First-time-in-human study of GSK923295, a novel antimitotic inhibitor of centromere-associated protein E (CENP-E), in patients with refractory cancer

No abstract is available for this paper.

• Publication year

  2012

• Venue

  Cancer Chemotherapy and Pharmacology

• Publication date

  2012-03-01

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1007/s00280-011-1756-zPMID 22020315
• 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.

• Antitumor activity of an allosteric inhibitor of centromere-associated protein-E

  2010influential reference
• Targeting a kinetochore-associated motor protein to kill cancer cells

  2010cited by this paper
• The role of kinesin family proteins in tumorigenesis and progression

  2010cited by this paper
• Kinesin motor proteins as targets for cancer therapy

  2009cited by this paper
• A Systems Analysis of Mitotic Apparatus Inhibitors Defines a Response Network for Breast Cancer.

  2009cited by this paper
• Targeted anti-mitotic therapies: can we improve on tubulin agents?

  2007cited by this paper
• Aneuploidy: instigator and inhibitor of tumorigenesis.

  2007cited by this paper
• A potent and selective inhibitor of the mitotic kinesin CENP-E (GSK923295A), demonstrates a novel mechanism of inhibiting tumor cell proliferation and shows activity against a broad panel of human tumor cell lines in vitro

  2007cited by this paper
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  2007cited by this paper
• Development of new cancer therapeutic agents targeting mitosis

  2006cited by this paper
• Phase I and pharmacokinetic study of the novel oral cell-cycle inhibitor Ro 31-7453 in patients with advanced solid tumors.

  2004cited by this paper
• Phase I and pharmacokinetic study of the new taxane analog BMS-184476 given weekly in patients with advanced malignancies.

  2002cited by this paper
• Anemia in Oncology Practice: Relation to Diseases and Their Therapies

  2002cited by this paper
• Phase II study of the cyclin-dependent kinase inhibitor flavopiridol administered to patients with advanced gastric carcinoma.

  2001cited by this paper
• [New guidelines to evaluate the response to treatment in solid tumors].

  2000cited by this paper
• New guidelines to evaluate the response to treatment in solid tumors. European Organization for Research and Treatment of Cancer, National Cancer Institute of the United States, National Cancer Institute of Canada.

  2000cited by this paper
• Accelerated titration designs for phase I clinical trials in oncology.

  1997cited by this paper

• From code to cancer: CircRNAs and lncRNAs regulate kinesin functions in tumorigenesis.

  2026cites this paper
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  2025cites this paper
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  2025cites this paper
• Kinesin superfamily proteins in ovarian cancer: from molecular mechanisms to clinical applications

  2025cites this paper
• ATAD2 bromodomain in cancer therapy: current status and future perspectives.

  2025cites this paper
• The emerging role of kinesin superfamily proteins in Wnt/β-catenin signaling: Implications for cancer.

  2025cites this paper
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  2025influential citation
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  2024cites this paper
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  2024cites this paper
• Centromeres in cancer: Unraveling the link between chromosomal instability and tumorigenesis

  2024cites this paper
• Recent Progress in Regulating the Activity of Enzymes with Photoswitchable Inhibitors

  2024cites this paper
• CENP-E inhibition induces chromosomal instability and synergizes with diverse microtubule-targeting agents in breast cancer.

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  2024cites this paper
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  2024cites this paper
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  2024cites this paper
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  2024cites this paper
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  2023cites this paper
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  2023cites this paper
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  2023cites this paper
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  2023cites this paper
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  2022cites this paper
• Tetraploidy‐linked sensitization to CENP‐E inhibition in human cells

  2022cites this paper
• [Photopharmacological Tools for Mitotic Cell Division].

  2022cites this paper
• KIF11 is upregulated in colorectal cancer and silencing of it impairs tumor growth and sensitizes colorectal cancer cells to oxaliplatin via p53/GSK3β signaling

  2021cites this paper
• Identification of potential druggable targets of cell cycle with small-molecule inhibitors in oral squamous cell carcinoma

  2021cites this paper
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  2021influential citation
• Inhibiting microcephaly genes as alternative to microtubule targeting agents to treat brain tumors

  2021cites this paper
• Second-Generation Antimitotics in Cancer Clinical Trials

  2021cites this paper
• Future prospects for mitosis-targeted antitumor therapies.

