IndraLab

Statements

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"The lower dependence of SARS-CoV-2 on the endosomal pathway explains the limited effect of endosomal acidification inhibitors such as hydroxychloroquine on restricting SARS-CoV-2 infection of target cells ."
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"CQ or HCQ inhibits lysosomal acidification and blocks the terminal phase of autophagy, potentiating the effects of different chemotherapeutic compounds, such as hydroxamic acid, suberoylanilide (SAHA)[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"HCQ can effectively inhibit lysosomal acidification and fusion of mitophagosomes with lysosomes to block the degradation of mitochondria65, which has been widely used in phase I and phase II clinical trials in combination with other anticancer agents66."
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"These data support the concern that some autophagy inhibitors such as HCQ that inhibit the fusion between autophagosomes and lysosomes could counteract some of the tumor inhibitory effects of autophag[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Concerning the molecular mechanism for their known antiviral activity, chloroquine or hydroxychloroquine was previously proposed to inhibit acidification of endosome and viral endocytosis."
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"Moreover, Nf2 cells were relatively insensitive to the lysosomal acidification inhibitor hydroxychloroquine (HCQ) or inhibition of PIKfyve localization (FTY720), which is important for the lysosomal processing of both autophagosomes and macropinosomes (Fig. 4F; Kim et al. 2016)."
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"Currently, two autophagic inhibitors, chloroquine (CQ) and hydroxychloroquine (HCQ), which block lysosomal acidification and consequently its degradatory potential, have been approved by the FDA, and autophagic targeting has been shown to efficiently augment standard chemotherapy and target therapy [3]."
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"HCQ mainly inhibits lysosomal acidification to impair autophagosome maturation and cargo degradation."
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"Hydroxychloroquine and chloroquine prevents the entry of the virus into host cells by receptor glycosylation, inhibition of proteolysis, decrease acidification of lysosomes, and exert immunomodulatory effects."
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"Hydroxychloroquine inhibits activation of endosomal NA sensors including TLR7 probably by preventing acidification of endosome, which is required for optimal NA recognition by endosomal NA sensors."
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"HCQ like CQ inhibits autophagy by preventing lysosomal acidification and degradation of autophagosome [ 155–157 ]."
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"HCQ inhibits autophagy by preventing acidification of the lysosome, making it unable to attach to and breakdown autophagosomes [XREF_BIBR]."
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"Similarly, chloroquine and hydroxychloroquine effectively inhibit lysosomal acidification by increasing pH inside the lysosome [142, 144] ."
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"Hydroxychloroquine (HCQ) attenuates lysosomal acidification, resulting in obstruction of the activity of the lysosomal degradative enzyme and inhibiting autophagy, but at a high concentration with greater cytotoxicity [31]."
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"Existing treatments already target this pathway; notably, hydroxychloroquine and bafilomycin inhibit endosome acidification and/or maturation, thereby inhibiting both TLR7 and TLR9 signalling 94."
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"HCQ blocks endosomal acidification and inhibits viral uncoating, thereby inhibiting viral proliferation, while lopinavir/r is a protease inhibitor that inhibits enzymes that process 16 nonstructural proteins (NSPs) required for viral replication [4]."
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"8 This suggests that hydroxychloroquine (HCQ), which inhibits endosomal acidification required for optimal TLR signalling 9 and is a medication used by patients with systemic lupus erythematosus (SLE) even during pregnancy, may prevent cardiac injury."
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"Since cathepsin L requires an acidic environment to function and that CQ and HCQ are known to inhibit endosome-lysosomal system acidification, CQ and HCQ efficiently blocked SARS-CoV-2 infection of Vero but failed to block infection of Calu-3 cells."
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"184 Chloroquine (CQ) and hydroxychloroquine (HCQ), autophagy inhibitors, inhibit lysosome acidification and have been demonstrated as regulators of antitumor immunity in pancreatic and colorectal cancers."
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"Therefore, hydroxychloroquine, which inhibits endosomal acidification required for optimal Toll like receptor signaling, is suggested as a preventive medication for fetal cardiac injury in patients with autoimmune disorders [XREF_BIBR XREF_BIBR]."
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"Hydroxychloroquine (HCQ), a lysosomotropic agent, can prevent endosomal acidification and block autophagosome-lysosome fusion."
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"HCQ inhibits autophagy by hampering lysosomal acidification that prevents autophagosomal degradation."
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"It should be noted that HCQ is actually an inhibitor of lysosome acidification, and hence is not specific to the autophagy pathway."
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"8–9 As a late-stage inhibitor of autophagy, HCQ blocks the acidification of the lysosome and prevents fusion with the autophagosome."
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"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]."
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"A study demonstrated that HCQ decreases lysosomal acidification by emancipating chemotherapeutic drugs from the lysosome to the cytoplasm or nucleus, ramifying into intensified cytotoxicity [38,39]."
