journal:  Chloroquine impairs maximal transdiaphragmatic pressure generation in old mice. (Pubmed Central) -  Nov 6, 2023   
    There were no sex or age effects on Pdi in older mice. The observed decrease in Pdi suggests aging-related susceptibility to impairments in autophagy, consistent with effects of chloroquine on this important homeostatic process.
  • ||||||||||  Estybon (rigosertib) / Onconova, SymBio Pharma, Knight Therap
    Journal, PD(L)-1 Biomarker, IO biomarker:  Rigosertib promotes anti-tumor immunity via autophagic degradation of PD-L1 in colorectal cancer cells. (Pubmed Central) -  Nov 6, 2023   
    Furthermore, apart from the immunomodulatory effect, we also confirmed the direct cytotoxicity of RGS in inducing mitochondria-related apoptosis. Altogether, considering its PD-L1 inhibitory and cytotoxic effects, RGS could be a promising drug for CRC therapy.
  • ||||||||||  Journal:  Interplay Between Zika Virus-Induced Autophagy and Neural Stem Cell Fate Determination. (Pubmed Central) -  Nov 4, 2023   
    Collectively, our findings highlight the novel role of NS4A and NS4B in mediating NSC fate alteration through autophagy-mediated notch degradation. The study also helps to advance our understanding of ZIKV-induced neuropathogenesis and suggests autophagy as a potential target for anti-ZIKV therapeutic intervention.
  • ||||||||||  narazaciclib (ON 123300) / Onconova
    Narazaciclib's differential targets and kinase inhibitory activity contribute to the enhanced inhibition of tumor growth in preclinical models (Hall 2-3) -  Nov 4, 2023 - Abstract #SABCS2023SABCS_1949;    
    P1, P1/2
    Narazaciclib is in Ph I trials; NCT04739293 and CXHL1900340; studying different administration regimens and in endometrial cancer in combination with letrozole (NCT05705505)...Kd values of CDK4/cyclinD1 binding show similar trends; abemaciclib (0.08 nM), narazaciclib (0.18 nM), palbociclib (0.75 nM) and ribociclib (1.3 nM)...Our findings identify important differences generated from assay models studying kinase inhibition, binding and pathway engagement. Understanding the role of the differential targets engaged by narazaciclib, the potential enhanced antitumor immunity and the sensitization by autophagy inhibitors to cell death, will guide future clinical studies.
  • ||||||||||  Preclinical, Journal:  Antiviral activity of prion protein against Japanese encephalitis virus infectionin vitroandin vivo. (Pubmed Central) -  Nov 4, 2023   
    Further analysis indicated that after virus entry, PrPc inhibited autophagic flux that prevented JEV replication inside the host cell. Our results from in vivo and in vitro investigations demonstrate that prion protein effectively inhibited JEV propagation by regulating autophagy flux which is used by JEV to release its genetic material and replication after entering the host cell, suggesting that prion protein may be a promising therapeutic target for flavivirus infection.
  • ||||||||||  Tafinlar (dabrafenib) / Novartis, BeiGene, Braftovi (encorafenib) / Ono Pharma, Pierre Fabre, Pfizer, Zelboraf (vemurafenib) / Roche
    Review, Journal:  The Cytoprotective Role of Autophagy in Response to BRAF-Targeted Therapies. (Pubmed Central) -  Nov 3, 2023   
    Clinical trials have also demonstrated a potential benefit from the inclusion of autophagy inhibition as an adjuvant therapy. This review of the scientific literature relating to the role of autophagy that is induced in response to BRAF-inhibitors supports the premise that autophagy targeting or modulation could be an effective adjuvant therapy.
  • ||||||||||  perillyl alcohol (NEO100) / NeOnc Technologies
    Journal:  Inhibition of autophagy and induction of glioblastoma cell death by NEO214, a perillyl alcohol-rolipram conjugate. (Pubmed Central) -  Nov 3, 2023   
    When combined with chloroquine and TMZ, the anticancer impact of NEO214 is further potentiated and unfolds against TMZ-resistant cells as well. Taken together, our findings characterize NEO214 as a novel autophagy inhibitor that could become useful for overcoming chemoresistance in glioblastoma.Abbreviations: ATG: autophagy related; BAFA1: bafilomycin A; BBB: blood brain barrier; CQ: chloroquine; GBM: glioblastoma; LAMP1: lysosomal associated membrane protein 1; MAP1LC3/LC3: microtubule associated protein 1 light chain 3; MGMT: O-6-methylguanine-DNA methyltransferase; MTOR: mechanistic target of rapamycin kinase; MTORC: MTOR complex; POH: perillyl alcohol; SQSTM1/p62: sequestosome 1; TFEB: transcription factor EB; TMZ: temozolomide.