"Combination of epirubicin with the autophagy inhibitor hydroxychloroquine resulted in a significant reduction in tumor growth compared with monotherapy with epirubicin."
"Herein, we describe our current understanding of the core components of the autophagy machinery, the functional relevance of autophagy within the tumor microenvironment and outline how this knowledge has informed preclinical investigations combining the autophagy inhibitor hydroxychloroquine (HCQ) with chemotherapy, targeted therapy and immunotherapy."
"Chloroquine (and its derivative hydroxychloroquine) inhibits autophagy, which is the proposed mechanism of its anti-ZIKV action since deficiency in an essential autophagy gene, Atg16l1, in mice limited ZIKV vertical transmission, placental and fetal damage, and improved placental and fetal outcomes overall."
"Based on the different types of inhibitory analyses, 10mM of the autophagy inhibitor 3-methyladenine (3-MA, Sigma-Aldrich Co., St. Louis, MO, USA), 100nM of the autophagy inhibitor bafilomycin A1 (ba A1, Sigma-Aldrich Co., St. Louis, MO, USA), 50muM of the autophagy inhibitor hydroxychloroquine (Selleck Chemicals, Houston, TX, USA), 5muM of the AKT inhibitor triciribine (Selleck Chemicals, Houston, TX, USA), 5muM of the PI3K agonist insulin like growth factors-1 (IGF-1, R&D Systems, Inc., Minneapolis, USA), 5muM of the PI3K inhibitor LY294002 (Selleck Chemicals, Houston, TX, USA), and 1muM of the mTOR inhibitor rapamycin (Rapa, Selleck Chemicals, Houston, TX, USA) were added to the culture medium together with HSYA for 4h."
"For these reasons, it is no surprise that autophagy inhibitors such as hydroxychloroquine are actively trialed in the clinic for treatment of cancers and development of novel autophagy inhibitors are earnestly pursued."
"In fact, the autophagy inhibitor hydroxychloroquine (HCQ) is currently in clinical trials to examine whether co-treatment with HCQ and imatinib offers a therapeutic benefit over imatinib alone [48]."
"It is thus reasonable to consider a cancer treatment approach that combines traditional anti-cancer chemotherapy with autophagy inhibitors such as hydroxychloroquine."
"Autophagy inhibitor hydroxychloroquine (HCQ) was used to identify the sensitivity of breast cancer subtypes to autophagy inhibition in the present study."
"The only autophagy inhibitors whose effectiveness in vivo and safety in clinical trials have been approved by the FDA are chloroquine (CQ) and its derivative hydroxychloroquine (HCQ) that suppress autophagy by blocking autophagosome fusion and degradation."
"To differentiate this, we treated the MCL cell line Mino with palbociclib and the downstream autophagy inhibitor hydroxychloroquine which inhibits the acidification of lysosomes, completely blocks autophagy in its final step and therefore leads to the accumulation of autophagosomes [XREF_BIBR]."
"Chi et al. reported a 40% response rate and a 84% disease control rate by simultaneously adding the autophagy inducer rapamycin and the autophagy inhibitor hydroxychloroquine in 25 patients with various tumor types presenting with intrinsic resistance to numerous MC regimens [XREF_BIBR]."
"ROC-325 exhibited superior in vitro anticancer effects than the existing autophagy inhibitor hydroxychloroquine in 12 different cancer cell lines with diverse genetic backgrounds."
"Hydroxychloroquine (HCQ), a drug routinely used in the clinical treatment of malaria and autoimmune disorders [XREF_BIBR], is a potent inhibitor of autophagy."
"Herein, we describe our current understanding of the core components of the autophagy machinery and the functional relevance of autophagy within the tumor microenvironment, and we outline how this knowledge has informed preclinical investigations combining the autophagy inhibitor hydroxychloroquine (HCQ) with chemotherapy, targeted therapy, and immunotherapy."
"Autophagy inhibition by chloroquine and hydroxychloroquine could adversely affect AKI and other organ injury in critically ill patients with COVID-19."
"Hydroxychloroquine inhibits autophagy to potentiate antiestrogen responsiveness in ER+ breast cancer."
