Published in J Med Chem on August 30, 2012
Insights into Aurora-A kinase activation using unnatural amino acids incorporated by chemical modification. ACS Chem Biol (2013) 0.97
Dual Aurora A and JAK2 kinase blockade effectively suppresses malignant transformation. Oncotarget (2014) 0.88
Molecular features of product release for the PKA catalytic cycle. Biochemistry (2014) 0.84
Development of novel ACK1/TNK2 inhibitors using a fragment-based approach. J Med Chem (2015) 0.82
Issues in interpreting the in vivo activity of Aurora-A. Expert Opin Ther Targets (2014) 0.80
A water-mediated allosteric network governs activation of Aurora kinase A. Nat Chem Biol (2017) 0.75
2-Chloro-5-fluoro-6-methyl-N-o-tolyl-pyrimidin-4-amine. Acta Crystallogr Sect E Struct Rep Online (2013) 0.75
Structural insights into the polypharmacological activity of quercetin on serine/threonine kinases. Drug Des Devel Ther (2016) 0.75
Discovery of a Diaminopyrimidine FLT3 Inhibitor Active against Acute Myeloid Leukemia. ACS Omega (2017) 0.75
Dynamic Equilibrium of the Aurora-A Kinase Activation Loop Revealed by Single Molecule Spectroscopy. Angew Chem Int Ed Engl (2017) 0.75
Coot: model-building tools for molecular graphics. Acta Crystallogr D Biol Crystallogr (2004) 227.01
The CCP4 suite: programs for protein crystallography. Acta Crystallogr D Biol Crystallogr (1994) 187.88
Crystallography & NMR system: A new software suite for macromolecular structure determination. Acta Crystallogr D Biol Crystallogr (1998) 169.28
Targeting cancer with small molecule kinase inhibitors. Nat Rev Cancer (2009) 9.26
The nuts and bolts of AGC protein kinases. Nat Rev Mol Cell Biol (2010) 6.91
VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. Nat Med (2004) 6.40
Aurora-A - a guardian of poles. Nat Rev Cancer (2005) 4.11
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. Nat Biotechnol (2011) 3.72
Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase. Proc Natl Acad Sci U S A (2007) 3.27
Aurora-kinase inhibitors as anticancer agents. Nat Rev Cancer (2004) 3.19
The Aurora kinase family in cell division and cancer. Biochim Biophys Acta (2008) 2.84
Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition. J Med Chem (2005) 2.38
Characterization of Alisertib (MLN8237), an investigational small-molecule inhibitor of aurora A kinase using novel in vivo pharmacodynamic assays. Clin Cancer Res (2011) 2.35
Validating Aurora B as an anti-cancer drug target. J Cell Sci (2006) 2.30
AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis. Clin Cancer Res (2007) 2.16
A novel Aurora-A kinase inhibitor MLN8237 induces cytotoxicity and cell-cycle arrest in multiple myeloma. Blood (2010) 2.08
Aurora kinase inhibitors--rising stars in cancer therapeutics? Mol Cancer Ther (2010) 1.91
5-Substituted-1H-tetrazoles as carboxylic acid isosteres: medicinal chemistry and synthetic methods. Bioorg Med Chem (2002) 1.86
Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase. J Med Chem (2007) 1.81
The Aurora kinase inhibitor VX-680 induces endoreduplication and apoptosis preferentially in cells with compromised p53-dependent postmitotic checkpoint function. Cancer Res (2006) 1.69
PHA-680632, a novel Aurora kinase inhibitor with potent antitumoral activity. Clin Cancer Res (2006) 1.61
MK-5108, a highly selective Aurora-A kinase inhibitor, shows antitumor activity alone and in combination with docetaxel. Mol Cancer Ther (2010) 1.48
Discovery and development of aurora kinase inhibitors as anticancer agents. J Med Chem (2009) 1.45
Drug-resistant aurora A mutants for cellular target validation of the small molecule kinase inhibitors MLN8054 and MLN8237. ACS Chem Biol (2010) 1.43
Crystal structure of an Aurora-A mutant that mimics Aurora-B bound to MLN8054: insights into selectivity and drug design. Biochem J (2010) 1.38
Clinical experience with aurora kinase inhibitors: a review. Oncologist (2009) 1.31
Aurora A is a negative prognostic factor and a new therapeutic target in human neuroblastoma. Mol Cancer Ther (2009) 1.22
1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. J Med Chem (2006) 1.22
The Akt activation inhibitor TCN-P inhibits Akt phosphorylation by binding to the PH domain of Akt and blocking its recruitment to the plasma membrane. Cell Death Differ (2010) 1.20
