PIK-93是第一个报道的PI 4-激酶抑制剂，能够在低纳摩尔范围内抑制PI 4 KIII 2（IC 50 =19 nM）。此外，该化合物在体外是PI 3 K β 3的有效抑制剂（IC 50 =16 nM）。该化合物抑制p110 β ± p110 β ² p110 β ′，IC 50分别为0.039 0.59 0.12 µM。PIK-93与Val 882的骨架酰胺和羰基以及其磺酰胺和Asp 964之间形成氢键。PI 4KIII 2对许多恶性疟原虫病毒的复制至关重要。抑制疟原虫的PI 4KIIIII 2被认为是一种抗疟疾的治疗方法。参考资料由Bioz提供技术支持更多详情请访问BiozJ. E. Burke et al.“Structures of PI4KIIIb complex show simultaneous recruitment of Rab11 and its effectors”Science 344 1035（2014）; DOI：10.1126/science.1253397
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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 Powered by Bioz See more details on BiozJ.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
