Chloroquine lysosome inhibitor mechanism

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  1. myominzaw User

    Chloroquine lysosome inhibitor mechanism


    Chloroquine has been extensively used in mass drug administrations, which may have contributed to the emergence and spread of resistance. It is recommended to check if chloroquine is still effective in the region prior to using it.

    Granulomatous nodules treated with plaquenil Chloroquine tablet brand name Plaquenil and alcohol lupus

    General mechanisms of viral inhibition by chloroquine Chloroquine/hydroxychloroquie can impair the replication of several viruses by interacting with the endosome-mediated viral entry or the late stages of replication of enveloped viruses figure 1. These treatments included the use of chloroquine CQ, an inhibitor of the lysosomal pH gradient, and Salicylihalamide A SalA, a selective inhibitor of the v‐ATPase Xie et al, 2004, as well as overexpression of PAT1, an amino acid transporter that causes massive transport of amino acids out of the lysosomal lumen Sagne et al, 2001. Although the precise mechanism underlying the antimalarial effects of chloroquine remains unknown, chloroquine seems to exert its effects through the weak-base lysosome-tropic feature. When chloroquine enters the lysosome, it becomes protonated because of the low pH within the lysosome, and accumulation of the protonated form of chloroquine within the lysosome leads to less acidic conditions and, thereby, decreased lysosomal function.

    The Centers for Disease Control and Prevention recommend against treatment of malaria with chloroquine alone due to more effective combinations. In areas where resistance is present, other antimalarials, such as mefloquine or atovaquone, may be used instead.

    Chloroquine lysosome inhibitor mechanism

    Lysosomal and Proteasomal Degradation Play Distinct Roles in., A lysosome‐to‐nucleus signalling mechanism senses and.

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  5. By inhibiting lysosome function, chloroquine synergistically activated glucocorticoid signaling. Lysosomal inhibition by either bafilomycin A1 an inhibitor of the vacuolar adenosine triphosphatase or knockdown of transcription factor EB TFEB, a master activator of lysosomal biogenesis mimicked the effects of chloroquine. The

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    Mechanism. 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. Chloroquine enters the red blood cell by simple diffusion, inhibiting the parasite cell and digestive vacuole. Chloroquine then becomes protonated to CQ2+, as the digestive vacuole is known to be acidic pH 4.7; chloroquine then cannot leave by diffusion. Chloroquine is a 4-aminoquinoline with antimalarial, anti-inflammatory, and potential chemosensitization and radiosensitization activities. Although the mechanism is not well understood, chloroquine is shown to inhibit the parasitic enzyme heme polymerase that converts the toxic heme into non-toxic hemazoin.

     
  6. dimitrus Guest

    Hydroxychloroquine is used to treat or prevent malaria, a disease caused by parasites that enter the body through the bite of a mosquito. Hydroxychloroquine MotherToBaby Plaquenil Uses, Dosage & Side Effects - Medications That Can Interfere With Birth Control Pills
     
  7. leos_ru User

    Hydroxychloroquine-related retinal toxicity Rheumatology. HCQ is used mainly in RA and SLE. Most of its benefits have been well described elsewhere, mainly in the context of lupus reduction of flares and damage, enhancement of MMF response, improvement of survival, and reduced risk of seizures and thromboses 9–15.

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