Small molecule inhibitor of aurora kinases. Medical search. Frequent questions

The inhibition of Aurora kinases in order to arrest mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells has generated significant discussion within the literature. (rcsb.org)
Analysis of DNA content and indirect immunofluoresence demonstrates that SNS-314 induces defects in cytokinesis and spindle checkpoint that are consistent with Aurora kinase inhibition. (cogershop.com)
Analysis of SNS-314 treated tumors confirms that the anti-tumor activity is consistent with Aurora kinase inhibition. (cogershop.com)
Auora kinase inhibitor MLN8054 binds to and inhibits Aurora kinase A, resulting in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregration, and inhibition of cell proliferation. (xcessbio.com)
40-fold more selective inhibitory activity for Aurora A compared with Aurora B. In vitro, MLN8054 exhibits the activity of growth inhibition across various cell lines from diverse tissue origins with IC50 values ranging from 0.11 μM to 1.43 μM. (xcessbio.com)
Combined Aurora kinase and EGFR targeting using a monoclonal anti-EGFR antibody was more effective compared to single EGFR and Aurora kinase inhibition. (oncotarget.com)

Puma Biotechnology, Inc. a biopharmaceutical company, announced an agreement with Takeda to license the worldwide research and development and commercial rights to alisertib, a selective, small-molecule, orally administered inhibitor of aurora kinase A. Alisertib is an adenosine triphosphate-competitive and reversible inhibitor of aurora kinase A and results in disruption of mitosis leading to apoptosis of rapidly proliferating tumor cells that are dependent on aurora kinase A. Alisertib h. (biotechnology.report)
Aurora A and B are essential in mitosis. (cogershop.com)
however, Aurora C can complement Aurora B kinase activity in mitosis. (cogershop.com)
Aurora A localizes in mitosis to the spindle poles and to spindle microtubules and is thought to regulate spindle assembly. (xcessbio.com)
Aurora kinase C is a chromosomal passenger protein that interacts with aurora kinase B in the regulation of MITOSIS. (lookformedical.com)
A family of highly conserved serine-threonine kinases that are involved in the regulation of MITOSIS. (lookformedical.com)
An aurora kinase that localizes to the CENTROSOME during MITOSIS and is involved in centrosome regulation and formation of the MITOTIC SPINDLE. (lookformedical.com)
An aurora kinase that is a component of the chromosomal passenger protein complex and is involved in the regulation of MITOSIS. (lookformedical.com)
Contrary to cells treated with a siRNA, cells treated with siRNAs against Bora often displayed multipolar spindles in mitosis, a phenotype that is also seen upon TPX2 RNAi Geneticin distributor and after injection of antibodies blocking Aurora A function. (others-signal.com)
Aurora A is involved with centrosome readiness, spindle assembly, and uneven protein localization throughout mitosis. (others-signal.com)
Mitosis is usually a dynamic process controlled by the activity of multiple kinases with attendant modification of proteins facilitating rigid checkpoint control. (ap26113.com)
GSK1904529A Aurora A is found at centrosomes in early mitosis and controls centrosome maturation centriole separation and chromosome alignment (33) whereas accurate targeting of Aurora B to the chromosomes and then to the spindle midzone and midbody is essential for maintaining microtubule/kinetochore attachments and therefore faithful chromosomal segregation (34). (ap26113.com)
GR phosphorylation by an Aurora kinase-dependent pathway provides the mechanism explaining the tight coupling GSK1904529A of ligand-independent GR phosphorylation to cell cycle phase because the maximal activity of these kinases occurs in mitosis. (ap26113.com)
Redox priming promotes Aurora A activation during mitosis. (cornell.edu)
The Aurora family of kinases and their downstream targets are key components of the cellular machinery that ensures the proper execution of mitosis and the accurate segregation of chromosomes to daughter cells. (cornell.edu)
These findings reveal a potential mechanistic link between Aurora A activation and changes in the intracellular redox state during mitosis and provide insights into how novel small-molecule inhibitors may be developed to target specific subpopulations of Aurora A. (cornell.edu)
kinase in candida, is an important mitosis regulatory proteins encoded on human being chromosome 20q13.2 that induces oncogenic change followed with centrosome amplification and aneuploidy when over indicated SEMA3E in rodent cells and (6-8). (arcillaresearch.com)