"Hydroxychloroquine inhibits systemic inflammation and autophagy and may thus have antineoplastic effects [1]."
"[Effect of Autophagy Inhibitor Hydroxychloroquine on Chemosensitivity of Castration resistant Prostate Cancer]."
"Chloroquine and hydroxychloroquine accumulate within lysosomes and are thought to block autophagy by elevating intralysosomal pH and inhibiting lysosomal enzymes [XREF_BIBR, XREF_BIBR]."
"In this Phase I/II clinical trial, we establish that preoperative treatment with the autophagy inhibitor hydroxychloroquine in combination with chemotherapy is safe and tolerable."
"Correction : Hydroxychloroquine Inhibits Autophagy to Potentiate Antiestrogen Responsiveness in ER+ Breast Cancer."
"Given the overall similar behavior to the autophagy inhibitor hydroxychloroquine (HCQ) (XREF_SUPPLEMENTARY), and that AMPK, CK2 and the PIK3C3 complex II positively regulate autophagy, palbociclib likely also inhibits autophagy."
"Since bafilomycin A1 could have non-autophagy-related activities, we performed confirmatory experiments with additional autophagy inhibitors including hydroxychloroquine sulfate (lysosomal acidification inhibitor), 3-methyladenine (3-MA, PI3K inhibitor), and MHY1485 (mTOR agonist)."
"Results : ROC-325 exhibited superior in vitro anticancer effects compared with the existing autophagy inhibitor hydroxychloroquine (HCQ) in 12 different cancer cell lines with diverse genetic backgrounds."
"Other inhibitors, such as 1) Bafilomycin A 1, a specific inhibitor of vacuolar-type H (+)-ATPases; 2) hydroxychloroquine, a lysosomal lumen alkalizer; and 3) pepstatin A, an inhibitor of acid proteases, have also been used to inhibit complete autophagy."
"Inhibition of autophagy by hydroxychloroquine, a well tolerated autophagy inhibitor, reduced cell viability in both ETV6-RUNX1 positive cell lines and primary acute lymphoblastic leukemia samples, and selectively sensitized primary ETV6-RUNX1 positive leukemia samples to L-asparaginase."
"When autophagy was pharmacologically suppressed by hydroxychloroquine , PEDV replication decreased from 8.5 x 105 TCID50 / mL to 7.9 x 104 TCID50 / mL ."
"Moreover, in vivo inhibition of autophagy by hydroxychloroquine in B16-F10 tumor bearing mice and mice vaccinated with tyrosinase related protein-2 peptide dramatically increased tumor growth inhibition."
"Antimalarial drugs, chloroquine and hydroxychloroquine, inhibit autophagy and are undergoing clinical trials as antitumor drugs XREF_BIBR."
"Autophagy was inhibited by hydroxychloroquine (HCQ), whereas the ability of Dex resistant MMcells to recover the susceptibility to apoptosis was measured."
"XREF_BIBR, XREF_BIBR In addition to its immunomodulatory effects, hydroxychloroquine has been noted to inhibit cellular autophagy."
"The lysosomotropic agents chloroquine and hydroxychloroquine have been used to impair the autophagy pathway, where their properties as weak bases suppress the degradation of autophagic cargo by lysosomal enzymes."
"Although a number of studies have demonstrated that autophagy may sensitize certain tumor cells to chemotherapeutic agents [XREF_BIBR - XREF_BIBR], the clinical applications of autophagy inhibitors such as CQ and hydroxychloroquine have been limited by their efficacy and side effects [XREF_BIBR, XREF_BIBR]."
"Interestingly, a phase 1 clinical trial including patients with relapsed and refractory myeloma showed promising results for the combination of bortezomib with the autophagy inhibitor hydroxychloroquine corroborating our results [XREF_BIBR]."
"Blockade of autophagy by hydroxychloroquine dramatically potentiated KG-135-induced FOXO3a and its downstream (FasL) ligand accompanied by the cleavage of caspase-8."
"Autophagy inhibitors, such as chloroquine and hydroxychloroquine, are currently in clinical trials for multiple types of cancer [XREF_BIBR]."
"Furthermore, preventing the acidification of lysosomes, hydroxychloroquine impairs cellular autophagy, a critical step for innate and adaptive immunity activation [XREF_BIBR]."
