 |
Companies | Products |
|
|
Products | |
Diseases | |
Trials |  |
News |  |
| «12...5152535455565758596061...135136» |
- | 5-fluorouracil / Generic mfg., cisplatin / Generic mfg.
Journal: Discovery of fused benzimidazole-imidazole autophagic flux inhibitors for treatment of triple-negative breast cancer. (Pubmed Central) - Aug 18, 2022
Through a medium throughput screening and iterative medicinal chemistry optimization, we identified compound 7h as an autophagic flux inhibitor, which showed potent activities against human TNBC (MDA-MB-231 and MDA-MB-468) cell lines with IC values of 8.3 μM, and 6.0 μM, respectively, which are comparable to the potency of 5-FU and Cisplatin, the first line therapies for TNBC...Our findings indicate that compound 7h is an autophagic flux inhibitor and induced the degradation of HR-related proteins. Compound 7h could be potentially developed as an anti-cancer therapeutics for TNBC.
- | sirolimus / Generic mfg.
Journal, IO biomarker: HMGB1/TLR4 induces autophagy and promotes neuroinflammation after intracerebral hemorrhage. (Pubmed Central) - Aug 18, 2022
Compound 7h could be potentially developed as an anti-cancer therapeutics for TNBC. During the acute phase of ICH, the HMGB1/TLR4/MyD88 axis acts via autophagy to promote inflammation.
- | chloroquine phosphate / Generic mfg.
Journal: Low-dose cadmium exposure promotes osteoclastogenesis by enhancing autophagy via inhibiting the mTOR/p70S6K1 signaling pathway. (Pubmed Central) - Aug 18, 2022
Deficiencies in autophagosomes and osteoclasts were also observed. Taken together, the results indicate that a low concentration of CdCl promotes osteoclastogenesis by enhancing autophagy via inhibiting the mTOR/p70S6K1 signaling pathway.
- | Journal: Trehalose improves palmitic acid-induced apoptosis of osteoblasts by regulating SIRT3-medicated autophagy via the AMPK/mTOR/ULK1 pathway. (Pubmed Central) - Aug 18, 2022
The results showed that Trehalose could inhibit the bone mass loss with HFD. Our study revealed the effect and mechanism of Trehalose in the treatment of osteoporosis.
- | Journal: Exosomal miR-7002-5p derived from highglucose-induced macrophages suppresses autophagy in tubular epithelial cells by targeting Atg9b. (Pubmed Central) - Aug 18, 2022
These results demonstrated that HG-exo carries excessive miR-7002-5p and inhibits autophagy through targeting Atg9b; this process then induces renal tubular dysfunction and inflammation. In conclusion, our study clarifies the important role of macrophage-derived exosomes in DN and is expected to provide new insight on DN prevention and treatment.
- | Journal: Phospholipid peroxidation inhibits autophagy via stimulating the delipidation of oxidized LC3-PE. (Pubmed Central) - Aug 17, 2022
Our results agree with the recognized role of endoplasmic reticulum as the primary source for autophagosomal membranes. In summary, our studies demonstrated that phospholipid peroxidation inhibited autophagy via stimulating the ATG4B-mediated delipidation of peroxidized LC3-PE.
- | acetylcysteine solution / Generic mfg.
Journal: Daurisoline Inhibits ESCC by Inducing G1 Cell Cycle Arrest and Activating ER Stress to Trigger Noxa-Dependent Intrinsic and CHOP-DR5-Dependent Extrinsic Apoptosis via p-eIF2α-ATF4 Axis. (Pubmed Central) - Aug 17, 2022
Moreover, DAS treatment significantly inhibited tumor growth and reduced tumor weight in the tumor xenograft mouse model by up-regulating key proteins related to cell cycle arrest and apoptotic pathway. Taken together, these findings identified DAS as a novel candidate for the treatment of ESCC.