The development of the phthalazinone template resulted in a potent Aurora-A selective series of compounds (typically >1000-fold selectivity over Aurora-B) that display good pharmacological profiles with significantly improved oral bioavailability compared to the well studied Aurora inhibitor VX-680. (rcsb.org)
SNS-314 is an ATP-competitive, selective, and potent nanomolar inhibitor of aurora kinases in vitro. (cogershop.com)
MLN8054 is an aurora kinase inhibitor MLN8054, which is an orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. (xcessbio.com)
In September 2022, Puma entered into an exclusive license agreement for the development and commercialization of the anti-cancer drug alisertib, a selective, small molecule, orally administered inhibitor of aurora kinase A. Initially, Puma intends to focus the development of alisertib on the treatment of small cell lung cancer and breast cancer. (pumabiotechnology.com)
Taken together, these data confirm ORIC-114 as a potent, selective, irreversible, brain penetrant EGFR exon 20 inhibitor, and a promising therapeutic candidate, including for patients with CNS metastases. (oricpharma.com)
ORIC discovered novel, potent, orally bioavailable small molecule inhibitors of PLK4 that are highly selective, including against the closely related aurora kinases and PLK1-3. (oricpharma.com)
Cell viability assessment across a cancer cell line panel revealed that the highly selective ORIC PLK4 inhibitors showed greater potency in TRIM37 high cancer cell lines as compared to TRIM37 low cell lines. (oricpharma.com)
Importantly, cell potency in TRIM37 high cancer cells was rescued with knockdown of TRIM37, illustrating that selective PLK4 inhibitors are synthetic lethal with TRIM37 amplification. (oricpharma.com)
In particular, compound 21 (SNS-314) is a potent and selective Aurora kinase inhibitor that exhibits significant activity in pre-clinical in vivo tumor models. (rcsb.org)
NTRC has developed a series of highly selective inhibitors of TTK enzyme activity that potently inhibit proliferation of human cancer cells and tumour growth in mouse models. (oncolines.com)
In addition, NTRC develops own novel targeted therapies based on small molecules, such as selective inhibitors of TTK (Mps1) protein kinase for chromosomal unstable tumours and inhibitors of the tryptophan metabolizing enzymes IDO1 and TDO for cancer immunotherapy. (oncolines.com)