"Notably, we observed that treatment with the autophagy inhibitor hydroxychloroquine reduced T cell mediated tumor killing."
"Given the divergent conclusions of published studies regarding autophagy protein markers and autophagosome formation, the utility of autophagy inhibitors (lysosomotropic agents) such as chloroquine (CQ) or hydroxychloroquine (HCQ) in clinical trials for melanoma (either alone or as a combination therapy) supports conclusions in the literature that autophagy is a pro survival feature of melanomas, and so inhibiting the process pharmacologically is not only of clinical relevance, but a priority [XREF_BIBR, XREF_BIBR, XREF_BIBR]."
"Hydroxychloroquine has been shown to inhibit autophagy, a process by which dying cells recycle injured organelles and internal toxins to generate needed energy for survival and reproduction."
"Furthermore, unfortunately, single proteasome inhibitor treatment has been proven unsatisfactory for solid tumors in clinical trials.5, 6 A recent clinical trial suggested that the anticancer effect of Bor is enhanced when it is combined with an autophagy inhibitor.7 To date, autophagy inhibitors including hydroxychloroquine (HCQ) and chloroquine (CQ) have been clinically viable."
"Accordingly, selective triple knockdown of the autophagy genes ATG7, ATG5 and ATG3, and pretreatment with the autophagy inhibitor hydroxychloroquine, efficiently overcame the resistance to Akt and mTOR inhibitors, leading to the activation of the mitochondrial apoptotic pathway."
"Autophagy was involved in doxorubicin induced resistance of myeloma cell line RPMI8226, DOX resistance in myeloma cells was reversed partly by autophagy inhibitor hydroxychloroquine or 3-MA, and autophagy may be one of mechanisms for drug resistance."
"XREF_BIBR - XREF_BIBR It is thus seemingly paradoxical that hydroxychloroquine, an anti-malarial drug that blocks autophagy by raising intralysosomal pH, is under evaluation in multiple cancer trials (XREF_TABLE)."
"In addition to the existing autophagy inhibitors such as hydroxychloroquine and chloroquine, which are approved for treatment of malaria by US FDA, identification of novel and highly effective autophagy inhibitors is obviously needed."
"Chloroquine (CQ) and its derivative hydroxychloroquine (HCQ), which are clinically used antimalarial drugs, also inhibit autophagy by preventing the acidification of the lysosomal compartment XREF_BIBR."
"These findings are currently under clinical investigation with several studies examining whether pharmacologic inhibition of autophagy with the anti-malaria and non specific autophagy inhibitor hydroxychloroquine augments the efficacy of standard anticancer regimens [XREF_BIBR - XREF_BIBR]."
"Similar to previously published data, treatment with the prototypical autophagy inducer rapamycin increased ZIKV titers whereas the prototypical autophagy inhibitor hydroxychloroquine decreased titers [XREF_BIBR, XREF_BIBR, XREF_BIBR]."
"Hydroxychloroquine has been shown to inhibit autophagy."
"Moreover, a study using murine endometriosis model revealed that inhibition of autophagy by hydroxychloroquine effectively promotes apoptosis of human endometriotic cells and decreases the number of endometriotic lesions."
"Meanwhile, autophagy inhibition by 3-methyaldenine (3-MA) and hydroxychloroquine, as well as by siRNA knocking down of Beclin-1 or ATG-7, inhibited AZD-2014-induced cytotoxicity, while the apoptosis inhibitor had no rescue effect."
"Finally, administration of vemurafenib with the autophagy inhibitor hydroxychloroquine promoted more pronounced tumor suppression in vivo."
"Hydroxychloroquine (HCQ) inhibits lysosomal acidification and blocks autophagy via influencing autophagosome fusion and degradation."
"The antimalarial drug hydroxychloroquine blocks autophagy, inhibits the growth of cancer cells, and induces cell death [XREF_BIBR] (see XREF_FIG)."
"In light of the sensitizing effect of autophagy inhibition on chemotherapy induced cell death, a number of clinical trials have been launched combining the first generation autophagy inhibitor hydroxychloroquine (HCQ) with individual chemotherapeutic agents in patients with solid tumors."
