Search Results - "BRAY, Mark R."
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Targeting Mitosis in Cancer: Emerging Strategies
Published in Molecular cell (19-11-2015)“…The cell cycle is an evolutionarily conserved process necessary for mammalian cell growth and development. Because cell-cycle aberrations are a hallmark of…”
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Functional Characterization of CFI-400945, a Polo-like Kinase 4 Inhibitor, as a Potential Anticancer Agent
Published in Cancer cell (11-08-2014)“…PLK4 was identified as a promising therapeutic target through a systematic approach that combined RNAi screening with gene expression analysis in human breast…”
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Functional characterization of CFI-402257, a potent and selective Mps1/TTK kinase inhibitor, for the treatment of cancer
Published in Proceedings of the National Academy of Sciences - PNAS (21-03-2017)“…Loss of cell-cycle control is a hallmark of human cancer. Cell-cycle checkpoints are essential for maintaining genome integrity and balanced growth and…”
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Fcmr regulates mononuclear phagocyte control of anti-tumor immunity
Published in Nature communications (18-06-2019)“…Myeloid cells contribute to tumor progression, but how the constellation of receptors they express regulates their functions within the tumor…”
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The Discovery of Orally Bioavailable Tyrosine Threonine Kinase (TTK) Inhibitors: 3‑(4-(heterocyclyl)phenyl)‑1H‑indazole-5-carboxamides as Anticancer Agents
Published in Journal of medicinal chemistry (23-04-2015)“…The acetamido and carboxamido substituted 3-(1H-indazol-3-yl)benzenesulfonamides are potent TTK inhibitors. However, they display modest ability to attenuate…”
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2-Methoxyestradiol inhibits experimental autoimmune encephalomyelitis through suppression of immune cell activation
Published in Proceedings of the National Academy of Sciences - PNAS (18-12-2012)“…The endogenous metabolite of estradiol, 2-Methoxyestradiol (2ME2), is an antimitotic and antiangiogenic cancer drug candidate that also exhibits…”
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Author Correction: Fcmr regulates mononuclear phagocyte control of anti-tumor immunity
Published in Nature communications (03-09-2019)“…An amendment to this paper has been published and can be accessed via a link at the top of the paper…”
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Predictive Biomarkers of Sensitivity to the Aurora and Angiogenic Kinase Inhibitor ENMD-2076 in Preclinical Breast Cancer Models
Published in Clinical cancer research (01-01-2013)“…The Aurora kinases are a family of conserved serine-threonine kinases with key roles in mitotic cell division. As with other promising anticancer targets,…”
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ENMD-2076, an oral inhibitor of angiogenic and proliferation kinases, has activity in recurrent, platinum resistant ovarian cancer
Published in European journal of cancer (1990) (01-01-2013)“…Abstract Purpose The purpose was to assess the activity and side effect profile of ENMD-2076, an oral anti-angiogenic and anti-proliferative kinase inhibitor,…”
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Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD‐2076, against multiple myeloma
Published in British journal of haematology (01-08-2010)“…Summary ENMD‐2076 is a novel, orally‐active molecule that has been shown to have significant activity against aurora and multiple receptor tyrosine kinases. We…”
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Assessment of the In vivo Antitumor Effects of ENMD-2076, a Novel Multitargeted Kinase Inhibitor, against Primary and Cell Line-Derived Human Colorectal Cancer Xenograft Models
Published in Clinical cancer research (01-06-2010)“…This in vivo study was designed to investigate the efficacy of ENMD-2076, a small-molecule kinase inhibitor with activity against the Aurora kinases A and B,…”
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Safety and tolerability of CFI-400945, a first-in-class, selective PLK4 inhibitor in advanced solid tumours: a phase 1 dose-escalation trial
Published in British journal of cancer (13-08-2019)“…Background CFI-400945 is a first-in-class oral inhibitor of polo-like kinase 4 (PLK4) that regulates centriole duplication. Primary objectives of this…”
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Inhibition of Aberrantly Overexpressed Polo-like Kinase 4 Is a Potential Effective Treatment for DNA Damage Repair-Deficient Uterine Leiomyosarcoma
Published in Clinical cancer research (03-09-2024)“…Uterine leiomyosarcoma (LMS) is an aggressive sarcoma and a subset of which exhibits DNA repair defects. Polo-like kinase 4 (PLK4) precisely modulates mitosis,…”
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Polo-like kinase 4 inhibitor CFI-400945 suppresses liver cancer through cell cycle perturbation and eliciting antitumor immunity
Published in Hepatology (Baltimore, Md.) (01-03-2023)“…Prognosis of HCC remains poor due to lack of effective therapies. Immune checkpoint inhibitors (ICIs) have delayed response and are only effective in a subset…”
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Analysis of binding of the family 2a carbohydrate-binding module from Cellulomonas fimi xylanase 10A to cellulose: specificity and identification of functionally important amino acid residues
Published in Protein engineering (01-11-2000)“…The family 2a carbohydrate-binding module (CBM2a) of xylanase 10A from Cellulomonas fimi binds to the crystalline regions of cellulose. It does not share…”
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Preclinical characterization and clinical trial of CFI-400945, a polo-like kinase 4 inhibitor, in patients with relapsed/refractory acute myeloid leukemia and higher-risk myelodysplastic neoplasms
Published in Leukemia (01-03-2024)“…CFI-400945 is a selective oral polo-like kinase 4 (PLK4) inhibitor that regulates centriole duplication. PLK4 is aberrantly expressed in patients with acute…”
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Identification of KIFC1 as a putative vulnerability in lung cancers with centrosome amplification
Published in Cancer gene therapy (01-10-2024)“…Centrosome amplification (CA), an abnormal increase in the number of centrosomes in the cell, is a recurrent phenomenon in lung and other malignancies…”
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ENMD-2076 is an orally active kinase inhibitor with antiangiogenic and antiproliferative mechanisms of action
Published in Molecular cancer therapeutics (01-01-2011)“…ENMD-2076 is a novel orally active, small molecule kinase inhibitor with a mechanism of action involving several pathways key to tumor growth and survival:…”
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DJ-1, a novel regulator of the tumor suppressor PTEN
Published in Cancer cell (01-03-2005)“…The phosphatidylinositol 3′ kinase (PI3′K) pathway, which regulates cell survival, is antagonized by the PTEN tumor suppressor. The regulation of PTEN is…”
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