The hinge (yellow), glycine-rich loop (blue), and activation loop (red) are key features of the protein kinase fold involved in binding adenosine. (wikipedia.org)
The protein backbone atoms of residues Glu-211, Ala-213 in the hinge region of Aurora-2, and the sidechain of residue Trp-277, located in the activation loop, bind adenosine through specific hydrogen bonds. (wikipedia.org)
Residues Lys-162 and Asp-274 are essential for Aurora-2 kinase activity but do not hydrogen bond to each other as seen in crystal structures of several other protein kinases. (wikipedia.org)
Recently, we reported that the nucleus-mitochondria positive feedback loop formed by p90 ribosomal S6 kinase (p90RSK) and phosphorylation of S496 on ERK5 (a unique member of the mitogen-activated protein kinase family that is not only a kinase but also a transcriptional co-activator) were vital signaling events that played crucial roles in linking mitochondrial dysfunction, nuclear telomere dysfunction, persistent SASP induction, and atherosclerosis. (oaepublish.com)
By using a direct in vivo shRNA screen, we show that liver cancer cells that have mutations in the gene encoding the tumor suppressor protein p53 (Trp53 in mice and TP53 in humans) and that are driven by the oncoprotein NRAS become addicted to MYC stabilization via a mechanism mediated by aurora kinase A (AURKA). (scite.ai)
An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. (lookformedical.com)
The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters. (lookformedical.com)
Mammalian aurora-A belongs to a multigenic family of mitotic serine/threonine kinases comprising two other members: aurora-B and aurora-C. In this review we will focus on aurora-A that starts to localize to centrosomes only in S phase as soon as centrioles have been duplicated, the protein is then degraded in early G1. (lookformedical.com)
Immune system Nevertheless, nuclear launch of Bora isn't the only system by which its service of Aurora A is controlled since the bora mutant phenotype can be rescued by Bora fused to a signal, which keeps the protein in the cytoplasm, or fused to a localization signal, which maintains the protein in the nucleus until nuclear envelope breakdown. (others-signal.com)
Patients characterized by elevated EGFR and elevated Aurora-A protein expression in tumor tissue represent a risk group with poor disease-free and overall survival (EGFR low Aurora-A low versus EGFR high Aurora-A high , p=0.024). (oncotarget.com)
Comparing pan-Aurora kinase and Aurora-A targeting hints towards a strong and clinically relevant biological effect mediated via Aurora kinase B. Taken together, our findings characterize a new poor risk group in SCCHN patients defined by elevated EGFR and Aurora-A protein expression. (oncotarget.com)
Background: The phosphorylation of NF-kappaB inhibitor alpha (IκBα) protein is pivotal to the regulation of NF-κB transcription factor activity in the cell. (researchsquare.com)
Moreover, decreasing this threshold with inhibitors of antiapoptotic Bcl-2 family members protein sensitized cells to p53-induced apoptosis. (arcillaresearch.com)
Oncogenic protein kinase signalling in neuroblastoma has conventionally focussed on transduction through the well-characterised PI3K/Akt and MAPK pathways, in which the latter has been implicated in treatment resistance. (molecularmetabolism.com)
Moreover, since the identification of ALK, several additional protein kinases, including the PIM and Aurora kinases , have emerged not only as drivers of the disease phenotype, but also as promising druggable targets. (molecularmetabolism.com)
Aided by significant advances in structural biology and a broader understanding of the mechanisms of protein kinase function and regulation, we comprehensively outline the role of protein kinase signalling, emphasising ALK, PIM and Aurora in neuroblastoma, their respective metabolic outputs, and broader implications for targeted therapies . (molecularmetabolism.com)
The protein kinase TTK is a component of the spindle assembly checkpoint, a protein machinery that regulates correct segregation of chromosomes over daughter cells during cell division. (oncolines.com)
1,2] At the AACR, the X-ray protein crystal structure of TTK in complex with NTRC 0066-0 and other TTK inhibitors will be presented. (oncolines.com)
In this thesis a model protein, namely cAMP-dependent protein kinase (PKA) is used to gain particular insights into kinase behavior and thermodynamics upon ligand binding. (uni-marburg.de)

Aurora kinases constitute a family of serine-threonine kinases that are strongly associated with cancer. (cogershop.com)

In addition, MLN8054 selectively inhibits Aurora A over Aurora B in cultured cells, and inhibits cell proliferation by promoting G2/M accumulation and spindle defects in multiple cultured human tumor cells lines. (xcessbio.com)
Works in various organisms have revealed that the kinase is involved in centrosome separation, duplication and maturation as well as in bipolar spindle assembly and stability. (lookformedical.com)
More over, TPX2 is only necessary for a part of Aurora A dependent processes: TPX2 inactivation by RNAi causes spindle problems and reduction of Aurora A from the mitotic spindle, but centrosome maturation is normal, and the centrosome pool of the kinase is unchanged. (others-signal.com)
TPX2/ Aurora A binding is stimulated by the little GTPase Ran, which in turn is activated by RCC1, an exchange factor that is found on condensed chromatin and is involved with microtubule nucleation and spindle formation. (others-signal.com)
Therefore, unlike Bora, TPX2 appears to be specifically in charge of the spindle assembly purpose of Aurora A. To date, no TPX2 homolog has been discovered in Drosophila. (others-signal.com)
Aurora A influences centrosome maturation and spindle assembly, while Auroras B and C direct chromosome alignment and segregation. (rndsystems.com)