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"Interestingly, the anti-malarial drugs chloroquine and the related hydroxychloroquine also block ZIKV infection in vivo and prevent acidification of endosomes."
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"XREF_BIBR As described, hydroxychloroquine inhibits acidification of intracellular vesicles, and in vitro studies clearly document the inhibition of IFN production induced by nucleic acid containing immune complexes by chloroquine."
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"To be specific, chloroquine (CQ) and hydroxychloroquine (HCQ) inhibit autophagosome degradation by inhibiting the lysosomal acidification."
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"Notably, hydroxychloroquine is an inhibitor of lysosomal acidification and mostly accumulates in acidic cytoplasmic vesicles."
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"Translational efforts to inhibit autophagy have predominantly focused on an antimalarial drug CQ or HCQ, which blocks lysosome acidification and autophagosome degradation (32)."
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"HCQ is known to inhibit endosomal acidification, which may diminish pDC activation."
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"In glioblastoma cells, HCQ inhibits acidification of lysosomes blocking autophagy [XREF_BIBR]."
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"One example is the endosomal acidification blocker hydroxychloroquine which indeed scored as antiviral in both cell types (9, 23, 24) ."
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"HCQ was believed to prevent lysosomal acidification and therefore prevent the degradation of LC3-II, whereas 3-MA was reported to curb the transformation from LC3-I to LC3-II due to its inhibitory effect on phosphoinositide 3-kinase (PI3K) activity."
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"Chloroquine and hydroxychloroquine are antimalarial drugs and block lysosomal acidification and degradation of autophagosomes, acting as autophagy inhibitors."
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"XREF_BIBR, XREF_BIBR In addition, the widely used antimalarial and anti-inflammatory drugs chloroquine (CQ) and hydroxychloroquine (HCQ), which block lysosomal acidification and degradation, have side effects including retinopathy (bull 's eye maculopathy) and vision loss."
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"Meanwhile, HCQ inhibits autophagy due to lysosomal acidification and blocks the fusion of autophagosomes with lysosomes, triggering the accumulation of autophagosomes [70]."
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"Chloroquine (CQ) and hydroxychloroquine (HCQ), which inhibit the final step of autophagy by preventing lysosomal acidification, have shown promising results in a clinical trial."
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"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."
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"Compounds such as chloroquine and hydroxychloroquine that prevent acidification of the lysosomal compartment are the sole clinically available inhibitors of autophagy."
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"The antimalarial drug hydroxychloroquine inhibits endolysosomal acidification during APCs nuclear particle processing, thereby blocking the adjuvant effect of endogenous nucleic acids by TLRs [ 148 ]."
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"Two inhibitors of autophagy (20 μΜ hydroxychloroquine [HCQ] and 5 mM of 3-methyladenine [3-MA]) were used for 24 hours in CRC cell lines to identify the protein levels of these autophagic markers after inhibition of autophagy in different stages—3-MA inhibits autophagy by blocking autophagosome formation through inhibition of type III phosphatidylinositol 3-kinases and HCQ prevents lysosomal acidification."
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"Also, HCQ is known to impair endosome acidification, and, since multiple TLRs require acidified endosomes for their activation, this effect results in the impairment of TLR-mediated production of cytokines, including TNFα, IL-6, and IFN-γ (Nirk et al., 2020)."
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"HCQ can inhibit lysosomal acidification and prevent the degradation of autophagosomes, thereby suppressing autophagy [XREF_BIBR, XREF_BIBR]."
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"Similar to P9R, well-known anti-malaria drugs chloroquine and hydroxychloroquine can also inhibit endosomal acidification in several viruses including zika virus (Li et al., 2017), enterovirus-A71 (Tan et al., 2018), and SARS-CoV-2 (Liu et al., 2020; Wang et al., 2020)."
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"Hydroxychloroquine impedes lysosomal acidification and autophagy, preventing in-vitro viral entry[106,116]."
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"Importantly, clinical trials have shown that hydroxychloroquine, which inhibits autophagic flux by preventing lysosomal acidification, enhances PDAC patient response to chemotherapy ."
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"Currently, hydroxychloroquine (HCQ), which blocks lysosome acidification and autophagosome degradation, is available as an autophagy inhibitor that will enable assessment of the utility of this approach."
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"The chloroquine derivative hydroxychloroquine (HCQ) inhibits the acidification of lysosomes and shows promising results when combined with gemcitabine."
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"Notably, hydroxychloroquine, recommended for most individuals with lupus, can gently reduce TLR7 activation by inhibiting endosome acidification."
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"Here, we demonstrated that IMP, HCQ, FLV, and FLX reduced lysosomal acidification and subsequent ASM and proteolytic activity within 2 h (Figure 2A–2C)."