"Hydroxychloroquine and chloroquine inhibits autophagy by entering the lysosomes (lysosomotropic) and changing the acidity through chelating protons."
"Thus, the effect of the autophagy inhibitor Hydroxychloroquine (HCQ) on B16-F10 tumor growth was evaluated alone or in combination with a Tyrosinase Related Protein-2 (TRP2) peptide based vaccination strategy."
"During the later stages of tumor progression, autophagy is thought to be important for tumor cell survival such that autophagy inhibitors like chloroquine or hydroxychloroquine can sensitize certain cells to chemotherapeutic agents [XREF_BIBR, XREF_BIBR - XREF_BIBR]."
"When autophagy was pharmacologically suppressed by hydroxychloroquine, PEDV replication decreased from 8.5 x10 5 TCID 50 / mL to 7.9 x10 4 TCID 50 / mL."
"Fortuitously, the autophagy inhibitor hydroxychloroquine (a chloroquine derivative) has been used for many years in the management of patients with systemic lupus erythematosus, rheumatoid arthritis and malaria and therefore information about dosage, safety and side-effects has been available."
"AML CD34 + cells were more sensitive to the autophagy inhibitor hydroxychloroquine (HCQ) than normal bone marrow CD34 + cells."
"The effects of autophagy on cell proliferation and apoptosis were studied by autophagy inhibitor hydroxychloroquine (HCQ) and autophagy promoter Rapamycin."
"Next, we tested the effects of hydroxychloroquine (HCQ), which inhibits autophagy by impairing the lysosomal acidification of the autophagic cargo, blocking the fusion of autophagosomes with lysosomes [XREF_BIBR]."
"Unlike the autophagy inhibitor hydroxychloroquine, however, Y100 treatment does not result in accumulation of lipidated LC3B (LC3B-II), suggesting that it causes p62 accumulation via a distinct mechanism."
"Autophagy inhibitors, such as chloroquine and hydroxychloroquine, have already been clinically approved, promoting drug combination treatment by targeting autophagic pathways as a means of discovering and developing more novel and more effective cancer therapeutic approaches."
"Autophagy inhibition by hydroxychloroquine (HCQ) reduced the effect of nilotinib in vivo."
"Autophagy inhibitor hydroxychloroquine (HCQ), ERK1/2 inhibitor U0126 and AKT inihbitor MK-2206 were obtained from Selleck Chemicals LLC (Houston, TX, USA)."
"Furthermore, high glucose induced autophagy in ARPE-19 with the treatment of glucose for 48h, and autophagy inhibitor hydroxychloroquine (HCQ) or bafilomycin further aggravated the senescence, accompanying by an increase in oxidant species."
"On other hand, CQ, Hydroxychloroquine, and Bafilomycin A inhibit autophagy at late stages by suppressing the lysosomal function XREF_BIBR - XREF_BIBR."
"Xie et al. showed that mTOR dependent melanoma cells can be driven to apoptosis when treated with the mTOR inhibitor temsirolimus and the autophagy inhibitor hydroxychloroquine."
"Hydroxychloroquine inhibits systemic inflammation and autophagy and may thus have antineoplastic effects [XREF_BIBR]."
"Bafilomycin A1 and hydroxychloroquine inhibit autophagy by preventing the fusion of autophagosomes and lysosomes."
"To see whether autophagy inhibition improves the efficacy of PI3K inhibitor in PIK3CA-mutant cancer cells, cells were treated with BKM120, a pan-PI3K inhibitor, and the autophagy inhibitor hydroxychloroquine (HCQ)."
"We also showed that treatment with the autophagy inhibitor hydroxychloroquine (HCQ) significantly decreased the cell viability of Ad-Fhit-infected H460 cells."
"We also found that the lysosomotropic agent and autophagy inhibitor hydroxychloroquine (HCQ) synergizes with CCI-779 and led to melanoma cell death via apoptosis."
"Adding hydroxychloroquine that inhibits autophagy would make it more difficult to clear the hydrogen peroxide, leading to quicker cell death."
"Based on the successful experimental findings in vitro and in vivo, clinical trials of autophagy inhibitor such as hydroxychloroquine in combination with chemotherapy in patients with blood cancers are currently underway."
