IndraLab

Statements


Amodiaquine inhibits PfPMT. 10 / 10
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"Here we provide biochemical and biophysical data indicating that PfPMT activity is inhibited by amodiaquine (AQ)."

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"Taken together, the effect on enzymatic activity, lack of binding in ITC experiments, and docking studies suggest that amodiaquine and other commonly used aminoquinolines weakly inhibit PfPMT."

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"In contrast to a previous report 17, amodiaquine was a weak inhibitor of PfPMT (IC 50 = 1.35 mM)."

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"To better characterize inhibition of PfPMT by amodiaquine, we determined the IC 50 values of a series o aminoquinolines using a direct radiochemical assay."

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"The poor inhibition of PfPMT by amodiaquine was comparable to the ~ 3 mM IC 50 values determined for the two PMT from the nematode parasite Haemonchus contortus 12."

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"Interestingly, PfPMT activity was not inhibited by the amodiaquine analog, chloroquine, or other aminoquinolines, amino alcohols, or histamine methyltransferase inhibitors."

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"Inhibition of PfPMT activity by amodiaquine in vitro and in yeast."

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"To better characterize inhibition of PfPMT by amodiaquine, we determined the IC (50) values of a series of aminoquinolines using a direct radiochemical assay."

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"Previous studies have also shown that PfPMT activity is inhibited by the 4-aminoquinoline compounds, amodiaquine (AQ) and chloroquine (CQ) with strong inhibition obtained with AQ."

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"To better understand amodiaquine inhibition of PfPMT, we determined the x-ray crystal structure of the enzyme in complex with S-adenosylhomocysteine (SAH) and amodiaquine 18."