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MLN8054

National Institutes of Health

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Benzazepines

Papers overview

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2016
2016
Phase I pharmacokinetic (PK) and pharmacodynamic (PD) study of the selective aurora A kinase (AAK) inhibitor MLN8054 in patients (pts) with advanced solid tumors.
2578 Background: MLN8054, a first-generation, selective AAK inhibitor, induces chromosome alignment and segregation defects… 
2012
2012
Molecular dynamics and free energy studies on Aurora kinase A and its mutant bound with MLN8054: insight into molecular mechanism of subtype selectivity.
Because of the high conservation of ATP-binding sites in kinases, the quest for selective kinase inhibitors has been increasingly… 
2012
2012
Combined inhibition of cellular pathways as a future therapeutic option in fatal anaplastic thyroid cancer
Conventional treatment by surgery, radioiodine, and thyroxin-suppressive therapy often fails to cure anaplastic thyroid cancer… 
2011
2011
Phase I assessment of new mechanism-based pharmacodynamic biomarkers for MLN8054, a small-molecule inhibitor of Aurora A kinase.
The mitotic kinase Aurora A is an important therapeutic target for cancer therapy. This study evaluated new mechanism-based… 
2011
2011
MLN8054, a small molecule inhibitor of aurora kinase a, sensitizes androgen-resistant prostate cancer to radiation.
2010
2010
Abstract 1398: Aurora kinase A inhibition with MLN8054 radiosensitizes prostate cancer by inducing cell cycle arrest leading to increased prolonged DNA damage and apoptosis
The purpose of this study is to investigate a potential new radioenhancer for the treatment of prostate cancer. Despite multiple… 
2008
2008
281 POSTER Phase I and pharmacokinetic study of MLN8054, a selective inhibitor of Aurora A kinase
2007
2007
Phase I clinical trial of MLN8054, a selective inhibitor of Aurora A kinase
3577 Background: MLN8054 is a small molecule inhibitor of Aurora A kinase, with > 150-fold greater potency against this enzyme… 
2006
2006
Preclinical pharmacodynamic studies of Aurora A inhibition by MLN8054.
13059 Background: The mitotic kinase Aurora A is implicated in the development of multiple tumor types. MLN8054 is an oral… 
2006
2006
MLN8054, an orally active Aurora A kinase small molecule inhibitor in phase I clinical trials
4724 The Aurora family of mitotic kinases play key roles in proper cell cycle progression. Aurora A and Aurora B are… 
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