Literature DB >> 17942892

Nek2 as an effective target for inhibition of tumorigenic growth and peritoneal dissemination of cholangiocarcinoma.

Toshio Kokuryo1, Takeshi Senga, Yukihiro Yokoyama, Masato Nagino, Yuji Nimura, Michinari Hamaguchi.   

Abstract

We investigated the role of Nek2, a member of the serine/threonine kinase family, Nek, in the tumorigenic growth of cholangiocarcinoma cells. Expression of Nek2 is elevated in cholangiocarcinoma in a tumor-specific manner as compared with that of normal fibroblast cells. Expression of exogenous Nek2 did not perturb the growth of cholangiocarcinoma cells, whereas suppression of the Nek2 expression with siRNA resulted in the inhibition of cell proliferation and induced cell death. In xenograft-nude mouse model, s.c. injection of Nek2 siRNA around the tumor nodules resulted in reduction of tumor size as compared with those of control siRNA injection. In peritoneal dissemination model, Nek2 siRNA-treated mice showed statistically longer survival periods in comparison with those of the control siRNA-treated mice. Taken together, our data indicate a pivotal role of Nek2 in tumorigenic growth of cholangiocarcinoma.

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Year:  2007        PMID: 17942892     DOI: 10.1158/0008-5472.CAN-07-1489

Source DB:  PubMed          Journal:  Cancer Res        ISSN: 0008-5472            Impact factor:   12.701


  40 in total

1.  The NIMA-family kinase Nek3 regulates microtubule acetylation in neurons.

Authors:  Jufang Chang; Robert H Baloh; Jeffrey Milbrandt
Journal:  J Cell Sci       Date:  2009-06-09       Impact factor: 5.285

2.  Local depletion of DNA methylation identifies a repressive p53 regulatory region in the NEK2 promoter.

Authors:  Nancy H Nabilsi; Daniel J Ryder; Ashley C Peraza-Penton; Rosha Poudyal; David S Loose; Michael P Kladde
Journal:  J Biol Chem       Date:  2013-10-25       Impact factor: 5.157

Review 3.  Role of E2Fs and mitotic regulators controlled by E2Fs in the epithelial to mesenchymal transition.

Authors:  Shirley Jusino; Harold I Saavedra
Journal:  Exp Biol Med (Maywood)       Date:  2019-10-01

Review 4.  Targeting NEK2 as a promising therapeutic approach for cancer treatment.

Authors:  Yanfen Fang; Xiongwen Zhang
Journal:  Cell Cycle       Date:  2016       Impact factor: 4.534

5.  Discovery of potent NEK2 inhibitors as potential anticancer agents using structure-based exploration of NEK2 pharmacophoric space coupled with QSAR analyses.

Authors:  Mohammad A Khanfar; Fahmy Banat; Shada Alabed; Saja Alqtaishat
Journal:  Mol Divers       Date:  2016-09-06       Impact factor: 2.943

6.  Aminopyrazine inhibitors binding to an unusual inactive conformation of the mitotic kinase Nek2: SAR and structural characterization.

Authors:  Daniel K Whelligan; Savade Solanki; Dawn Taylor; Douglas W Thomson; Kwai-Ming J Cheung; Kathy Boxall; Corine Mas-Droux; Caterina Barillari; Samantha Burns; Charles G Grummitt; Ian Collins; Rob L M van Montfort; G Wynne Aherne; Richard Bayliss; Swen Hoelder
Journal:  J Med Chem       Date:  2010-11-11       Impact factor: 7.446

7.  Abnormal expression of Nek2 in pancreatic ductal adenocarcinoma: a novel marker for prognosis.

Authors:  Zhen Ning; Aman Wang; Jinxiao Liang; Jiwei Liu; Tao Zhou; Qiu Yan; Zhongyu Wang
Journal:  Int J Clin Exp Pathol       Date:  2014-04-15

Review 8.  Therapeutic melting pot of never in mitosis gene a related kinase 2 (Nek2): a perspective on Nek2 as an oncology target and recent advancements in Nek2 small molecule inhibition.

Authors:  Brendan Frett; Robert V Brown; Mingliang Ma; Wenhao Hu; Haiyong Han; Hong-yu Li
Journal:  J Med Chem       Date:  2014-02-25       Impact factor: 7.446

9.  Novel small molecules disrupting Hec1/Nek2 interaction ablate tumor progression by triggering Nek2 degradation through a death-trap mechanism.

Authors:  C-M Hu; J Zhu; X E Guo; W Chen; X-L Qiu; B Ngo; R Chien; Y V Wang; C Y Tsai; G Wu; Y Kim; R Lopez; A R Chamberlin; E Y-H P Lee; W-H Lee
Journal:  Oncogene       Date:  2014-03-24       Impact factor: 9.867

10.  Insights into the conformational variability and regulation of human Nek2 kinase.

Authors:  Isaac Westwood; Donna-Marie Cheary; Joanne E Baxter; Mark W Richards; Rob L M van Montfort; Andrew M Fry; Richard Bayliss
Journal:  J Mol Biol       Date:  2008-12-24       Impact factor: 5.469

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