IndraLab

Statements

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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."
35552447
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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 is known to inhibit endosomal acidification, which may diminish pDC activation."
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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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"Hydroxychloroquine (HCQ) inhibits lysosomal acidification and blocks autophagy via influencing autophagosome fusion and degradation."
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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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"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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"Similarly, chloroquine and hydroxychloroquine effectively inhibit lysosomal acidification by increasing pH inside the lysosome [142, 144] ."
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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) ."
| DOI
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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."
20202598
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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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"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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"Notably, hydroxychloroquine, recommended for most individuals with lupus, can gently reduce TLR7 activation by inhibiting endosome acidification."
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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 Wang et al., 2020) ."
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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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"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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"HCQ inhibits the endosome acidification and block NA-TLR signaling."
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"HCQ mainly inhibits lysosomal acidification to impair autophagosome maturation and cargo degradation."
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"HCQ inhibition of endosome acidification also affects antigen processing and presentation, which, in turn, alters both T‐cell and B‐cell responses."
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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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"Cette thérapie CQ/HCQ doit suivre un algorithme précis destiné à réduire les effets indésirables liés aux médications.Chloroquine (CQ) and its derivative, hydroxychloroquine (HCQ), are known to prevent acidification of lysosomes, resulting in the inhibition of endocytic vesicle fusion."
| PMC
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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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"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."
| DOI
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"Hydroxychloroquine (HCQ), a lysosomotropic agent, can prevent endosomal acidification and block autophagosome-lysosome fusion."
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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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"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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"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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"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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"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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"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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"The chloroquine derivative hydroxychloroquine (HCQ) inhibits the acidification of lysosomes and shows promising results when combined with gemcitabine."
27537393
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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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"Chloroquine and hydroxychloroquine are antimalarial drugs and block lysosomal acidification and degradation of autophagosomes, acting as autophagy inhibitors."
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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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"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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"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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"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.35-37 Antiviral acts on 3C protease, S protein and ACE2, and RNA polymerase and inhibits membrane fusion.3,38 Monoclonal antibodies act by inhibiting IL-6 and thereby reducing cytochrome storm.22 Convalescent plasma obtained from patients who have recovered from COVID-19 patients and developed humoral immunity against the virus, contains neutralizing antibodies in large quantities of."
33384519
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"In glioblastoma cells, HCQ inhibits acidification of lysosomes blocking autophagy [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 (HCQ) is known to inhibit endosomal acidification which may diminish pDC activation."
33442685
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"Chloroquine (CQ) and its derivative, hydroxychloroquine (HCQ), are known to prevent acidification of lysosomes, resulting in the inhibition of endocytic vesicle fusion."
| PMC
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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."
29348606
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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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"Hydroxychloroquine impedes lysosomal acidification and autophagy, preventing in-vitro viral entry[106,116]."
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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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"One example is the endosomal acidification blocker hydroxychloroquine which indeed scored as antiviral in both cell types (9, 23, 24) ."
| DOI
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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 inhibits autophagy by preventing acidification of the lysosome, making it unable to attach to and breakdown autophagosomes [XREF_BIBR]."
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"Furthermore, preventing the acidification of lysosomes, hydroxychloroquine impairs cellular autophagy, a critical step for innate and adaptive immunity activation [132] ."
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"HCQ inhibits autophagy by hampering lysosomal acidification that prevents autophagosomal degradation."
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"HCQ increases lysosome pH due to the accumulation of its protonated form in lysosomes [28] while Baf-A1, an inhibitor of vacuolar-type proton-ATPase (V-ATPase) also known as the vacuolar proton pump [30] , prevents the luminal acidification of lysosomes."
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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 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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"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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