- | Preclinical, Journal: Corosolic Acid Protects Rat Chondrocytes Against IL-1β-Induced ECM Degradation by Activating Autophagy via PI3K/AKT/mTOR Pathway and Ameliorates Rat Osteoarthritis. (Pubmed Central) - Aug 17, 2022
Correspondingly, the protective effect of CRA was also confirmed in a rat OA model. Herein, we demonstrate that CRA can enhance autophagy by inhibiting PI3K/AKT/mTOR signaling pathway, prevent IL-1β-induced cartilage ECM degradation, and may be a potentially applicable candidate for the treatment of OA.
- | Journal: Hepatic RACK1 deletion disturbs lipid and glucose homeostasis independently of insulin resistance. (Pubmed Central) - Aug 17, 2022
In summary, this study uncovers that hepatic RACK1 might be required in maintaining bile acid homeostasis and glucose uptake in hepatocytes. This study also provides an additional case of hepatic steatosis disassociation with insulin resistance.
- || Lysodren (mitotane) / HRA Pharma
Review, Journal: Modulation of Autophagy in Adrenal Tumors. (Pubmed Central) - Aug 17, 2022
Mitotane, the most commonly used drug for the treatment of adrenocortical carcinoma, was recently shown to also modulate autophagy...In this review, we describe what is known about the role of autophagy modulation in treatment of adrenal tumors. We will also highlight the aspects that need further evaluation to understand the paradoxical role of autophagy in adrenal tumors.
- | ketoconazole / Generic mfg., rifampicin / Generic mfg.
Journal: Role of nuclear pregnane X receptor in Cu-induced lipid metabolism and xenobiotic responses in largemouth bass (Micropterus salmoides). (Pubmed Central) - Aug 17, 2022
Taken together, PXR played a cytoprotective role in Cu-induced hepatotoxicity through regulations on autophagy and apoptosis. Overall, our data has demonstrated for the first time on the dual roles of PXR as a co-regulator in mediating xenobiotic responses and lipid metabolism in fish, which implying the potential of PXR as a therapy target for xenobiotics-induced lipid dysregulation and hepatotoxicity.
- Expression of autophagy markers in ovarian cancer () - Aug 16, 2022 - Abstract #ECP2022ECP_290;
While p62 and LC3 expression was associated with higher tumour stages and tumour grades, the opposite was found for Beclin1. Prominent p62 and LC3 expression in combination with weak Beclin1 expression in HGSOC indicate the potential for application of autophagy inhibitors in patients with this tumour subtype.
- || Review, Journal: Tumor-Treating Fields in Glioblastomas: Past, Present, and Future. (Pubmed Central) - Aug 14, 2022
However, the overall acceptance of TTFields in real-world clinical practice is still low. Given that increasing studies on this promising topic have been published recently, we conducted this updated review on the past, present, and future of TTFields in GBMs.
- | sirolimus / Generic mfg.
Preclinical, Journal: Letter on Rapamycin and 3-Methyladenine Influence the Apoptosis, Senescence, and Adipogenesis of Human Adipose-Derived Stem Cells by Promoting and Inhibiting Autophagy: An In Vitro and In Vivo Study. (Pubmed Central) - Aug 14, 2022
Given that increasing studies on this promising topic have been published recently, we conducted this updated review on the past, present, and future of TTFields in GBMs. No abstract available
- | Journal: Glutamine metabolism modulates chondrocyte inflammatory response. (Pubmed Central) - Aug 14, 2022
Finally, we display that glutamine deprivation promotes autophagy and that ammonia is an inhibitor of autophagy. Overall, we identify a relationship between glutamine metabolism and inflammatory signaling and display the need for increased study of chondrocyte metabolic systems.
- | Journal: Endoplasmic reticulum stress triggered autophagy and regulated the phenotype transformation of rheumatoid arthritis synovial fibroblasts via the IRE1/JNK pathway. (Pubmed Central) - Aug 14, 2022
Moreover, the proliferation and invasion of RASFs were inhibited after transfection with sh-RNA-ERN1 to downregulate IRE1 expression. ER stress triggered autophagy via the IRE1/JNK pathway to regulate the phenotype transformation of RASFs, indicating an important role of the ER stress-autophagy pathway in the pathological process of synovitis in RA.
