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VX680

Known as: VX-680, MK-0457, MK0457 
National Institutes of Health

Related topics

Related topics

4 relations

Broader (2)

Aurora kinase inhibitor MK-0457Piperazines

Narrower (2)

TozasertibVE 465

Papers overview

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Highly Cited
2011
Highly Cited
2011
Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase.
The inhibition of Aurora kinases in order to arrest mitosis and subsequently inhibit tumor growth via apoptosis of proliferating… 
Highly Cited
2011
Highly Cited
2011
Combining histone deacetylase inhibitor vorinostat with aurora kinase inhibitors enhances lymphoma cell killing with repression of c-Myc, hTERT, and microRNA levels.
MK-0457 and MK-5108 are novel aurora kinase inhibitors (AKi) leading to G(2)-M cell-cycle arrest. Growth and survival of multiple… 
2011
2011
An Integrated Chemical Biology Approach Identifies Specific Vulnerability of Ewing's Sarcoma to Combined Inhibition of Aurora Kinases A and B
Ewing's sarcoma is a pediatric cancer of the bone that is characterized by the expression of the chimeric transcription factor… 
Highly Cited
2010
Highly Cited
2010
Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237.
The Aurora kinases regulate multiple aspects of mitotic progression, and their overexpression in diverse tumor types makes them… 
Review
2009
Review
2009
Dasatinib in chronic myeloid leukemia: a review
Deregulated BCR-ABL tyrosine kinase (TK) activity is the molecular marker for chronic myeloid leukemia (CML), which provides an… 
Highly Cited
2008
Highly Cited
2008
Aurora A Is Essential for Early Embryonic Development and Tumor Suppression*
Aurora A is a serine/threonine kinase that functions in various stages of mitosis. Accumulating evidence has demonstrated that… 
Highly Cited
2007
Highly Cited
2007
MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation.
MK-0457 (VX-680) is a small-molecule aurora kinase (AK) inhibitor with preclinical antileukemia activity. The T315I BCR-ABL… 
Highly Cited
2007
Highly Cited
2007
Structural basis for potent inhibition of the Aurora kinases and a T315I multi-drug resistant mutant form of Abl kinase by VX-680.
Review
2007
Review
2007
The Bcr-Abl tyrosine kinase inhibitor imatinib and promising new agents against Philadelphia chromosome-positive leukemias
Chronic myeloid leukemia (CML) was the first human malignant disease to be linked to a single, acquired genetic abnormality… 
Highly Cited
2006
Highly Cited
2006
Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680.
We present a high-resolution (2.0 A) crystal structure of the catalytic domain of a mutant form of the Abl tyrosine kinase (H396P… 
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