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"Two anti-malarial drugs, hydroxychloroquine (HCQ) and chloroquine (CQ), can inhibit lysosomal acidification and prevent the degradation of autophagosomes, thereby suppressing autophagy in Myc driven lymphoma and increasing the antitumor effects of cyclophosphamide XREF_BIBR - XREF_BIBR."
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"Additionally, hydroxychloroquine could inhibit lysosomes’ acidification and interfere with the fusion process of the SARS-CoV-2 with the host cell [54]."
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"Hydroxychloroquine (HCQ) is known to inhibit endosomal acidification which may diminish pDC activation."
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"One example is the endosomal acidification blocker hydroxychloroquine, which indeed scored as an antiviral in both cell types ( de Duve et al., 1974 ; Ducharme and Farinotti, 1996 ; Liu et al., 2020 )[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Chloroquine and hydroxychloroquine prevent the endosomal acidification and fusion in pDCs and also inhibit IDO, a regulator of T-cell responses [XREF_BIBR]."
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"HCQ has been reported to abrogate endosomal TLR (TLR3, TLR7, TLR8, and TLR9) responses by preventing acidification [64] ."
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"Hydroxychloroquine (HCQ), a lysosomal inhibitor, inhibits macropinocytosis by interrupting lysosomal acidification [64]."
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"Hydroxychloroquine (HCQ) inhibits lysosomal acidification and blocks autophagy via influencing autophagosome fusion and degradation."
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"Increasing number of studies have demonstrated that block of autophagy effectively increased the sensitivity of NSCLC cells to cisplatin [5–7], thereby providing a reasonable basis for the combined use of autophagy inhibitors and cisplatin for NSCLS treatment.Currently, chloroquine (CQ) and its derivative hydroxychloroquine (HCQ), which inhibit autophagosome degradation by limiting the acidification of lysosomes, are still the only clinically available autophagy inhibitors [8]."
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"However, chloroquine (CQ) and hydroxychloroquine (HCQ), which disrupt lysosomal acidification and manifest anti-cancer activity in mice (Yang et al., 2011), have not improved overall patient survival when combined with chemotherapy (Karasic et al., 2019)."
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"Hydroxychloroquine (HCQ) blocks autophagy by blunting lysosomal acidification."
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"Chloroquine, hydroxychloroquine, and other lysosome-tropic agents can block lysosome acidification, in turn resulting in disruption in autophagosome degradation [31]."
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"50 For example, chloroquine and hydroxychloroquine, routinely used for the treatment of diverse diseases, inhibit lysosomal acidification and prevent autophagy."
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"HCQ inhibits the endosome acidification and block NA-TLR signaling."
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"Hydroxychloroquine (HCQ) is known to inhibit endosomal acidification which may diminish pDC activation (Kuznik et al., 2011, 9; Sacre et al., 2012) ."
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"These data indicate that autophagy is coupled with melanoma progression, which motivated the search for anti-melanoma therapeutic targets interfering with autophagy.Phase I clinical trials indicated t[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"HCQ abrogates endosomal acidification thereby reducing endosomal TLR activation [XREF_BIBR], but interestingly, enough data confirming this HCQ effect on endosomal TLRs in primary human cells are scarce."
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"Hydroxychloroquine reduces endosomal acidification, SSAA09E2 acts by blocking early interactions of SARS-CoV with its receptor, the angiotensin converting enzyme 2 (ACE2), shared by SARS-CoV-2 and SSAA09E3 prevents fusion of the viral membrane with the host cellular membrane."
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"We treated HEI-OC1 cells with HCQ and trehalose, which inhibited lysosomal acidification and autophagic clearance."
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"Hydroxychloroquine, traditionally used for malaria and autoimmune diseases, inhibits lysosomal acidification, disrupting autophagy and promoting CLL cells (116)."
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"Acidification of lysosomes and function of TLR-7 and TLR-9 are inhibited by hydroxychloroquine, and its activation and release of cytokines is suppressed by prednisone."
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"To further test which pathway is responsible for the decreased LC3-II levels (XREF_FIG), we incubated cells with hydroxychloroquine (CQ), which blocks lysosome acidification and thereby autophagic influx and degradation of LC3-II."
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"IFNalpha production by SLE-IC can be inhibited by blocking FcRgamma mediated uptake of IgG, by hydroxychloroquine, which increases the intracytoplasmic pH and prevents acidification and maturation of endosomes, or by C-reactive protein, which binds apoptotic cells and nucleoprotein auto-antigens."
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"Hydroxychloroquine (HCQ), which inhibits lysosomal acidification, negatively impacts both autophagy and macropinocytosis dependent scavenging and is currently under investigation for its cancer therapeutic potential."
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"In this study, super-resolution structured illumination microscope (SIM) was used to analyze molecular mechanism of endocytic acidification inhibitors in the SARS-CoV-2 pandemic, such as Chloroquine (CQ), Hydroxychloroquine (HCQ) and Bafilomycin A1 (BafA1)."
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