Aurora kinase inhibitors in preclinical and clinical testing

No abstract is available for this paper.

• Publication year

  2009

• Venue

  Expert Opinion on Investigational Drugs

• Publication date

  2009-04-01

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1517/13543780902806392PMID 19335272
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.

  2009cited by this paper
• Advances in Aurora kinase inhibitor patents

  2009cited by this paper
• A dose-escalation and pharmacodynamic study of AT9283 in patients with refractory solid tumours

  2008cited by this paper
• Higher doses of lenalidomide are associated with unacceptable toxicity including life-threatening tumor flare in patients with chronic lymphocytic leukemia.

  2008cited by this paper
• Phase I study of the pan aurora kinases (AKs) inhibitor PHA-739358 administered as a 24 h infusion without/with G-CSF in a 14-day cycle in patients with advanced solid tumors

  2008cited by this paper
• Frequent overexpression of Aurora Kinase A in upper gastrointestinal adenocarcinomas correlates with potent antiapoptotic functions

  2008cited by this paper
• Phase I accelerated dose-escalation, pharmacokinetic (PK) and pharmacodynamic study of PF-03814735, an oral aurora kinase inhibitor, in patients with advanced solid tumors: Preliminary results

  2008cited by this paper
• Phase 1 trial of SNS-314, a novel selective inhibitor of aurora kinases A, B, and C, in advanced solid tumor patients

  2008cited by this paper
• Aurora Kinases as Anticancer Drug Targets

  2008cited by this paper
• Phase I and pharmacodynamic trial of AT9283, an aurora kinase inhibitor, in patients with refractory leukemia

  2008cited by this paper
• Activity of the Multi-Targeted Kinase Inhibitor, AT9283 on Imatinib-Resistant CML Models.

  2008cited by this paper
• Aurora kinase expression in colorectal adenocarcinoma: correlations with clinicopathological features, p16 expression, and telomerase activity.

  2008cited by this paper
• Discovery of a potent and selective aurora kinase inhibitor.

  2008cited by this paper
• The Aurora Kinase Inhibitor MLN8237 Has Potent Anticancer Activity in CML and Ph+ ALL Models and Significantly Increases the Efficacy of Nilotinib

  2008cited by this paper
• ASAP is a novel substrate of the oncogenic mitotic kinase Aurora-A: phosphorylation on Ser625 is essential to spindle formation and mitosis.

  2008cited by this paper
• Phosphorylation of HsMis13 by Aurora B Kinase Is Essential for Assembly of Functional Kinetochore*

  2008cited by this paper
• Aurora-A and ch-TOG act in a common pathway in control of spindle pole integrity

  2008cited by this paper
• Molecular basis of drug resistance in aurora kinases.

  2008cited by this paper
• Aurora kinase inhibitors: identification and preclinical validation of their biomarkers

  2008cited by this paper
• MLN8237: an orally active small molecule inhibitor of Aurora A kinase in phase I clinical trials

  2008influential reference
• Aurora B kinase and protein phosphatase 1 have opposing roles in modulating kinetochore assembly

  2008cited by this paper
• The Aurora kinase family in cell division and cancer.

  2008cited by this paper
• In vivo mode of action of CYC116, a novel small molecule inhibitor of Aurora kinases and VEGFR2

  2008cited by this paper
• Targeting Aurora Kinase with MK-0457 Inhibits Ovarian Cancer Growth

  2008cited by this paper
• SAR and chemistry of Aurora kinase inhibitors: Discovery of PF-3814735, an oral clinical candidate

  2008cited by this paper
• Requirement of Aurora-A kinase in astral microtubule polymerization and spindle microtubule flux

  2008cited by this paper
• Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I.

  2008influential reference
• Acute myeloblastic leukemia in adult patients: ESMO clinical recommendations for diagnosis, treatment and follow-up.

  2007cited by this paper
• Aurora B controls the association of condensin I but not condensin II with mitotic chromosomes

  2007cited by this paper
• Targeted anti-mitotic therapies: can we improve on tubulin agents?