Update on Aurora Kinase Targeted Therapeutics in Oncology. Expert Opin Drug Discov (2011) 1.19
Aurora A selective inhibitor MLN8237 suppresses the growth and survival of HTLV-1-infected T-cells in vitro. Cancer Sci (2010) 1.17
Aurora kinase inhibitors in preclinical and clinical testing. Expert Opin Investig Drugs (2009) 1.16
Mitotic drivers--inhibitors of the Aurora B Kinase. Cancer Metastasis Rev (2009) 1.14
High-throughput screening with quantitation of ATP consumption: a universal non-radioisotope, homogeneous assay for protein kinase. Assay Drug Dev Technol (2004) 1.12
Crystal structures of the FAK kinase in complex with TAE226 and related bis-anilino pyrimidine inhibitors reveal a helical DFG conformation. PLoS One (2008) 1.11
The Aurora-A/TPX2 complex: a novel oncogenic holoenzyme? Biochim Biophys Acta (2010) 1.10
A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B. J Med Chem (2009) 1.09
Small molecule aurora kinases inhibitors. Curr Med Chem (2009) 1.06
A generic, homogenous method for measuring kinase and inhibitor activity via adenosine 5'-diphosphate accumulation. J Biomol Screen (2006) 1.05
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 2: identification and optimisation of substituted 2,4-bis anilino pyrimidines. Bioorg Med Chem Lett (2003) 1.05
Aurora kinase inhibitors as anti-cancer therapy. Anticancer Drugs (2010) 1.04
The discovery of the potent aurora inhibitor MK-0457 (VX-680). Bioorg Med Chem Lett (2009) 1.04
The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: a new class of Aurora-A kinase inhibitors. Bioorg Med Chem Lett (2006) 1.03
A novel mechanism by which small molecule inhibitors induce the DFG flip in Aurora A. ACS Chem Biol (2012) 0.98
Physiological and oncogenic Aurora-A pathway. Int J Biol Sci (2009) 0.97
Aurora B: a new prognostic marker and therapeutic target in cancer. Curr Med Chem (2011) 0.97
Aurora kinase inhibitor patents and agents in clinical testing: an update (2009-10). Expert Opin Ther Pat (2011) 0.96
Inhibitors of the tyrosine kinase EphB4. Part 4: Discovery and optimization of a benzylic alcohol series. Bioorg Med Chem Lett (2011) 0.94
Exploration of secondary and tertiary pharmacophores in unsymmetrical N,N'-diaryl urea inhibitors of soluble epoxide hydrolase. Bioorg Med Chem Lett (2010) 0.92
Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. J Med Chem (2010) 0.92
Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies. Bioorg Med Chem Lett (2006) 0.92
Phase I assessment of new mechanism-based pharmacodynamic biomarkers for MLN8054, a small-molecule inhibitor of Aurora A kinase. Cancer Res (2010) 0.92
Inhibitors of the tyrosine kinase EphB4. Part 2: structure-based discovery and optimisation of 3,5-bis substituted anilinopyrimidines. Bioorg Med Chem Lett (2008) 0.90
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines. Bioorg Med Chem Lett (2003) 0.89
Testing the promiscuity of commercial kinase inhibitors against the AGC kinase group using a split-luciferase screen. J Med Chem (2012) 0.87
Aurora kinase inhibitors: a new class of drugs targeting the regulatory mitotic system. Clin Transl Oncol (2009) 0.86
Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core. ACS Med Chem Lett (2010) 0.84
Identification, SAR studies, and X-ray co-crystallographic analysis of a novel furanopyrimidine aurora kinase A inhibitor. ChemMedChem (2010) 0.83
Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors. Bioorg Med Chem Lett (2010) 0.83
Aurora-B kinase inhibitors for cancer chemotherapy. Mini Rev Med Chem (2008) 0.82
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor. J Med Chem (2010) 0.82
Aurora-A kinase: a novel target both for cellular immunotherapy and molecular target therapy against human leukemia. Expert Opin Ther Targets (2009) 0.81
Structural basis for the inhibition of Aurora A kinase by a novel class of high affinity disubstituted pyrimidine inhibitors. Bioorg Med Chem Lett (2006) 0.79
Aurora A and B kinases--targets of novel anticancer drugs. Recent Pat Anticancer Drug Discov (2010) 0.79
Shining the light on aurora-a kinase as a drug target in pancreatic cancer. Mol Cancer Ther (2011) 0.78
Identification of small molecules that inhibit GSK-3beta through virtual screening. Bioorg Med Chem Lett (2008) 0.78