Pyrantel pamoate demonstrates diverse bioactivities, functioning as both an inhibitor and an activator across various biological pathways and processes. It is a potent inhibitor of Human Galactosidase (GALK) and HSD17B4 with potencies of 42,128.5 nM and 31,622.8 nM, respectively. It inhibits Tau Fibril Formation with potencies of 15,848.9 nM and 14,125.4 nM via fluorescence polarization and Thioflavin T Binding, respectively. It shows inhibition of 15-hLO and 15-hLO-2 with potencies ranging from 25,059.4 nM to 31,622.8 nM, and inhibits Menin-MLL interaction in MLL-related leukemias at 14,125.4 nM. It is also an inhibitor of Fructose-1,6-bisphosphate Aldolase from Giardia Lamblia at 25,059.4 nM potency.
Additionally, Pyrantel pamoate acts as an activator and substrate of Cytochrome P450 3A4 at 25,118.9 nM potency. It inhibits the vitamin D receptor (VDR), Polymerase Kappa, and USP1/UAF1, with respective potencies of 35,481.3 nM, 31,622.8 nM, and 50,118.7 nM.
In terms of antiparasitic activity, Pyrantel pamoate acts effectively against Ancylostoma caninum isolates NT and PR, with an EC50 of 217,200.0 nM for isolate NT and 681,300.0 nM for isolate PR, and exhibits notable larval arrested morphology effects.
Moreover, the compound inhibits sodium fluorescein uptake in OATP1B1 and OATP1B3-transfected CHO cells, with inhibition percentages of 31.41% and 34.84% at 10 µM concentration. It also displays antiviral activity against SARS-CoV-2 by inhibiting cytotoxicity in Caco-2 and VERO-6 cells, with an inhibition of -1.07% in Caco-2 cells and -0.17% in VERO-6 cells at 10 µM concentration. Furthermore, it inhibits SARS-CoV-2 3CL-Pro protease activity by 16.14% at 20 µM.
Overall, Pyrantel pamoate shows potential as a multi-faceted therapeutic agent with activities spanning from enzyme inhibition and receptor modulation to antiparasitic and antiviral effects..
Note: Summary generated by AI. Data source: ChEMBL 