  2007influential reference
• The kinases aurora B and mTOR regulate the G1–S cell cycle progression of T lymphocytes

  2007influential reference
• PHA-739358, a potent inhibitor of Aurora kinases with a selective target inhibition profile relevant to cancer

  2007cited by this paper
• Antitumor activity of MLN8054, an orally active small-molecule inhibitor of Aurora A kinase

  2007influential reference
• AS703569, a novel aurora kinase inhibitor, enhances the antiproliferative effects of other targeted therapies in human cancer cell lines

  2007cited by this paper
• A novel treatment strategy targeting Aurora kinases in acute myelogenous leukemia

  2007cited by this paper
• Cellular and molecular mechanisms of action of AS703569, a novel aurora kinase inhibitor, in human cancer cell lines

  2007cited by this paper
• Phase I clinical trial of MLN8054, a selective inhibitor of Aurora A kinase

  2007influential reference
• Discovery and development of MP529, a new effective and selective inhibitor of Aurora A kinase.

  2007cited by this paper
• The role of Aurora-A inhibitors in cancer therapy.

  2007cited by this paper
• Differential functions of the Aurora-B and Aurora-C kinases in mammalian spermatogenesis.

  2007cited by this paper
• AZD1152, a Selective Inhibitor of Aurora B Kinase, Inhibits Human Tumor Xenograft Growth by Inducing Apoptosis

  2007cited by this paper
• MLN8054, a Small-Molecule Inhibitor of Aurora A, Causes Spindle Pole and Chromosome Congression Defects Leading to Aneuploidy

  2007cited by this paper
• A phase I two arm trial of AS703569 (R763), an orally available aurora kinase inhibitor, in subjects with solid tumors: preliminary results

  2007cited by this paper
• Perimembrane Aurora-A Expression is a Significant Prognostic Factor in Correlation with Proliferative Activity in Non-Small-Cell Lung Cancer (NSCLC)

  2007influential reference
• Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.

  2007cited by this paper
• Analysis of the role of Aurora B on the chromosomal targeting of condensin I

  2007cited by this paper
• High copy amplification of the aurora-A gene is associated with chromosomal instability phenotype in human colorectal cancers

  2007cited by this paper
• MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation.

  2007cited by this paper
• Enhancement of radiation response in p53-deficient cancer cells by the Aurora-B kinase inhibitor AZD1152

  2007cited by this paper
• Roles of Aurora Kinases in Mitosis and Tumorigenesis

  2007cited by this paper
• MK-0457, a Novel Multikinase Inhibitor, Is Active in Patients with Chronic Myeloid Leukemia (CML) and Acute Lymphocytic Leukemia (ALL) with the T315I BCR-ABL Resistance Mutation and Patients with Refractory JAK-2 Positive Myeloproliferative Diseases (MPD).

  2006cited by this paper
• Overexpression of Aurora-A kinase promotes tumor cell proliferation and inhibits apoptosis in esophageal squamous cell carcinoma cell line

  2006cited by this paper
• Identification of a lead small-molecule inhibitor of the Aurora kinases using a structure-assisted, fragment-based approach

  2006cited by this paper
• Overexpression of aurora kinase A in mouse mammary epithelium induces genetic instability preceding mammary tumor formation

  2006cited by this paper
• Aurora Kinase A Messenger RNA Overexpression Is Correlated with Tumor Progression and Shortened Survival in Head and Neck Squamous Cell Carcinoma

  2006cited by this paper
• Aurora A, mitotic entry, and spindle bipolarity.

  2006cited by this paper
• PHA-680632, a Novel Aurora Kinase Inhibitor with Potent Antitumoral Activity

  2006cited by this paper
• Expression of Aurora kinases in human thyroid carcinoma cell lines and tissues

  2006cited by this paper
• 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile.

  2006cited by this paper
• Dynamic localization and functional implications of Aurora-C kinase during male mouse meiosis.

  2006influential reference
• Validating Aurora B as an anti-cancer drug target

  2006cited by this paper
• Aurora kinase is required for chromosome segregation in tobacco BY-2 cells.

  2006cited by this paper
• Phase I and pharmacological study of the novel aurora kinase inhibitor AZD1152.

  2006influential reference
• Aurora B expression correlates with aggressive behaviour in glioblastoma multiforme

  2006cited by this paper
• SAR and inhibitor complex structure determination of a novel class of potent and specific Aurora kinase inhibitors.

  2006cited by this paper
• MK-0457, a Novel Multikinase Inhibitor, Has Activity in Refractory AML, Including Transformed JAK2 Positive Myeloproliferative Disease (MPD), and in Philadelphia-Positive ALL.

