Pyranonaphthoquinone lactones: a new class of AKT selective kinase inhibitors alkylate a regulatory loop cysteine.

@article{Salaski2009PyranonaphthoquinoneLA,
  title={Pyranonaphthoquinone lactones: a new class of AKT selective kinase inhibitors alkylate a regulatory loop cysteine.},
  author={Edward J Salaski and Girija Krishnamurthy and W Ding and Ker Yu and Shabana S Insaf and Clark N Eid and Jaechul Shim and Jeremy I. Levin and Keiko Tabei and Lourdes Toral-Barza and Weiguo Zhang and Leonard A. McDonald and Erick E Honores and Cilien Hanna and Ayako Yamashita and Bernard D Johnson and Zhongqiao Li and Leif M Laakso and Dennis W Powell and Tarek S. Mansour},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 8},
  pages={2181-4}
}
The naturally occurring pyranonaphthoquinone (PNQ) antibiotic lactoquinomycin and related aglycones were found to be selective inhibitors of the serine-threonine kinase AKT. A set of synthetic PNQs were prepared and a minimum active feature set and preliminary SAR were determined. PNQ lactones inhibit the proliferation of human tumor cell lines containing constitutively activated AKT and show expected effects on cellular biomarkers. Biochemical data are presented supporting a proposed… CONTINUE READING

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