Possible Interaction: Chloroquine and Leucine

“ Chloroquine … leucine appearance, a measure of whole body proteolysis, from 2.45 +/- 0.08 to 2.19 +/- 0.08 mumol.kg-1.min-1 (P = 0.… of whole body protein synthesis, from 2.16 +/- 0.08 to 1.95 +/- 0.06 mumol.kg-1.min-1 (P = 0.050).”

“ CQ treatment significantly decreased the activities of cathepsins D, B and L , and the inhibition of cathepsins B and L mimicked the effect of CQ and increased tau levels in cells.”

“INCUBATION of cultured hippocampal slices with chloroquine , a compound that increases the pH of acidic subcellular organelles, for 1 0 h reduced the activity of cathepsin L by 8 3 ± 0.87% (mea n ± s.e.m.)”

“It was shown that in vitro chloroquine reversibly inhibited purified cathepsins H, B, L in concentrations less than those observed inside lysosomes in vivo.”

“Suramine inhibited pure preparations of cathepsin B and L, while chloroquine inhibited cathepsins B, L and H. The inhibitors were effective in vitro at lower concentrations as compared with these administered in vivo.”

“ Leucine accumulation by the intact cells is 80% inhibited by 0.1 mM chloroquine and 50% inhibited by 20 mM NH4Cl and methylamine, lysosomotropic agents that elevate the intralysosomal pH. These observations suggest that the azurophilic granules of these cells, generally considered to be primary lysosomes, are internally acidified.”

“ Chloroquine in dose-dependent fashion partially inhibited basal [3H]leucine incorporation into acinar cell protein, but in contrast to its effects on 2-deoxy-D-glucose uptake, the drug had no effects on the stimulation of this function by insulin.”

“ Leucine accumulation was inhibited by submillimolar concentrations of chloroquine , by the protease inhibitor L-1-tosylamido-2-phenylethyl chloromethyl ketone, and by lowering the pH below 7.0.”

“In contrast, in C2C12 cells, 1 mM leucine increased mTORC1 and S6K1 phosphorylation ( P < 0.05), which was inhibited by 2 mg/ml chloroquine.”

“The uptake of sorbitol and coproporphyrin was slightly stimulated, while the uptake of 6-deoxyglucose was slightly, that of 2-aminoisobutyric acid and leucine strongly inhibited by chloroquine.”