  2006cited by this paper
• Mechanism of Aurora B activation by INCENP and inhibition by hesperadin.

  2005cited by this paper
• Aurora B overexpression associates with the thyroid carcinoma undifferentiated phenotype and is required for thyroid carcinoma cell proliferation.

  2005cited by this paper
• 1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.

  2005cited by this paper
• Kinetochore-spindle microtubule interactions during mitosis.

  2005cited by this paper
• Histone H3 serine 10 phosphorylation by Aurora B causes HP1 dissociation from heterochromatin

  2005cited by this paper
• Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.

  2005cited by this paper
• Overexpression of an Aurora-C kinase-deficient mutant disrupts the Aurora-B/INCENP complex and induces polyploidy.

  2005influential reference
• Aurora A phosphorylation of TACC3/maskin is required for centrosome-dependent microtubule assembly in mitosis

  2005cited by this paper
• Overexpression of aurora B kinase (AURKB) in primary non-small cell lung carcinoma is frequent, generally driven from one allele, and correlates with the level of genetic instability

  2005cited by this paper
• The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases.

  2005cited by this paper
• Stabilization of microtubule dynamics at anaphase onset promotes chromosome segregation

  2005cited by this paper
• Regulation of HP1–chromatin binding by histone H3 methylation and phosphorylation

  2005cited by this paper
• Aurora‐B and Rho‐kinase/ROCK, the two cleavage furrow kinases, independently regulate the progression of cytokinesis: possible existence of a novel cleavage furrow kinase phosphorylates ezrin/radixin/moesin (ERM)

  2005cited by this paper
• Aurora C is directly associated with Survivin and required for cytokinesis

  2005cited by this paper
• Potent and selective Aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition.

  2005cited by this paper
• Aurora-C kinase is a novel chromosomal passenger protein that can complement Aurora-B kinase function in mitotic cells.

  2004cited by this paper
• Aurora-kinase inhibitors as anticancer agents

  2004cited by this paper
• Aurora-A Abrogation of p53 DNA Binding and Transactivation Activity by Phosphorylation of Serine 215*

  2004cited by this paper
• Phosphorylation by aurora kinase A induces Mdm2-mediated destabilization and inhibition of p53

  2004cited by this paper
• Megakaryocytes express functional Aurora-B kinase in endomitosis.

  2004cited by this paper
• VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo

  2004cited by this paper
• Autophosphorylation of a Newly Identified Site of Aurora-B Is Indispensable for Cytokinesis*

  2004cited by this paper
• Aurora-A Kinase Maintains the Fidelity of Early and Late Mitotic Events in HeLa Cells*

  2003cited by this paper
• The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore–microtubule attachment and in maintaining the spindle assembly checkpoint

  2003cited by this paper
• Mitotic regulation of the human anaphase‐promoting complex by phosphorylation

  2003cited by this paper
• TACC1–chTOG–Aurora A protein complex in breast cancer

  2003cited by this paper
• Roles of aurora‐A kinase in mitotic entry and G2 checkpoint in mammalian cells

  2002cited by this paper
• Gene profiling of cell cycle progression through S-phase reveals sequential expression of genes required for DNA replication and nucleosome assembly.

  2002cited by this paper
• Aurora B kinase exists in a complex with survivin and INCENP and its kinase activity is stimulated by survivin binding and phosphorylation.

  2002cited by this paper
• Cell-cycle-dependent Regulation of Human aurora A Transcription Is Mediated by Periodic Repression of E4TF1*

  2002influential reference
• Molecular dynamics of Aurora-A kinase in living mitotic cells simultaneously visualized with histone H3 and nuclear membrane protein importinalpha.

  2002cited by this paper
• CENP-A is phosphorylated by Aurora B kinase and plays an unexpected role in completion of cytokinesis

  2001cited by this paper
• Aurora-A kinase is required for centrosome maturation in Caenorhabditis elegans

  2001influential reference
• Inhibition of DNA Replication and Induction of S Phase Cell Cycle Arrest by G-rich Oligonucleotides*

  2001cited by this paper

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• Aurora kinases signaling in cancer: from molecular perception to targeted therapies

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• Master Orchestrators of Cellular Regulation: Advances in Protein Kinase Inhibitors for Therapeutic Intervention

  2025cites this paper
• A comprehensive review on role of Aurora kinase inhibitors (AKIs) in cancer therapeutics.