- | Journal: Mycoplasma bovis inhibits autophagy in bovine mammary epithelial cells via a PTEN/PI3K-Akt-mTOR-dependent pathway. (Pubmed Central) - Aug 14, 2022
In the present study, the number of intracellular M. bovis was inversely related to the change in the level of autophagy markers (e.g., LC3-II, SQSTM1/P62) within host cells induced by the low knockdown of Akt or PTEN. We concluded that M. bovis-infected bMECs alleviated cellular autophagy through a PI3K-Akt-mTOR pathway, and that PTEN acted as a protective gene regulating autophagy, a key step in controlling infection.
- | sirolimus / Generic mfg.
Journal: Experimental Study on Danggui Shaoyao San Improving Renal Fibrosis by Promoting Autophagy. (Pubmed Central) - Aug 13, 2022
With rapamycin (RAPA) used as the positive control, we detected the expression of fibronectin (FN), caspase-3, and autophagy-related proteins in the NRK-52E cells treated with DSS by Western blot and immunofluorescence assay...It has also been found that DSS can increase the expression of LC3 II/I and Beclin 1 proteins and can reduce the level of mTOR in cells treated with 3-MA, suggesting that DSS can promote autophagy. In conclusion, DSS has been proved to reduce the apoptosis and fibrosis of NRK-52E cells induced by TGF-β1, which may be achieved by promoting autophagy.
- | sirolimus / Generic mfg.
Journal: Brucea javanica Oil Emulsion Promotes Autophagy in Ovarian Cancer Cells Through the miR-8485/LAMTOR3/mTOR/ATG13 Signaling Axis. (Pubmed Central) - Aug 13, 2022
The purpose of this study was to investigate the effect of BJOE on the regulation of mammalian rapamycin target protein (mTOR) autophagy signal pathway and related autophagy factors on ovarian cancer cells through miR-8485...The results of qRT-PCR and Western blot showed that BJOE and overexpressed miR-8485 downregulated the expression of LAMTOR3 and mTOR and up-regulated the expression of ATG13 and LC3-Ⅱ. 1) MiR-8485 may be the key factor of BJOE in promoting autophagy and apoptosis and inhibiting cell proliferation of ovarian cancer cells; 2) BJOE may play an antitumor role by regulating LAMTOR3/mTOR/ATG13 signaling axis through miR-8485 to promote autophagy in ovarian cancer cells.
- JQ-1 / Roche
Unc-51 Like Kinase 3 protein (ULK3)-mediated autophagy is responsible for multiple myeloma resistance to chemotherapy () - Aug 13, 2022 - Abstract #IMW2022IMW_354;
ULK3 represents a novel target for treatment of MM refractory disease. Our dual inhibitors can increase overall survival in vivo and ex vivo, therefore we expect to quickly translate our novel molecules to the clinic.
- ER-phagic control of lipid metabolism supports multiple myeloma cell survival () - Aug 13, 2022 - Abstract #IMW2022IMW_348;
Despite the unrivaled secretory proteosynthetic activity of PCs, ER-phagy does not mediate quality control in MM, but maintains LDs, which in turn fuel mitochondria to sustain bioenergetics. We infer an unexpected level of ER plasticity in PCs, which exploit constitutive ER biogenesis as a default source of fatty acids as energy equivalents via an autophago-lysosomal recycling route.
- | Journal: UNC5B Overexpression Alleviates Peripheral Neuropathic Pain by Stimulating Netrin-1-Dependent Autophagic Flux in Schwann Cells. (Pubmed Central) - Aug 13, 2022
The enhanced phosphorylation of AMP-activated protein kinase (AMPK) and Unc51-like autophagy activating kinase 1 (ULK1) by UNC5B overexpression was also correlated with netrin-1. Our results suggest that UNC5B facilitates autophagic flux in SCs via phosphorylation of AMPK and ULK1, dependent on its ligand netrin-1, protecting myelin and partly preventing injury-induced NP.