"We here demonstrate that hydroxychloroquine preferentially induces apoptosis of CD45RO+ memory and effector T cells by inhibiting the survival pathway of autophagy."
"Rapamycin and its analogs are strong inducers of autophagy by inhibiting mTOR activity, and hydroxychloroquine can inhibit autophagy by blocking the fusion of autophagosomes with lysosomes."
"The latest reports have shown that the autophagy inhibitor hydroxychloroquine is tolerable and potentially effective in combination with the MTOR targeted agent temsirolimus XREF_BIBR and the proteasome inhibitor bortezomib XREF_BIBR in phase I trials and may be a valid complement to STAT3 targeted therapy."
"Interestingly, HLTF was found to be one of the genetic determinants conferring sensitivity or resistance to lysosomal autophagy inhibitors such as hydroxychloroquine (HCQ) in several cancer cell lines XREF_BIBR."
"Classic autophagy inhibitors such as chloroquine and hydroxychloroquine have been introduced into phase I/II clinical trials, while more experimental compounds are moving forward in preclinical development."
"Hydroxychloroquine (HCQ) has been shown to disrupt autophagy and sensitize cancer cells to radiation and chemotherapeutic agents."
"The most recent reports have shown that the autophagy inhibitor hydroxychloroquine is tolerable and potentially effective in combination with the MTOR targeted agent temsirolimus [XREF_BIBR] and the proteasome inhibitor bortezomib [XREF_BIBR] in phase I trials (www.clinicaltrials.gov)."
"Here, effects of the autophagy inhibitor hydroxychloroquine (HCQ) and activator LiCl on postharvest jujube fruit senescence were investigated."
"Additionally, hydroxychloroquine, a derivative of chloroquine, has been shown to inhibit autophagy in cancer cells and restore sensitivity to ER pathway inhibitors, such as tamoxifen, in ER positive cancer cells [XREF_BIBR]."
"Recently, a phase I/II study in patients with glioblastoma multiforme showed that hydroxychloroquine could inhibit autophagy in vivo [XREF_BIBR]."
"Hydroxychloroquine (HCQ) inhibits autophagy."
"The pharmacological targeting of control points of the autophagy system by combining established cancer treatments with autophagy inhibitors such as Atg5/7 silencing or hydroxychloroquine was presented by Professor Eileen White of Rutgers University (NJ, USA)."
"In contrast, the autophagy inhibitors hydroxychloroquine (HCQ), 3-methyladenine (3-MA), and bafilomycin A1 (BafA1) prevented ENT1 degradation and enhanced RBV antiviral activity."
"To explore potential anti-melanoma activity of systemic autophagy deficiency, pharmacologic inhibition (as opposed to genetic ablation), of autophagy was tested by administration of the lysosomal autophagy inhibitor hydroxychloroquine (HCQ)."
"In fact, the autophagy inhibitor hydroxychloroquine (HCQ) is currently in clinical trials to examine whether co-treatment with HCQ and imatinib offers a therapeutic benefit over imatinib alone [XREF_BIBR]."
"Rapamycin can inhibit the proliferation, induce apoptosis and autophagy of RPMI 8226, the hydroxychloroquine can inhibit autophagy and proliferation of RPMI 8226, and induce apoptosis, the 3-MA can inhibit autophagy of RPMI 8226, but hardly has any effects on proliferation and apoptosis of RPMI 8226 cells."
"Autophagy inhibitors such as 3-MA (a class-III-PI3K inhibitor), bafilomycin A1, hydroxychloroquine and monensin (autophagosome-lysosome fusion inhibitors) have shown different efficacies in mitigating the effects of chemo- and radiotherapeutic anti-cancer treatments [XREF_BIBR], indicating the complexity with which this process is executed."
"Chloroquine and hydroxychloroquine accumulate within lysosomes and are thought to block autophagy through elevation of intralysosomal pH and inhibition of lysosomal enzymes XREF_BIBR, XREF_BIBR."