  2024cites this paper
• Discovery of N-benzylbenzamide-based allosteric inhibitors of Aurora kinase A.

  2024cites this paper
• Recent advancements in mechanistic research, therapeutic potential, and structure-activity relationships of aurora kinase inhibitors in cancer therapies.

  2024cites this paper
• Development and therapeutic evaluation of 5D3(CC-MLN8237)3.2 antibody-theranostic conjugates for PSMA-positive prostate cancer therapy

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• Chromosomal instability: a key driver in glioma pathogenesis and progression

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• Six‐transmembrane epithelial antigen of prostate 3 (STEAP3) is a potential prognostic biomarker in clear cell renal cell carcinoma that correlates with M2 macrophage infiltration and epithelial–mesenchymal

  2023cites this paper
• Utilization of kinase inhibitors as novel therapeutic drug targets: A review

  2023cites this paper
• Synthesis, biological evaluation and molecular docking of new sulfonamide-based indolinone derivatives as multitargeted kinase inhibitors against leukemia.

  2021cites this paper
• Preclinical small molecule WEHI-7326 overcomes drug resistance and elicits response in patient-derived xenograft models of human treatment-refractory tumors

  2021cites this paper
• Reversing tozasertib resistance in glioma through inhibition of pyruvate dehydrogenase kinases

  2020cites this paper
• Recent researches for dual Aurora target inhibitors in antitumor field.

  2020cites this paper
• Effective Delivery of a Microtubule Polymerization Inhibitor Synergizes with Standard Regimens in Models of Pancreatic Ductal Adenocarcinoma

  2019cites this paper
• Indolin-2-one Derivatives: Theoretical Studies Aimed at Finding More Potent Aurora B Kinase Inhibitors

  2018cites this paper
• Pyrazolo[4,3-b]pyrimido[4,5-e][1,4]diazepine derivatives as new multi-targeted inhibitors of Aurora A/B and KDR.

  2018cites this paper
• The multifaceted allosteric regulation of Aurora kinase A

  2018cites this paper
• Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.

  2018cites this paper
• Aurora Kinase Inhibitors in Head and Neck Cancer.

  2018influential citation
• Critical risk-benefit assessment of the novel anti-cancer aurora a kinase inhibitor alisertib (MLN8237): A comprehensive review of the clinical data.

  2017cites this paper
• Mécanisme de contrôle de l'entrée en mitose par Polo-like kinase 1 (PlK1)

  2017cites this paper
• Unsuccessful mitosis in multicellular tumour spheroids

  2017influential citation
• Consecuencias de las alteraciones en la expresión de aurora quinasa B sobre la segregación cromosómica y la progresión del ciclo celular

  2017cites this paper
• Human Cancer Cell Lines: Potential to Evaluate the Therapeutic Efficacy of Anticancer Agents

  2017cites this paper
• Determination of a novel Aurora-A (AurA) kinase AKI603 by UPLC-MS/MS and its application to a bioavailability study in rat.

  2016cites this paper
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• Discovery of BPR1K871, a quinazoline based, multi-kinase inhibitor for the treatment of AML and solid tumors: Rational design, synthesis, in vitro and in vivo evaluation

  2016cites this paper
• Mitotic Kinase Aurora B is Frequently Overexpressed in Aggressive B-Cell Lymphoma

  2015cites this paper
• Structural Biology Insight for the Design of Sub-type Selective Aurora Kinase Inhibitors.

  2015cites this paper
• Integrated cross-coupling strategy for an α-carboline-based Aurora B kinase inhibitor.

  2015cites this paper
• Aurora kinase A inhibitors: promising agents in antitumoral therapy

  2014cites this paper
• Discovery of 4-aminoquinazoline--urea derivatives as Aurora kinase inhibitors with antiproliferative activity.

  2014cites this paper
• Facile Identification of Dual FLT3–Aurora A Inhibitors: A Computer‐Guided Drug Design Approach

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• CDKN1A‐mediated responsiveness of MLL‐AF4‐positive acute lymphoblastic leukemia to Aurora kinase‐A inhibitors

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• Molecular Pathways: Regulation and Targeting of Kinetochore–Microtubule Attachment in Cancer

  2014cites this paper
• Design, synthesis and bioevaluation of N-trisubstituted pyrimidine derivatives as potent aurora A kinase inhibitors.

