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Molecular Cancer Therapeutics
Molecular Cancer Therapeutics
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About the Cover

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The polo-box domain (PBD) has critical roles in the mitotic functions of PLK1. Fragment ligated inhibitory peptides (FLIP) were generated with comparable affinity to peptide PBD inhibitors and possess antiproliferative phenotypes in cells consistent with the observed decrease in PLK1 centrosomal localization. FLIPs induced monopolar and multipolar spindles, in contrast to previously reported small molecule PBD inhibitors that display phenotypes only partially representative of PLK1 knockdown. PBD inhibitors retain high specificity for PLK1 over PLK3 and show the promise of non-ATP competitive kinase inhibitors as antitumor therapeutics. For details, see the article by McInnes and colleagues on page 1683.

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Molecular Cancer Therapeutics: 11 (8)
August 2012
Volume 11, Issue 8
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Issue Highlights

  • Targeting Subcellular Localization through the Polo-Box Domain: Non-ATP Competitive Inhibitors Recapitulate a PLK1 Phenotype
  • MEDI0639: A Novel Therapeutic Antibody Targeting Dll4 Modulates Endothelial Cell Function and Angiogenesis In Vivo
  • A Small-Molecule Inhibitor of Glucose Transporter 1 Downregulates Glycolysis, Induces Cell-Cycle Arrest, and Inhibits Cancer Cell Growth In Vitro and In Vivo
  • Molecular Mechanisms Involved in the Synergistic Interaction of the EZH2 Inhibitor 3-Deazaneplanocin A with Gemcitabine in Pancreatic Cancer Cells
  • Characterization of the Mechanism of Action of the Pan Class I PI3K Inhibitor NVP-BKM120 across a Broad Range of Concentrations
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Molecular Cancer Therapeutics
eISSN: 1538-8514
ISSN: 1535-7163

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