Thursday, March 27, 2014
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Rational design platform to
generate dual-acting kinase and bromodomain inhibitors
In vitro studies suggest dual-acting kinase and bromodomain
inhibitors can be rationally designed to treat cancer and inflammatory
disease. In vitro, 9 of 628 structurally diverse kinase inhibitors
potently inhibited bromodomain
containing 4 (BRD4).
In cultured multiple myeloma (MM) cells, two dual-acting kinase inhibitors
suppressed expression of c-Myc
marker of BRD4 inhibition-whereas compounds that blocked the same kinase
targets without inhibiting BRD4 did not. Structural studies suggested
pharmacophores for the kinase and bromodomain inhibitory activities
overlapped but had distinct features, so the activities could be
independently optimized. Next steps include synthesizing inhibitors with
potency optimized for both target classes.
Published online March 27, 2014
licensing status not applicable
Ciceri, P. et al. Nat.
Chem. Biol.; published online March 2, 2014;
Contact: Stefan Knapp, University of Oxford, Oxford, U.K.
Contact: Daniel K. Treiber,
Corp., San Diego, Calif.
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