  2014cites this paper
• Aurora kinase inhibitor patents and agents in clinical testing: an update (2011 – 2013)

  2014cites this paper
• Biological Characterization of TAK-901, an Investigational, Novel, Multitargeted Aurora B Kinase Inhibitor

  2013cites this paper
• Nucleolar proteins and cancer: The roles of aurora a-interacting nucleolar proteins in mitosis and cancer

  2013cites this paper
• 3D‐QSAR‐Assisted Drug Design: Identification of a Potent Quinazoline‐Based Aurora Kinase Inhibitor

  2013cites this paper
• Aurora Kinase B Is a Potential Therapeutic Target in Pediatric Diffuse Intrinsic Pontine Glioma

  2013cites this paper
• AMG 900, pan-Aurora kinase inhibitor, preferentially inhibits the proliferation of breast cancer cell lines with dysfunctional p53

  2013cites this paper
• Integrity of p53 Associated Pathways Determines Induction of Apoptosis of Tumor Cells Resistant to Aurora-A Kinase Inhibitors

  2013cites this paper
• Novel pyrimidine-2,4-diamine derivative suppresses the cell viability and spindle assembly checkpoint activity by targeting Aurora kinases.

  2013cites this paper
• Design, synthesis, quantum chemical studies and biological activity evaluation of pyrazole-benzimidazole derivatives as potent Aurora A/B kinase inhibitors.

  2013cites this paper
• BRCA1 downregulates the kinase activity of Polo-like kinase 1 in response to replication stress

  2013cites this paper
• Management of Diffuse Pontine Gliomas in Children: Recent Developments

  2013cites this paper
• Small molecule kinase inhibitors as anti-cancer therapeutics.

  2012cites this paper
• Inhibiting the aurora B kinase potently suppresses repopulation during fractionated irradiation of human lung cancer cell lines.

  2012cites this paper
• A novel Aurora kinase A inhibitor MK-8745 predicts TPX2 as a therapeutic biomarker in non-Hodgkin lymphoma cell lines

  2012cites this paper
• Clinical and Preclinical Treatment Aspects of Castration Resistant Prostate Cancer (CRPC)

  2012cites this paper
• Molecular dynamics and free energy studies on Aurora kinase A and its mutant bound with MLN8054: insight into molecular mechanism of subtype selectivity.

  2012cites this paper
• Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.

  2012cites this paper
• Aurora kinase B/C inhibition impairs malignant glioma growth in vivo

  2012cites this paper
• Dual Targeting of mTOR and Aurora-A Kinase for the Treatment of Uterine Leiomyosarcoma

  2012cites this paper
• Paclitaxel and CYC3, an aurora kinase A inhibitor, synergise in pancreatic cancer cells but not bone marrow precursor cells

  2012cites this paper
• Discovery of highly potent and selective pan-Aurora kinase inhibitors with enhanced in vivo antitumor therapeutic index.

  2012cites this paper
• Exploration of diverse hinge-binding scaffolds for selective Aurora kinase inhibitors.

  2012cites this paper
• Targeted Therapy and Molecular Genetics

  2012cites this paper
• The spindle assembly checkpoint as a drug target - Novel small-molecule inhibitors of Aurora kinases

  2012cites this paper
• Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity.

  2012cites this paper
• For Peer Review Novel Pyrimidine-2,4-Diamine Derivative Suppresses the Cell Viability and Spindle Assembly Checkpoint Activity by

  2012cites this paper
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• The flavonoid eupatorin inactivates the mitotic checkpoint leading to polyploidy and apoptosis.

  2012cites this paper
• Aurora A is differentially expressed in gliomas, is associated with patient survival in glioblastoma and is a potential chemotherapeutic target in gliomas

  2012cites this paper
• High expression of nuclear survivin and Aurora B predicts poor overall survival in patients with head and neck squamous cell cancer

  2012cites this paper
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  2011cites this paper
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  2011cites this paper
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  2011cites this paper
• Aurora B kinase inhibitor AZD1152: determinants of action and ability to enhance chemotherapeutics effectiveness in pancreatic and colon cancer

  2011cites this paper
• Aurora-A kinase inhibitor scaffolds and binding modes.

  2011cites this paper
• Unliganded progesterone receptors attenuate taxane-induced breast cancer cell death by modulating the spindle assembly checkpoint

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• Phase 1 study of MLN8054, a selective inhibitor of Aurora A kinase in patients with advanced solid tumors

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