Literature DB >> 21184800

The polo-like kinase inhibitor BI 2536 exhibits potent activity against malignant plasma cells and represents a novel therapy in multiple myeloma.

Helen J Stewart1, Lyudmila Kishikova, Fiona L Powell, Sally P Wheatley, Timothy J Chevassut.   

Abstract

OBJECTIVE: Polo-like kinase 1 (Plk1) is a regulator of the cell cycle that has been implicated in the pathology of many cancers. We have investigated whether this kinase plays a role in multiple myeloma (MM) using the Plk1 inhibitor BI 2536.
MATERIALS AND METHODS: We have used six MM cell lines and six patient-derived samples to determine the effects of the Plk1 inhibitor, BI 2536, on cell viability, apoptosis, and cytokinesis. We have also examined the effect of the microenvironment on these parameters and the effects of BI 2536 in combination with other antimyeloma agents.
RESULTS: We show that MM cell lines and patient samples express PLK1 and that cell death by apoptosis occurs when Plk1 is inhibited. Cells treated with BI 2536 accumulate in the G(2)/M phase of the cell cycle causing endoduplication. The effects of BI 2536 are not abrogated when cells are cultured on extracellular matrix components, in the presence of interleukin-6, or with bone marrow stromal cells.
CONCLUSIONS: Plk1 inhibition leads to cell death in MM cell lines and patient myeloma samples. Our data suggest that inhibition of Plk1 may have potential use as a therapeutic strategy in multiple myeloma.
Copyright © 2011 ISEH - Society for Hematology and Stem Cells. Published by Elsevier Inc. All rights reserved.

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Year:  2010        PMID: 21184800     DOI: 10.1016/j.exphem.2010.12.006

Source DB:  PubMed          Journal:  Exp Hematol        ISSN: 0301-472X            Impact factor:   3.084


  11 in total

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2.  Kinome-level screening identifies inhibition of polo-like kinase-1 (PLK1) as a target for enhancing non-viral transgene expression.

Authors:  Matthew D Christensen; Jacob J Elmer; Seron Eaton; Laura Gonzalez-Malerva; Joshua LaBaer; Kaushal Rege
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Authors:  María Sol Brassesco; Julia Alejandra Pezuk; Andressa Gois Morales; Jaqueline Carvalho de Oliveira; Gabriela Molinari Roberto; Glenda Nicioli da Silva; Harley Francisco de Oliveira; Carlos Alberto Scrideli; Luiz Gonzaga Tone
Journal:  Cancer Biol Ther       Date:  2013-05-31       Impact factor: 4.742

4.  Microenvironmental influence on pre-clinical activity of polo-like kinase inhibition in multiple myeloma: implications for clinical translation.

Authors:  Douglas W McMillin; Jake Delmore; Joseph Negri; Melissa Ooi; Steffen Klippel; Chandrasekhar V Miduturu; Nathanael S Gray; Paul G Richardson; Kenneth C Anderson; Andrew L Kung; Constantine S Mitsiades
Journal:  PLoS One       Date:  2011-07-07       Impact factor: 3.240

5.  Deficient spindle assembly checkpoint in multiple myeloma.

Authors:  Elena Díaz-Rodríguez; Stela Álvarez-Fernández; Xi Chen; Bruno Paiva; Ricardo López-Pérez; Juan Luis García-Hernández; Jesús F San Miguel; Atanasio Pandiella
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6.  BRD4 associates with p53 in DNMT3A-mutated leukemia cells and is implicated in apoptosis by the bromodomain inhibitor JQ1.

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Review 7.  The therapeutic potential of cell cycle targeting in multiple myeloma.

Authors:  Anke Maes; Eline Menu; Kim De Veirman; Ken Maes; Karin Vand Erkerken; Elke De Bruyne
Journal:  Oncotarget       Date:  2017-06-28

8.  Evaluation of in vitro effects of various targeted drugs on plasma cells and putative neoplastic stem cells in patients with multiple myeloma.

Authors:  Katharina Blatt; Harald Herrmann; Gabriele Stefanzl; Wolfgang R Sperr; Peter Valent
Journal:  Oncotarget       Date:  2016-10-04

9.  Human ABCB1 (P-glycoprotein) and ABCG2 mediate resistance to BI 2536, a potent and selective inhibitor of Polo-like kinase 1.

Authors:  Chung-Pu Wu; Sung-Han Hsiao; Hong-May Sim; Shi-Yu Luo; Wei-Cherng Tuo; Hsing-Wen Cheng; Yan-Qing Li; Yang-Hui Huang; Suresh V Ambudkar
Journal:  Biochem Pharmacol       Date:  2013-08-17       Impact factor: 5.858

Review 10.  Kinase inhibitors as potential agents in the treatment of multiple myeloma.

Authors:  Hanley N Abramson
Journal:  Oncotarget       Date:  2016-12-06
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