"Consistent with this hypothesis, a cytoprotective role of autophagy in established tumors exposed to stressors like anticancer treatments is suggested in studies where autophagy inhibitors like hydroxychloroquine or 3-methyladenine (3-MA) sensitize cancer cells to treatments like tamoxifen treatment, radiation, DNA alkylating agents cylophosphamide and cisplatin, and tyrosine kinase receptor inhibitor imatinib."
"Furthermore, inhibition of autophagy by hydroxychloroquine (HCQ) or shRNA targeting BECN or Atg5 led to increased sensitivity to GCB in LM7 OS cells and decreased sensitivity to GCB in the CCH-OS-D and K7M3 cells, confirming the dual role of autophagy in OS."
"In contrast, the autophagy inhibitors hydroxychloroquine (HCQ), 3-methyladenine (3-MA), and bafilomycin A1 (BafA1) prevented ENT1 degradation and enhanced RBV antiviral activity."
"Therefore, autophagy inhibitors, such as chloroquine or hydroxychloroquine, have a therapeutic potential in cancer treatment XREF_BIBR - XREF_BIBR."
"In a relevant clinical trial in dogs with non Hodgkin 's lymphoma, the combined treatment of autophagy inhibitor hydroxychloroquine (12.5 mg/kg/d) with a lower dose of doxorubicin (25 mg/m 2) has resulted in clinical benefit with superior overall response rate (93.3%) and comparable median progression-free interval (5 months) compared to standard single agent doxorubicin (30 mg/m 2) treatment [XREF_BIBR]."
"Chloroquine (CQ) and hydroxychloroquine (HCQ) are known to inhibit autophagy and have been investigated in preclinical studies and in more than 30 clinical trials; however, the ocular toxicities and minimal single-agent anticancer efficacy of CQ or HCQ have restricted their clinical application."
"Appropriate interpretation of the outcomes of these trials would require knowledge as to whether the drugs or radiation used promote the cytoprotective form of autophagy in the tumor cells as well as whether the chloroquine or hydroxychloroquine actually inhibit the autophagy."
"Autophagy inhibitors such as 3-MA and hydroxychloroquine sensitize tumors to the anti-cancer drugs, while autophagy inducers like rapamycin inhibits tumor proliferation 44 and sensitizes tumors to the radiation 45."
"We thus conducted a first-in-human study to investigate the safety, preliminary efficacy, pharmacokinetics (PK), and pharmacodynamics (PD) of the combination of the autophagy inhibitor hydroxychloroquine (HCQ) and VOR in patients with advanced solid tumors."
"Here we demonstrate that in human T cells there is a basal level of autophagy and that the inhibition of autophagy by hydroxychloroquine induces apoptosis."
"Moreover, current clinical trials use the autophagy inhibitor hydroxychloroquine for treatment of a wide range of cancers, with promising results [XREF_BIBR - XREF_BIBR]."
"The autophagy inhibitors such as hydroxychloroquine (HCQ), 3-methyladenine (3-MA) might be helpful to restore the sensitivity of the resistant cells to Lapatinib via abolishing the formation process and degradation ability of autophagosome [33,34]."
"The PEDV yield was suppressed when autophagy was inhibited by hydroxychloroquine at an early stage, while the viral titers were increased when autophagy was induced by rapamycin."
"Based on such evidence, clinical trials are underway in which various cancers are being treated with a combination of existing anticancer drugs and autophagy inhibitors such as chloroquine and hydroxychloroquine XREF_BIBR XREF_BIBR."
"Two antimalarial drugs, CLQ and hydroxychloroquine, inhibited the autophagy induced by p53 mediated apoptosis and augmented the anticancer activity of cyclophosphamide in Myc driven lymphoma [XREF_BIBR, XREF_BIBR]."
"We investigated the effects of the autophagy inhibitor hydroxychloroquine (HCQ) on cell death of cytosine arabinoside (Ara-C)-resistant human acute myeloid leukemia (AML) cells."
"We have explored the ability of hydroxychloroquine (HCQ), which inhibits autophagy, to affect antiestrogen responsiveness."
"Hydroxychloroquine preferentially induces apoptosis of CD45RO+ effector T cells by inhibiting autophagy : A possible mechanism for therapeutic modulation of T cells."
