IndraLab

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"These include chloroquine [6], which in addition to its weak-base lysosomotropism also inhibits cathepsin B directly [12]; the microtubule poisons vinblastine and colchicine [13], which presumably blo[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"Chloroquine or hydroxy-chloroquine are already used against COVID-19, inhibiting the activity of CTSB/CTSL non-specifically [79]."

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"As the NLRP3 inflammasome can be activated due to lysosomal damage and release of cathepsin B, ammonium chloride (NH 4 Cl) and chloroquine diphosphate (CQ), which inhibit endosomal-lysosomal system acidification, and CA-074-Me, which acts as a cell-permeable inhibitor of thiol proteases, were used to block lysosomal acidification and cathepsin B activity, respectively."

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"The weak base chloroquine accumulates within acidic intracellular compartments, raises their pH, and can inhibit proteolysis as well as cathepsin B."

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"In addition, chloroquine has been shown to inhibit specifically cathepsin B1 (10), a lysosomal protease capable of degrading collagen (18)."

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"Assessment of the effect of protease inhibitors on the capacity of MCF-7 cells to incorporate [3 H] E 2 confirmed our enzyme immunological data : four lysosomal inhibitors (i.e. chloroquine, NH 4 Cl, [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"

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"It is known that addition of chloroquine to lysosomes in vitro causes inhibition of lysosomal cathepsin B [15] and release of the enzyme (s) into the medium [16]."

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"CQ, monodesthyl chloroquine (mdCQ), amodiaquine (AQ), mdAQ, MF, and quinacrine inhibited cathepsin B in vitro."

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"In addition, chloroquine inhibits the lysosomal protease cathepsin B [8]."

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"Chloroquine, at concentrations attained inside the lysosomes, inhibited cathepsin B 1 but not cathepsin D."

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"Chloroquine inhibits cathepsin B and the intralysosomal chloroqine concentration of 50~100 PM attained in cultured fibroblasts could be sufficient to inhibit cathepsin B by 99% (Wibo and Poole, 1974)."

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"Inhibition of serine and cysteine proteases, including cathepsins, with leupeptin increases tau secretion (Mohamed et al., 2014), while chloroquine treatment, which inhibits CTSB, CTSD, and CTSL, increases tau accumulation (Hamano et al., 2008), providing additional evidence that cathepsins play an important role in the degradation and clearance of tau."

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"At high concentrations, chloroquine also directly inhibits the proteolytic activity of the cysteine endoprotease cathepsin B (Wibo and Poole, 1974)."