Phosphorylation of Histone H3 on serine 10, a known Aurora B cellular target, is inhibited with an EC50 of ~9nM following treatment of cells with SNS-314. (cogershop.com)
The phosphorylation of IκBα by IκB kinase family have been so many identified, but the phosphorylation sites of IκBα by other kinases remain poorly understood. (researchsquare.com)
To identify the essential domains of IκBα for phosphorylation of IκBα by AURK, kinase assay was performed with a series of IκBα truncation mutants. (researchsquare.com)

Bora can activate Aurora A in vitro. (others-signal.com)
Although in Drosophila, Bora so far may be the only known activator of Aurora A, many in vitro activators of Aurora A have now been discovered in other creatures. (others-signal.com)

Aurora kinases regulate cell cycle transit from G2 through cytokinesis, and thus are targets in cancer therapy. (wikipedia.org)
Treating SCCHN cell lines with a pan-Aurora kinase inhibitor resulted in defective cytokinesis, polyploidy and apoptosis, which was effective irrespective of the EGFR status. (oncotarget.com)

Aurora kinases, so named because the scattered mitotic spindles generated by mutant forms resemble the Aurora Borealis, have gained a great deal of attention as possible anticancer drug targets. (wikipedia.org)
A family of serine/threonine kinase Aurora constitutes a key regulator in the orchestration of mitotic events. (lookformedical.com)

Taken together, these results demonstrate that the ORIC small molecule CD73 inhibitor potently inhibits the adenosine pathway, which restores anti-tumor immunity and therefore holds potential for patients with multiple myeloma. (oricpharma.com)

Kinase selectivity studiesshowed that AP24534 does not inhibit Aurora kinases, clearly distinguishing it from other T315I inhibitors in development. (others-signal.com)
A kinase screen testing 16 ligands against 39 different kinases was performed in order to evaluate if thermodynamic properties can be correlated to the selectivity profile of a potential drug. (uni-marburg.de)
Especially for kinases, selectivity is challenging but of utmost importance. (uni-marburg.de)

The Aurora enzymes are particularly significant because they are involved in a direct path to the nucleosome by phosphorylating histone H3. (wikipedia.org)

There are three mammalian aurora kinase genes, encoding aurora A, B and C. Intense investigation has focused on aurora A and B as they appear to play a role in oncogenesis with aurora A identified as a low penetrance tumor susceptibility gene in mice and humans. (wikipedia.org)
We showed in both egg extracts and mammalian cells that a conserved cysteine residue within the Aurora A activation loop is crucial for Aurora A activation by autophosphorylation. (cornell.edu)
The mammalian Aurora kinase family contains three serine/threonine kinase members that participate in cell division. (rndsystems.com)

Furthermore, combinations of YK-4-279 with vincristine, paclitaxel or the Aurora kinase A inhibitor MLN8237/Alisertib show strong synergy, particularly at low doses. (researcher-app.com)

A comprehensive kinase interaction map for dasatinib was recently described, though assay differences preclude direct comparison of the kinase users of AP24534 and dasatinib. (others-signal.com)

Furthermore, Aurora kinases are known to be oncogenic and overexpressed in various forms of cancerous growth, including leukemia, colon cancer, prostate cancer and breast cancer tumors. (wikipedia.org)

TWS 119 is a potent inhibitor of glycogen synthase kinase-3β (IC 50 = 30 nM). (tocris.com)
All of Brequinar the data highlighted the potential of HGP-1 to be always a potent inhibitor for HGF/MET signaling. (arcillaresearch.com)

So far three Aurora-kinase inhibitors have been described: ZM447439, hesperadin and VX-680. (wikipedia.org)
ZM447439 Hesperadin VX-680 The structure and active site of Aurora-2-adenosine complex has been determined. (wikipedia.org)

Janssen has called off development of its Bace inhibitor atabecestat owing to serious liver enzyme elevations seen in the phase II/III Early trial , which aimed to prove that the project could slow cognitive decline in amyloid-positive asymptomatic people at risk of developing Alzheimer's dementia. (evaluate.com)