"Lysosomal autophagy inhibitors (LAI) such as hydroxychloroquine (HCQ) have significant activity in a subset of cancer cell lines."
"Recent studies showed that hydroxychloroquine can inhibit the latter step of autophagy and therefore enhance the anti-glioma efficiency of ZD6474, a tyrosine kinase inhibitor."
"Although some clinical successes have been noted with chloroquine, a phase I/II clinical trial with the autophagy inhibitor hydroxychloroquine administered in combination with standard and adjuvant chemoradiotherapy failed to show a significant benefit in patients with newly diagnosed GBM."
"This is in accordance with the recent clinical trial showing dose dependent inhibition of autophagy by hydroxychloroquine in GBM patients and suggests that dosing needs to be adapted to the specific patient tumour."
"Appropriate interpretation of the outcomes of these trials would require knowledge as to whether the drugs or radiation utilized promote the cytoprotective form of autophagy in the tumor cells as well as whether the chloroquine or hydroxychloroquine actually inhibited the autophagy."
"As discussed above, current autophagy inhibitors, such as chloroquine, hydroxychloroquine, and bafilomycin A1, mainly inhibit lysosomal functions."
"Autophagy inhibitor hydroxychloroquine sulfate (HCQ) was obtained from Tokyo Chemical Industry (Japan)."
"Chloroquine and hydroxychloroquine inhibit autophagy at a late stage by blocking lysosomal acidification resulting in an inability to digest its engulfed cargo."
"A significant decrease in tumor growth in mice treated with the autophagy inhibitor hydroxychloroquine (HCQ) was reported 53."
"Interestingly, in vivo administration of the autophagy inhibitor hydroxychloroquine (HCQ) with a tyrosinase related protein-2 (TRP2) peptide based vaccination strategy led to a significant reduction of melanoma growth compared to vaccine or HCQ treatment alone."
"Autophagy inhibition by chloroquine and hydroxychloroquine could adversely affect AKI and other organ injury in critically ill patients with COVID-19."
"We have previously shown that autophagy is rapidly induced following TKI treatment in CML cells and pharmacological autophagy inhibition, using the nonspecific autophagy inhibitor hydroxychloroquine (HCQ; inhibits autophagy at a late stage by preventing the fusion of autophagosomes and lysosomes), enhances the effect of TKI treatment in CML cells, including primary CD34 + stem or progenitor cells."
"Similarly, the effects of 5-FU are augmented in colon cancer when treated with autophagy inhibitor hydroxychloroquine (HCQ)."
"Currently, autophagy inhibitors such as CQ and hydroxychloroquine (HCQ) are under investigation in clinical phase I/II for various cancers including lung cancer [XREF_BIBR, XREF_BIBR]."
"Consistent with these findings, we show that Tat protein levels increase dramatically in cells with the autophagy inhibitor hydroxychloroquine, which permeabilizes lysosomal membranes, blocking both macroautophagy as well as chaperone mediated autophagy."
"Blockade of autophagy by hydroxychloroquine (HCQ) potentially enhances the KG-135-mediated increase of FOXO3a and its downstream death receptor ligand Fas ligand (FasL), as well as the decrease of survivin and Bcl-2, resulting in massive apoptosis."
"We performed a randomized controlled trial to assess the autophagy inhibitor hydroxychloroquine in combination with gemcitabine and nab-paclitaxel."
"Autophagy inhibitors such as hydroxychloroquine are being tested in a number of clinical trials as a chemo sensitizer."
"The results of this study are predicted to show that hydroxychloroquine effectively reduces autophagy in tumor cells and make them more likely to undergo cell death in the hypoxic environment since the main survival mechanism of the tumor cells is eliminated."
"The antimalarial drugs chloroquine and hydroxychloroquine inhibit autophagy, leading to increased cytotoxicity in combination with several anticancer drugs in preclinical models."
"Currently, the only FDA approved agents able to inhibit autophagy are chloroquine, an anti-malaria drug, and its derivative hydroxychloroquine, which block autophagy by disrupting lysosome acidification."
"Given recent studies demonstrating that autophagy is a resistance mechanism to multiple therapeutic agents in the setting of apoptotic inhibition, we hypothesized that hydroxychloroquine (HCQ), an anti-malarial drug that inhibits autophagy, will increase cytotoxicity of ABT-737."
