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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors.

Dramatic improvements in mTOR-targeting selectivity were achieved by replacing morpholine in pyrazolopyrimidine inhibitors with bridged morpholines. Analogues with subnanomolar mTOR IC(50) values and up to 26000-fold selectivity versus PI3Kalpha were prepared. Chiral morpholines gave inhibitors whose enantiomers had different selectivity and potency profiles. Molecular modeling suggests that a single amino acid difference between PI3K and mTOR (Phe961Leu) accounts for the profound selectivity seen by creating a deeper pocket in mTOR that can accommodate bridged morpholines.[1]

References

  1. Morpholine derivatives greatly enhance the selectivity of mammalian target of rapamycin (mTOR) inhibitors. Zask, A., Kaplan, J., Verheijen, J.C., Richard, D.J., Curran, K., Brooijmans, N., Bennett, E.M., Toral-Barza, L., Hollander, I., Ayral-Kaloustian, S., Yu, K. J. Med. Chem. (2009) [Pubmed]
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