- | Journal: TMEM189 promotes breast cancer through inhibition of autophagy-regulated ferroptosis. (Pubmed Central) - Aug 13, 2022
These findings suggested that TMEM189 could inhibit autophagy to mediate ferroptosis in breast cancer cells. Collectively, all our findings revealed the therapeutic potential of TMEM189 in the treatment of breast cancer.
- | Journal: New Monoterpene-Conjugated Phenolic Constituents from Nutmeg and Their Autophagy Modulating Activities. (Pubmed Central) - Aug 13, 2022
Compounds 4-6, 12, and 13 showed potent autophagy inhibitory activities in a concentration-dependent manner. Our findings showed an uncommon class of monoterpene-conjugated phenolic derivatives in nature and reported their autophagy inhibition activities for the first time, which may give a new insight into the benefits or safety of nutmeg in foods.
- | Preclinical, Journal: FXR deficiency in hepatocytes disrupts the bile acid homeostasis and inhibits autophagy to promote liver injury in Schistosoma japonicum-infected mice. (Pubmed Central) - Aug 13, 2022
All these findings suggest that FXR deficiency in hepatocytes disrupts bile acid homeostasis and inhibits autophagy, which may aggravate the damages of hepatocytes caused by S. japonicum infection. It highlights that FXR in hepatocytes plays a regulatory role in the progression of schistosomiasis.
- | Journal, IO biomarker: Curcumin activates autophagy and attenuates high glucose-induced apoptosis in HUVECs through the ROS/NF-κB signaling pathway. (Pubmed Central) - Aug 13, 2022
Furthermore, the addition of autophagy inhibitor 3-MA impaired the autophagy, exacerbated the apoptotic death and increased the ROS and NF-κB levels in HUVECs under the high glucose condition, P<0.05. In brief, autophagy served a protective role in the HG-induced apoptosis in HUVECs and CUR alleviated apoptosis by promoting autophagy and inhibiting the ROS/NF-κB signaling pathway.
- | temozolomide / Generic mfg.
Journal: STAT3-mediated upregulation of LINC00520 contributed to temozolomide chemoresistance in glioblastoma by interacting with RNA-binding protein LIN28B. (Pubmed Central) - Aug 12, 2022
Further experiments demonstrated that LINC00520 could interact with RNA-binding protein LIN28B to inhibit autophagy and reduce DNA damage, thereby contributing to TMZ chemoresistance in GBM. These findings suggested that STAT3/LINC00520/LIN28B axis might be a promising target to improve TMZ chemoresistance of GBM.
- | AZ 628 / AstraZeneca
Journal: AZ-628 delays osteoarthritis progression via inhibiting the TNF-α-induced chondrocyte necroptosis and regulating osteoclast formation. (Pubmed Central) - Aug 12, 2022
Similarly, the in vivo study demonstrated that AZ-628 could inhibit chondrocyte breakdown and lower osteoclast formation and bone resorption, thereby slowing down subchondral bone changes induced by dynamic bone remodeling and reversing the progression of osteoarthritis in mice. The results of this study indicate that AZ-628 could be used to treat OA byinhibiting chondrocyte necroptosis and regulating osteoclast formation.
- The Natural History of Familial Hypercholesterolemia Diagnosis, Treatment, and Outcomes in Patients With Incidental LDLR Pathogenic Mutation Found in Population Based Sequencing Study (Zone 1, Science and Technology Hall, Level 200) - Aug 11, 2022 - Abstract #AHA2022AHA_5167;
The results of this study indicate that AZ-628 could be used to treat OA byinhibiting chondrocyte necroptosis and regulating osteoclast formation. Abstract is embargoed at this time.
- doxorubicin hydrochloride / Generic mfg.