"XREF_BIBR, XREF_BIBR Chloroquine and hydroxychloroquine can inhibit autophagy induced by p53 controlled apoptosis in Myc driven lymphoma and augmented the anticancer activity of cyclophosphamide."
"Our previous work demonstrated that co-treatment with the autophagy inhibitor hydroxychloroquine (HCQ) could effectively block the last step of autophagy and enhance cell death induced by activation of p53 or treatment with alkylating chemotherapy in a model of Myc induced tumorigenesis."
"In this regard, we also show that treatment of mice with the autophagy inhibitor hydroxychloroquine, which is currently being used in several clinical trials, significantly accelerates tumour formation in mice containing oncogenic Kras but lacking p53."
"More recently, two second generation autophagy inhibitors, Lys05 a highly potent lysosometric agent and PIK-III a selective inhibitor of VPS34, demonstrated synergistic effects with TKIs to reduce primary CML LSCs quiescence, compared to the first generation autophagy inhibitor Hydroxychloroquine [XREF_BIBR]."
"Recently, preclinical studies demonstrated that autophagy inhibition by hydroxychloroquine augments the efficacy of the proteasome inhibitor bortezomib in myeloma, indicating that the combination of autophagy and proteasome inhibition might be clinically useful for improving the outcomes of this neoplasia [XREF_BIBR, XREF_BIBR]."
"Hydroxychloroquine (HCQ) inhibits autophagy and therefore can sensitize some cancer cells to chemotherapy, but the high doses required limit its clinical use."
"When autophagy was pharmacologically suppressed by hydroxychloroquine , PEDV replication decreased from 8.5 x 10 5 TCID 50 / mL to 7.9 x 10 4 TCID 50 / mL ."
"Research has shown that treatment with the autophagy inhibitor hydroxychloroquine reduces the incidence of ZIKV vertical transmission in pregnancy."
"Furthermore, selective triple knockdown of the autophagy genes ATG7, ATG5 and ATG3, and pre-treatment with the autophagy inhibitor hydroxychloroquine, efficiently overcame the resistance to Akt and mTOR inhibitors in this model, leading to the activation of the mitochondrial apoptotic pathway."
"The lysosomotropic agent hydroxychloroquine (HCQ), has been shown to inhibit autophagy in preclinical cancer models XREF_BIBR."
"Vorinostat and hydroxychloroquine improve immunity and inhibit autophagy in metastatic colorectal cancer."
"HeLa cells exposed to the autophagy inhibitors hydroxychloroquine, bafilomycin A1, and monensin displayed increased mitochondrial cell death."
"Inhibition of autophagy by hydroxychloroquine enhances antioxidant nutrients and delays postharvest fruit senescence of Ziziphus jujuba."
"Autophagy flux induced by apelin-13 was inhibited by NAC and catalase but not hydroxychloroquine (HCQ)."
"Introduction Hydroxychloroquine ( Plaquenil ) is an aminoquinoline that is commonly used to treat malaria and a variety of rheumatic and dermatologic diseases , including systemic lupus erythematosus , rheumatoid arthritis , Sjogren syndrome , and porphyria cutanea tarda.1 ,2 In addition to its immunomodulatory effects , hydroxychloroquine has been noted to inhibit cellular autophagy ."
"Multiple trials using relatively nonspecific autophagy inhibitors, such as chloroquine and hydroxychloroquine, have been launched for the treatment of cancer."
"For example, there are currently almost 3 dozen clinical trials in the U.S. attempting to block the cellular survival functions of autophagy in cancer treatment by combining chemotherapy with the autophagy inhibitor hydroxychloroquine."
"Furthermore, because patients with Copa syndrome show an increase in autophagy with abnormal autophagosomes, hydroxychloroquine, which prevents autophagy by inhibiting lysosomal acidification and impairing fusion of the autophagosome with the lysosome, may also be useful for therapy for Copa syndrome."
"To assess the functional importance of increased levels of autophagy observed in aggressive compared to indolent melanoma spheroids, spheroids were treated with PBS or a low dose of the autophagy inhibitor hydroxychloroquine."