Background Aurora kinase A (AURKA) is amplified with varying occurrence in multiple human being cancers including mind and throat squamous cell carcinoma (HNSCC). (arcillaresearch.com)
Additional analysis of small-molecule AURKA inhibitors as restorative agents is usually warranted. (arcillaresearch.com)

The zinc finger domain of Tzfp binds to the tbs motif located at the upstream flanking region of the Aie1 (aurora-C) kinase gene. (lookformedical.com)
Substantial reductions will be anticipated to require at least two modifications at nonproximal residues?a forecast consistent with findings from our mutagenesis screen, though mutations that destabilize the inactive conformation of ABL to which AP24534 binds, including T315I and E255V, lead to small reductions in binding affinity. (others-signal.com)
Methods: Previously we observed that aurora kinase (AURK) binds IκBα in the cell. (researchsquare.com)

As both ALK and RAS signal through the MEK/ERK pathway, we sought to evaluate two previously reported inhibitors of ETS-related transcription factors, which are transcriptional mediators of the Ras-MEK/ERK pathway in other cancers. (researcher-app.com)
physicochemical actions and bioactivities, a HGF focusing on peptide was chosen to be always a potential inhibitor applicant for HGF/MET signaling pathway. (arcillaresearch.com)
Future strategies employing specific kinase inhibitors as part of the treatment regimen should consider combinatorial attempts at interfering with tumour metabolism, either through metabolic pathway inhibitors, or by dietary means, with a view to abolish metabolic flexibility that endows cancerous cells with a survival advantage. (molecularmetabolism.com)

In this study, x-ray crystal structures of the Aurora A kinase domain delineate redox-sensitive cysteine residues that, upon covalent modification, can allosterically regulate kinase activity and oligomerization state. (cornell.edu)

Some kinases are essential scientific objectives of imatinib, nilotinib, and/or dasatinib, although only dasatinib has been reported to inhibit all SRC family kinases. (others-signal.com)

Sizeable expression modifications between MEN2A and VHL PCC The comparison small molecule Aurora Kinases inhibitor of MEN2A and VHL associated PCC was feasible on three platforms, as well as a even further dataset was analyzed by SAM, also three substantial gene lists had been col lected from literature search. (tcr-signal.com)
Through the comparison of those seven gene lists, we've got identified 162 genes which were widespread in no less than two gene lists, as an example, CHGB, neural cell adhesion molecule 1, pla cental development factor, PNMT, vascular endothelial development factor. (tcr-signal.com)
Cooperative game theory examination The amount of index genes revealed tgf beta 1 inhibitor from cooperative game theory examination was similar to the number of sizeable gene expression changes and showed excellent overlap with them. (tcr-signal.com)
Furthermore, hypothesizing that the transcriptional response was graded dependant upon the anxiety intensity, we tested if, at greater selelck kinase inhibitor WOA uptake charges, amplified gene expression modifications would result in higher biomass growth compared to the measured gene expression alterations. (tcr-signal.com)
Aurora Kinase-A gene is usually amplified and overexpressed in lots of human malignancies, including colorectal, breasts, ovarian, bladder, gastric and pancreatic malignancies. (arcillaresearch.com)

Different subclasses of PI3K/mTOR, Aurora and EZH2 inhibitors were identified that relate to different mechanisms of activity or different genetic targeting. (oncolines.com)

Preclinical results for VX-680 reported by Vertex scientists in early 2004 demonstrated for the first time that a compound targeting the Aurora mechanism could induce tumor regression in human models of solid tumor cancers. (vrtx.com)

The term "oncotarget" encompasses all molecules, pathways, cellular functions, cell types, and even tissues that can be viewed as targets relevant to cancer as well as other diseases. (oncotarget.com)
Despite massively divergent regulatory mechanisms, ALK, PIM and Aurora kinases all obtain significant roles in cellular glycolytic and mitochondrial metabolism and neuroblastoma progression, and in several instances are implicated in treatment resistance. (molecularmetabolism.com)

