Lysosomal inhibitor chloroquine

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  1. shine New Member

    Lysosomal inhibitor chloroquine


    In MDA-MB-231 cells, immunolocalization and brefeldin A protein transport blocking studies revealed that there was a propensity for newly synthesized Cx43 to be transported to lysosomes. On the other hand, light and electron microscopic analysis of BICR-M1R cells showed that Cx43 gap junctions were prevalent with a subpopulation of intracellular Cx43 localized to lysosomes.

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    Cell surface BMPR-II is susceptible to lysosomal degradation. Chloroquine is an inhibitor of autophagy and inhibits autolysosomal degradation pathways. Chloroquine and methylamine, which accumulate in lysosomes by virtue of their weak base properties, inhibited hepatocytic protein degradation to the same extent as ammonia, with no additivity. Chloroquine accumulates inside the acidic parts of the cell lysosomes and raises their pH, that way it inhibits autophagosome-lysosome fusion and degradation.

    Interestingly, lactacystin inhibition of proteosomal degradation in MDA-MB-231 cells resulted in a marked increase in phosphorylated Cx43 at the expense of non-phosphorylated Cx43, and this change corresponded with an increase in “oversized” gap junction plaques. In both cell types, Western blots revealed a notable increase in total cellular Cx43 in response to lysosome inhibitors.

    Lysosomal inhibitor chloroquine

    Inhibition of endo-lysosomal function exacerbates vascular., Inhibition of the Lysosomal Pathway of Protein Degradation

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  3. Nov 15, 2015 Endosomal Acidification Inhibitor Chloroquine is a lysosomotropic agent that prevents endosomal acidification 1. It accumulates inside the acidic parts of the cell, including endosomes and lysosomes. This accumulation leads to inhibition of lysosomal enzymes that require an acidic pH, and prevents fusion of endosomes and lysosomes.

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    Dec 02, 2016 In this study, we aimed to investigate the influence of lysosomotropic agent, chloroquine, on the efficacy of obinutuzumab-mediated cytotoxicity. As PCD is dependent on lysosomal destabilization, we hypothesized that combination of obinutuzumab with lysosome-destabilizing agent would result in increased cell death. Sep 15, 2013 Chloroquine is a lysosomotropic agent as it is usually prepared as a diprotic weak base pKa 8.5. The unprotonated form of chloroquine preferentially accumulates in lysosomes as it rapidly diffuses across cell/organelle membranes. Chloroquine is a weak base with hydrophobic characteristics that diffuses into lysosomes, where it becomes protonated and trapped, thus leading to a rise in lysosomal pH. These lysosomes can no longer fuse with autophagosomes, thus blocking autophagy. Other, more potent lysosomal inhibitors 12, 13 are also under

     
  4. medisto XenForo Moderator

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  5. lagunaclub Well-Known Member

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