Chemotherapy in Pregnancy: Assessing the Safety of Adriamycin Administration in Pregnancy Complicated by Breast Cancer (Zone 4, Science and Technology Hall, Level 200) - Aug 11, 2022 - Abstract #AHA2022AHA_5073;
Abstract is embargoed at this time. Abstract is embargoed at this time.
- Sex Disparities in Outcomes of Adults With Cardiogenic Shock Using Impella; a Propensity-Matched Analysis (Zone 2, Science and Technology Hall, Level 200) - Aug 11, 2022 - Abstract #AHA2022AHA_3448;
Abstract is embargoed at this time. Abstract is embargoed at this time.
- | ifenprodil tartrate / Chiba University Hospital
Journal: Therapeutic advantage of targeting lysosomal membrane integrity supported by lysophagy in malignant glioma. (Pubmed Central) - Aug 11, 2022
Finally, chloroquine dramatically enhanced effects of the compounds inducing lysosomal membrane damage in a patient-derived xenograft model. These data demonstrate a therapeutic advantage of targeting lysosomal membrane integrity in GBM.
- | Journal: Celastrol upregulated ATG7 triggers autophagy via targeting Nur77 in colorectal cancer. (Pubmed Central) - Aug 11, 2022
Celastrol induced apoptosis and autophagy played an important role in human colorectal cancer, Nur77 was involved in the anti-CRC effect of celastrol and decreased expression of Nur77 induced high expression of ATG7. Celastrol exerted anti-CRC effects by inhibiting Nur77 to induce high expression of ATG7 signaling and Nur77/ATG7 signaling may be a potential pathway for colorectal cancer treatment.
- | Journal: The environmental enrichment ameliorates chronic unpredictable mild stress-induced depressive-like behaviors and cognitive decline by inducing autophagy-mediated inflammation inhibition. (Pubmed Central) - Aug 11, 2022
Celastrol exerted anti-CRC effects by inhibiting Nur77 to induce high expression of ATG7 signaling and Nur77/ATG7 signaling may be a potential pathway for colorectal cancer treatment. This study demonstrates that EE can play neuroprotective effects on depression and cognitive impairment by inducing autophagy-mediated inflammation inhibition, which accounts for the reduction of proinflammatory cytokines, including IL-1β, IL-6 and TNF-α.
- | fluoxetine / Generic mfg.
Preclinical, Journal: Fluoxetine Protects Against Inflammation and Promotes Autophagy in Mice Model of Post-traumatic Stress Disorder. (Pubmed Central) - Aug 11, 2022
Microglia depletion mice showed a lower inflammatory level. In conclusion, fluoxetine can promote autophagy and inhibit neuroinflammation in mice model of PTSD, providing a theoretical basis for fluoxetine in treating PTSD.
- | selisistat (SEN-196) / AOP Orphan Pharma
Journal: Salidroside Ameliorates Ultraviolet-Induced Keratinocyte Injury by Inducing SIRT1-Dependent Autophagy. (Pubmed Central) - Aug 10, 2022
SAL protected UVB-induced damage in a dependent manner on autophagy and SIRT1, as SAL-induced increase in viability was significantly attenuated by specific autophagy inhibitor Wortmannin (1 μM) or SIRT1 inhibitor EX-527 (100 nM). The present study results speculate that SAL suppresses UVB-induced injury and autophagy by enhancing SIRT1 expression.
- | sirolimus / Generic mfg.
Journal: Role of Autophagy Inducers and Inhibitors in Intestinal Barrier Injury Induced by Intestinal Ischemia-Reperfusion (I/R). (Pubmed Central) - Aug 10, 2022
The autophagy inhibitor 3-MA and the autophagy inducer rapamycin (RAP) were used to change the level of autophagy, and then, the expressions of tight junction proteins and intestinal barrier function were detected...In addition, promoting autophagy may promote occludin expression by inhibiting claudin-2 expression. Upregulation of autophagy levels by autophagy inducers can enhance intestinal epithelial barrier function after intestinal I/R.
