Literature DB >> 22902653

Modulation of cofilin phosphorylation by inhibition of the Lim family kinases.

Liqi He1, Steven P Seitz, George L Trainor, David Tortolani, Wayne Vaccaro, Michael Poss, Christine M Tarby, John S Tokarski, Becky Penhallow, Chen-Yi Hung, Ricardo Attar, Tai-An Lin.   

Abstract

A series of aminothiazoles that are potent inhibitors of LIM kinases 1 and 2 is described. Appropriate choice of substituents led to molecules with good selectivity for either enzyme. An advanced member of the series was shown to effectively interfere with the phosphorylation of the LIM kinases substrate cofilin. Consistent with the important role of the LIM kinases in regulating cytoskeletal structure, treated cells displayed dramatically reduced F-actin content. Published by Elsevier Ltd.

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Year:  2012        PMID: 22902653     DOI: 10.1016/j.bmcl.2012.07.002

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma.

Authors:  Bryce A Harrison; Zheng Y Almstead; Hugh Burgoon; Michael Gardyan; Nicole C Goodwin; Jason Healy; Ying Liu; Ross Mabon; Brett Marinelli; Lakshman Samala; Yulian Zhang; Terry R Stouch; N Andrew Whitlock; Suma Gopinathan; Beth McKnight; Shuli Wang; Nita Patel; Alan G E Wilson; Brian D Hamman; Dennis S Rice; David B Rawlins
Journal:  ACS Med Chem Lett       Date:  2014-11-24       Impact factor: 4.345

2.  Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors.

Authors:  Yan Yin; Ke Zheng; Nibal Eid; Shannon Howard; Ji-Hak Jeong; Fei Yi; Jia Guo; Chul Min Park; Mathieu Bibian; Weilin Wu; Pamela Hernandez; HaJeung Park; Yuntao Wu; Jun-Li Luo; Philip V LoGrasso; Yangbo Feng
Journal:  J Med Chem       Date:  2015-02-04       Impact factor: 7.446

Review 3.  LIM Kinases, Promising but Reluctant Therapeutic Targets: Chemistry and Preclinical Validation In Vivo.

Authors:  Rayan Berabez; Sylvain Routier; Hélène Bénédetti; Karen Plé; Béatrice Vallée
Journal:  Cells       Date:  2022-06-30       Impact factor: 7.666

Review 4.  LIM kinases: cofilin and beyond.

Authors:  Chloé Prunier; Renaud Prudent; Reuben Kapur; Karin Sadoul; Laurence Lafanechère
Journal:  Oncotarget       Date:  2017-06-20

5.  LIM kinase regulation of cytoskeletal dynamics is required for salivary gland branching morphogenesis.

Authors:  Shayoni Ray; Joseph A Fanti; Diego P Macedo; Melinda Larsen
Journal:  Mol Biol Cell       Date:  2014-06-25       Impact factor: 4.138

6.  LIM kinase inhibitors disrupt mitotic microtubule organization and impair tumor cell proliferation.

Authors:  Katerina Mardilovich; Mark Baugh; Diane Crighton; Dominika Kowalczyk; Mads Gabrielsen; June Munro; Daniel R Croft; Filipe Lourenco; Daniel James; Gabriella Kalna; Lynn McGarry; Oliver Rath; Emma Shanks; Mathew J Garnett; Ultan McDermott; Joanna Brookfield; Mark Charles; Tim Hammonds; Michael F Olson
Journal:  Oncotarget       Date:  2015-11-17
  6 in total

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