  2021cites this paper
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  2021cites this paper
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  2020cites this paper
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  2020cites this paper
• Tubulin Proteins in Cancer Resistance: A review.

  2020cites this paper
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  2020cites this paper
• Kinesin family members KIF2C/4A/10/11/14/18B/20A/23 predict poor prognosis and promote cell proliferation in hepatocellular carcinoma.

  2020cites this paper
• Kinesin-7 CENP-E regulates cell division, gastrulation and organogenesis in development.

  2020cites this paper
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  2020cites this paper
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  2020cites this paper
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  2019cites this paper
• Mechanisms of kinesin‐7 CENP‐E in kinetochore–microtubule capture and chromosome alignment during cell division

  2019cites this paper
• Regulation and Pharmacology of the Mitotic Kinesin Kif15

  2019cites this paper
• Mitosis inhibitors in anticancer therapy: When blocking the exit becomes a solution.

  2019cites this paper
• Natural products as new antimitotic compounds for anticancer drug development

  2018cites this paper
• CENP‐E as a target for cancer therapy: Where are we now?

  2018cites this paper
• Small Molecules Identified from a Quantitative Drug Combinational Screen Resensitize Cisplatin's Response in Drug-Resistant Ovarian Cancer Cells

  2018cites this paper
• Targeting mitotic pathways for endocrine-related cancer therapeutics.

  2017cites this paper
• Mechanisms of Chromosome Congression during Mitosis

  2017cites this paper
• Anti‐mitotic agents: Are they emerging molecules for cancer treatment?☆

  2017cites this paper
• Clinical Development of Anti-mitotic Drugs in Cancer.

  2017cites this paper
• Mitosis in Animal Cells

  2016cites this paper
• A review of first-in-human small molecule oncology clinical trials

  2016cites this paper
• Review Article A review of first-in-human small molecule oncology clinical trials

  2016cites this paper
• Downregulation of miR-137 and miR-6500-3p promotes cell proliferation in pediatric high-grade gliomas

  2016cites this paper
• KIFC1: a promising chemotherapy target for cancer treatment?

  2016cites this paper
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  2016cites this paper
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  2016cites this paper
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  2016cites this paper
• Aneuploidy generates proteotoxic stress and DNA damage concurrently with p53-mediated post-mitotic apoptosis in SAC-impaired cells

  2015cites this paper
• Clinical Trials of Mitotic Kinesin Inhibitors

  2015cites this paper
• Hitting the brakes: targeting microtubule motors in cancer

  2015cites this paper
• Targeting the Mitotic Catastrophe Signaling Pathway in Cancer

  2015cites this paper
• Non-Small Cell Lung Carcinoma: An Overview on Targeted Therapy.

  2015cites this paper
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  2015cites this paper
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  2015cites this paper
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  2015cites this paper
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  2015cites this paper
• Down-Regulating CENP-E Activity: For Better or for Worse

  2015cites this paper
• Target driven preclinical screening for new antimitotic chemotherapy agents.

  2014cites this paper
• Chemogenetic Evaluation of the Mitotic Kinesin CENP-E Reveals a Critical Role in Triple-Negative Breast Cancer

  2014cites this paper
• Companion Diagnostics and Cancer Biomarkers Chemogenetic Evaluation of the Mitotic Kinesin CENP-E Reveals a Critical Role in Triple-Negative Breast Cancer

  2014cites this paper
• Mitosis-targeting therapies: a troubleshooting guide.

  2013cites this paper
• Antimitotic drugs in cancer chemotherapy: promises and pitfalls.

  2013cites this paper
• Current World Literature

  2013cites this paper
• Mitosis as an anti-cancer drug target

  2013cites this paper
• Synthetic studies of centromere-associated protein-E (CENP-E) inhibitors: 1.Exploration of fused bicyclic core scaffolds using electrostatic potential map.

  2013cites this paper
• Kinesin Spindle Protein (KSP) Inhibitors in Combination with Chemotherapeutic Agents for Cancer Therapy

  2013cites this paper
• Oncogenic role of kinesin proteins and targeting kinesin therapy

  2013cites this paper
• Mitosis-targeted anti-cancer therapies: where they stand

  2012cites this paper
• Kinesins and cancer

  2012cites this paper