8 research outputs found
Discovery of a Potent and Orally Bioavailable Benzolactam-Derived Inhibitor of Polo-Like Kinase 1 (MLN0905)
No full textThis article describes the discovery of a series of potent
inhibitors
of Polo-like kinase 1 (PLK1). Optimization of this benzolactam-derived
chemical series produced an orally bioavailable inhibitor of PLK1
(<b>12c</b>, MLN0905). In vivo pharmacokinetic–pharmacodynamic
experiments demonstrated prolonged mitotic arrest after oral administration
of <b>12c</b> to tumor bearing nude mice. A subsequent efficacy
study in nude mice achieved tumor growth inhibition or regression
in a human colon tumor (HT29) xenograft model
Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S β5-subunit
No full textManaging Alone: Barack Obama, Organizing for Action, and Policy Advocacy in the Digital Era
No full text