For other types of ligands, e.g. longer nucleotides and peptides, a manually drawn representation of the molecule may be provided. (guidetopharmacology.org)

Aurora kinases are found in all organisms in which their function has been conserved throughout evolution, namely the control of chromosome segregation. (lookformedical.com)

Increased target residence time correlated with increased activity of TTK inhibitors in cancer cell line proliferation assays. (oncolines.com)

Thus, a low concentration of signal in the environment, even as little as a single molecule, can yield a large intracellular signal and response. (axonmedchem.com)
Also, it can be conceivable the favorable intracellular distribution Secretase inhibitors of weakly essential drugs within cancer cells with defective lysosomal acidification could offset the aforementioned unfavorable accumulation differences that could exist. (pkainhibitors.com)

citation needed] Kinome Cyclin-dependent kinase Signal transduction Andrews, Paul D. (wikipedia.org)

We analyzed the clinical data and performed immunohistochemistry for Epidermal growth factor receptor (EGFR) and Aurora kinase A (Aurora-A) expression in 180 SCCHN patients. (oncotarget.com)
Our results demonstrate that combined targeting of EGFR and Aurora kinases represents a therapeutic means to activate cell cycle checkpoints and apoptosis in SCCHN. (oncotarget.com)

PCa samples from the 66 patients were analyzed using immunohistochemical staining for the detection of chromogranin, neural cell adhesion molecule 1, and synaptophysin. (biomedcentral.com)

Mechanistic and evolutionary insights into isoform-specific 'supercharging' in DCLK family kinases. (liverpool.ac.uk)

In human, aurora-A has focused a lot of attention, since its overexpression has been found to be correlated with the grade of various solid tumours. (lookformedical.com)
Those transformed cells form tumours when implanted in immunodeficient mice, indicating that the kinase is an oncogene. (lookformedical.com)

We previously have identified POSTN (which encodes periostin) as an invasion-promoting molecule in HNSCC. (bvsalud.org)

In addition, the companies will conduct a joint research program to characterize VX-680's activity across a broad range of cancer types as well as to identify follow-on drug candidates directed at Aurora kinases, using molecular profiling approaches and microarray technologies pioneered by Merck. (vrtx.com)
This collaboration unites Vertex's drug discovery leadership targeting Aurora kinases with Merck's proprietary molecular profiling technologies and clinical development infrastructure in oncology. (vrtx.com)
Calculated molecular properties are available for small molecules and natural products (not peptides). (guidetopharmacology.org)
SMILES (Simplified Molecular Input Line Entry Specification) A specification for unambiguously describing the structure of chemical molecules using short ASCII strings. (guidetopharmacology.org)

In Merck, we have a partner that is a global leader in the development and commercialization of innovative medicines, and one with the breadth of capabilities and resources that we expect to be required to establish the clinical benefit of an Aurora kinase inhibitor across a spectrum of solid tumors and hematologic cancers. (vrtx.com)
It has consequently been proposed that such molecules could constitute ideal chemoprotectants for individuals bearing p53-mutant tumors. (immune-source.com)

AURK significantly promotes activation of IκBα at serine 32, but not serine 36 residues, unlike IκB kinase (IKK) family proteins activate both IκBα serine residues. (researchsquare.com)

Mutation is contributed substantially to the inhibitors affinity for its target, by each of the hydrogen bonding and contact residue interactions based interruption of just one component of the binding system or distortion of a within the binding pocket results in merely a slight reduction in affinity. (others-signal.com)
Beyond Affinity: Drug-Kinase I. (uni-marburg.de)

Several small-molecule activators of the p53 tumor suppressor have been shown to induce a slight cytostatic response in normal cells in tradition. (immune-source.com)