- | Journal, IO biomarker: Therapeutic Mechanisms of Berberine to Improve the Intestinal Barrier Function via Modulating Gut Microbiota, TLR4/NF-κ B/MTORC Pathway and Autophagy in Cats. (Pubmed Central) - Aug 10, 2022
Berberine can restore intestinal microbiota homeostasis and regulate the TLR4/NF-κB pathway, thereby controlling inflammatory responses. We propose a novel mechanism of berberine therapy for IBD, namely, berberine therapy can simultaneously activate MTORC and autophagy to restore intestinal mucosal barrier function in cats, which should be further studied to shed light on berberine to IBD.
- | sirolimus / Generic mfg.
Journal: The human cathelicidin peptide LL-37 inhibits pancreatic cancer growth by suppressing autophagy and reprogramming of the tumor immune microenvironment. (Pubmed Central) - Aug 10, 2022
With combined treatment of LL-37 with the mTOR inhibitor rapamycin, LL-37-induced ROS production and cancer cell growth inhibition were attenuated...By using an in vitro co-culture system, it was shown that promotion of M2 macrophage polarization would be suppressed by LL-37 with inhibition of autophagy, which possessed significant negative impact on cancer growth. Taken together, our findings implicate that LL-37 could attenuate the development of pancreatic cancer by suppressing autophagy and reprogramming of the tumor immune microenvironment.
- | chloroquine phosphate / Generic mfg.
Journal: Type II alveolar epithelial cell aryl hydrocarbon receptor protects against allergic airway inflammation through controlling cell autophagy. (Pubmed Central) - Aug 10, 2022
The involvement of autophagy in airway inflammation was analyzed by using autophagy inhibitor chloroquine...In addition, RNA-seq analysis suggests that autophagy is one of the major pathways and that CALCOCO2/NDP52 and S1009 are major autophagy-associated genes in AT2 cells that may contribute to the AhR-mediated cockroach allergen-induced airway inflammation and, subsequently, allergic asthma. These results suggest that AhR in AT2 cells functions as a protective mechanism against allergic airway inflammation through controlling cell autophagy.
- | Preclinical, Journal: Ambient fine particulate matter exposure disrupts placental autophagy and fetal development in gestational mice. (Pubmed Central) - Aug 10, 2022
Correspondingly, AMPK/mTOR signaling pathway, a critical negative regulator of autophagy, was activated in placenta on GD15 by PM exposure as well. These findings provide evidences that placental developmental disorder caused by autophagy inhibition might be an important mechanism for the growth restriction caused by PM exposure.
- | Journal: Ginsenoside Rg1 suppresses paraquat-induced epithelial cell senescence by enhancing autophagy in an ATG12-dependent manner. (Pubmed Central) - Aug 10, 2022
Inhibition of autophagy via 3-MA or transfection of the siRNA targeting ATG12 can impair the antiaging effect of Rg1. Taken together, our data implicates that Rg1 can protect pulmonary epithelial cells from PQ-induced cellular senescence in an ATG12 dependent manner, which may provide a preventive and therapeutic strategy for PQ poisoning-induced pulmonary fibrosis.
- | chloroquine phosphate / Generic mfg.
Journal, IO biomarker: Selenium nanoparticles coupling with Astragalus Polysaccharides exert their cytotoxicities in MCF-7 cells by inhibiting autophagy and promoting apoptosis. (Pubmed Central) - Aug 10, 2022
Taken together, our data implicates that Rg1 can protect pulmonary epithelial cells from PQ-induced cellular senescence in an ATG12 dependent manner, which may provide a preventive and therapeutic strategy for PQ poisoning-induced pulmonary fibrosis. APS-Se NPs exerted their cytotoxic activity in MCF-7 cells by blocking autophagy and facilitating mitochondrial pathway-mediated apoptosis.
- | metformin / Generic mfg.
