PIK-93 is the first reported PI4-kinase inhibitor, which is able to inhibit PI4KIIIβ at low-nanomolar range (IC50=19 nM). In addition, this compound is a potent inhibitor of PI3Kγ in vitro (IC50=16 nM). This compound inhibits p110α, p110β, p110δ with IC50’s of 0.039, 0.59, 0.12 µM respectively. PIK-93 hydrogen bonds to the backbone amide and carbonyl of Val882 and between its sulphonamide and Asp964. PI4KIIIβ is essential for replication of numerous viruses P. falciparum. Inhibition of plasmodial PI4KIIIβ has been proposed as an anti-malaria treatment.

References

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J.E. Burke, et al. “Structures of PI4KIIIb complexes show simultaneous recruitment of Rab11 and its effectors” Science, 344, 1035 (2014);, DOI: 10.1126/science.1253397

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