Whitehouse Station, NJ and Cambridge, MA, June 22, 2004 -- Merck & Co., Inc. (NYSE: MRK) and Vertex Pharmaceuticals Incorporated (Nasdaq: VRTX) announced today that they have entered into a global collaboration to develop and commercialize VX-680, Vertex's lead Aurora kinase inhibitor that is expected to enter clinical development this year for the treatment of cancer. (vrtx.com)
Oss, April, 8th, 2016 - At the AACR 2016 conference, to be held in New Orleans next week, Jos de Man, Senior Investigator Chemistry at NTRC, will present on the unique binding mode of NTRC's TTK kinase inhibitor clinical candidate NTRC 0066-0. (oncolines.com)

Ectopic kinase overexpression in any culture cell line leads to polyploidy and centrosome amplification. (lookformedical.com)

Taken together, our data demonstrate that the small molecule AurA inhibitor AKI603 may be used to overcome drug resistance induced by BCR-ABL-T315I mutation in CML. (scite.ai)
However, despite progress in the development of small-molecule inhibitors of ALK, treatment resistance frequently arises and appears to be a feature of the disease. (molecularmetabolism.com)

HSP90AA1 Aurora kinases are grasp regulators of both centrosome and checkpoint control function. (ap26113.com)

This feature probably contributes to the relatively wide kinase specificity profile of AP24534, including VEGFR and FGFR family kinases, receptors perhaps not restricted by the three currently authorized BCR ABL drugs. (others-signal.com)

Aurora kinase inhibitors are a putative drug class for treating cancer. (wikipedia.org)
We are pleased to enter this collaboration with Merck, which shares our vision of Aurora kinase inhibitors as a class of drugs that may have the potential to transform the future of cancer treatment," said Joshua Boger, Ph.D., Chairman and CEO of Vertex. (vrtx.com)
This agreement places a significant value on our innovations in the area of Aurora kinases and cancer, and highlights Vertex's progress in realizing our 2004 business development and collaborative revenue objectives," Boger added. (vrtx.com)
A recent study shows that MLN8054 sensitizes androgen-resistant prostate cancer to radiation by inhibiting Aurora A kinase, which is associated with sustained DNA double-strand breaks. (xcessbio.com)
Jones D, Noble M, Wedge SR, Robson CN, Gaughan L. Aurora A regulates expression of AR-V7 in models of castrate resistant prostate cancer . (ncl.ac.uk)
It is shown that the biochemical target of an inhibitor predicts its clustering, and that empirical cell line responses correspond to well-known cancer hallmarks. (oncolines.com)
Due to their implication in various diseases such as cancer, kinases are of utmost importance in drug design. (uni-marburg.de)

This compound has been shown to selectively shield normal cells against S-phase poisons 8 tubulin poisons 9 10 a Polo-like kinase 1 inhibitor (PLK1I)12 and an Aurora kinase inhibitor.7 Most importantly oral administration of nutlin-3 protects mice against PLK1I-induced neutropenia.12 Table?1. (immune-source.com)
This compound is a highly cell-permeable purine compound that acts as an ATP-competitive inhibitor of cyclin dependent kinases (CDKs). (guidetoimmunopharmacology.org)

Anatomy21

Organisms9

Diseases6

Chemicals and Drugs128

Analytical, Diagnostic and Therapeutic Techniques and Equipment32

Phenomena and Processes63

Disciplines and Occupations3

Technology, Industry, Agriculture1

Information Science4

Inhibition6

Mitosis17

Selective11

Protein19

Serine-threoni1

Spindle6

Phosphorylation3

Vitro2

Cytokinesis2

Mitotic2

Potently inhibits1

Selectivity3

Enzymes1

Mammalian3

Alisertib1

Assay1

Oncogenic1

Potent inhibitor2

ZM4474392

Enzyme1

AURKA2

Binds3

Pathway3

Regulate1

Inhibit1

Gene5

MTOR1

Mechanism1

Cellular2

Ligands1

Chromosome1

Proliferation1

Intracellular2

Transduction1

EGFR2

Neural1

Insights1

Tumours2

HNSCC1

Molecular4

Tumors2

Proteins1

Affinity2

Activators1

Clinical2

Polyploidy1

Resistance2

Regulators1

Family1

Cancer7

Compound2