Journal: AXL Promotes Metformin-Induced Apoptosis Through Mediation of Autophagy by Activating ROS-AMPK-ULK1 Signaling in Human Esophageal Adenocarcinoma. (Pubmed Central) - Aug 10, 2022
AXL may be a valuable biomarker to identify tumors that are sensitive to metformin. Therefore, AXL expression could inform the selection of patients for future clinical trials to evaluate the therapeutic efficacy of metformin in EAC.
- Autophagy regulation using multifunctional chlorin-e6 polysilsesquioxane nanoparticles to improve photodynamic therapy of cancer (W178a (McCormick Place Convention Center)) - Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_6138;
Our results obtained reactive oxygen species (ROS) generation assay, apoptosis and autophagy flux analysis demonstrate that the reduced autophagy flux mediated by the combination approach afforded an increase in the phototherapeutic efficacy of Ce6-PSilQ nanoparticles. We envision that the promising results in the use of multimodal Ce6-PSilQ material against cancer pave the way of its evaluation in preclinical models.
- Synthesis and optimization of autophagy modulators for evaluation in Niemann-Pick type C disease | Poster Board #3168 (Hall F2 (McCormick Place Convention Center)) - Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_3356;
Current efforts are focused on the synthesis of analogues to improve the potency and properties of the initial hits. One the two identified hits was a racemic mixture, so our major goals have been to develop a strategy to efficiently access both enantiomers, to determine which enantiomer is responsible for the observed biological activity, and to prepare analogues of the active enantiomer to optimize this hit in preparation for in vivo evaluation in NPC animal models.
- chloroquine phosphate / Generic mfg., hydroxychloroquine / Generic mfg.
Synthesis and optimization of ATG14L-beclin 1 protein-protein interaction inhibitors to selectively inhibit autophagy | Poster Board #3174 (Hall F2 (McCormick Place Convention Center)) - Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_3319;
Our current focus is the iterative synthesis and testing of analogues to improve the potency and properties of compound 19 to support in vitro and in vivo efficacy studies. These efficacy studies will help clarify the role of autophagy in cancer through selective inhibition of this pathway and will reveal the utility of autophagy inhibition as a potential therapeutic strategy in cancer.
- chloroquine phosphate / Generic mfg., hydroxychloroquine / Generic mfg.
Development of autophagy inhibitors that target the ATG5-ATG16L1 protein-protein interaction | Poster Board #3175 (Hall F2 (McCormick Place Convention Center)) - Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_3289;
We identified two inhibitors using this target-based assay, but they did not show significant activity in cells, potentially due to their lack of solubility and moderate potency. Our current focus is the development of synthetic strategies to access both of these hits and analogues to improve potency and properties to enable evaluation of ATG5-ATG16L1 protein-protein interaction inhibitors in cancer cells.Synthetic route for hit compound, H3.
- chloroquine phosphate / Generic mfg., hydroxychloroquine / Generic mfg.
Synthesis of reverse sulfonamide analogues of an ATG14L-Beclin1 protein-protein interaction inhibitor | Poster Board #2701 (Hall F2 (McCormick Place Convention Center)) - Aug 9, 2022 - Abstract #ACSFall2022ACS_Fall_1252;
Our current focus is the iterative synthesis and evaluation of compound 19 analogues to improve potency and solubility of the original hit. Compounds with improved activity and properties will enable the evaluation of this novel therapeutic strategy in cancer cell lines and animal models.
- | deferoxamine / Generic mfg.
Journal: NCOA4-mediated ferritinophagy is involved in ionizing radiation-induced ferroptosis of intestinal epithelial cells. (Pubmed Central) - Aug 7, 2022
In addition, the iron chelator deferoxamine (DFO) attenuated IR-induced ferroptosis and intestinal injury in vitro and in vivo...In addition, mice fed with an iron-deficient diet for 3 weeks showed a significant reversal in the intestinal injury induced by abdominal IR exposure. Taken together, ferroptosis is a novel mechanism of IR-induced intestinal epithelial cytotoxicity, and is dependent on NCOA4-mediated ferritinophagy.