Literature DB >> 24900464

Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.

James E Dowling1, Claudio Chuaqui1, Timothy W Pontz1, Paul D Lyne1, Nicholas A Larsen1, Michael H Block1, Huawei Chen1, Nancy Su1, Allan Wu1, Daniel Russell1, Hannah Pollard1, John W Lee1, Bo Peng1, Kumar Thakur1, Qing Ye1, Tao Zhang1, Patrick Brassil1, Vicki Racicot1, Larry Bao1, Christopher R Denz1, Emma Cooke1.   

Abstract

In this paper we describe a series of 3-cyano-5-aryl-7-aminopyrazolo[1,5-a]pyrimidine hits identified by kinase-focused subset screening as starting points for the structure-based design of conformationally constrained 6-acetamido-indole inhibitors of CK2. The synthesis, SAR, and effects of this novel series on Akt signaling and cell proliferation in vitro are described.

Entities:  

Keywords:  CK2; casein kinase; pyrazolo[1,5-a]pyrimidine; structure-based design

Year:  2012        PMID： 24900464      PMCID： PMC4025639          DOI： 10.1021/ml200257n

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  17 in total

Review 1.  Protein kinase CK2: a challenge to canons.

Authors:  Lorenzo A Pinna
Journal:  J Cell Sci       Date:  2002-10-15       Impact factor: 5.285

2.  Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.

Authors:  Zhe Nie; Carin Perretta; Philip Erickson; Stephen Margosiak; Robert Almassy; Jia Lu; April Averill; Kraig M Yager; Shaosong Chu
Journal:  Bioorg Med Chem Lett       Date:  2007-05-18       Impact factor: 2.823

Review 3.  Too much of a good thing: the role of protein kinase CK2 in tumorigenesis and prospects for therapeutic inhibition of CK2.

Authors:  James S Duncan; David W Litchfield
Journal:  Biochim Biophys Acta       Date:  2007-08-30

4.  A quantitative analysis of kinase inhibitor selectivity.

Authors:  Mazen W Karaman; Sanna Herrgard; Daniel K Treiber; Paul Gallant; Corey E Atteridge; Brian T Campbell; Katrina W Chan; Pietro Ciceri; Mindy I Davis; Philip T Edeen; Raffaella Faraoni; Mark Floyd; Jeremy P Hunt; Daniel J Lockhart; Zdravko V Milanov; Michael J Morrison; Gabriel Pallares; Hitesh K Patel; Stephanie Pritchard; Lisa M Wodicka; Patrick P Zarrinkar
Journal:  Nat Biotechnol       Date:  2008-01       Impact factor: 54.908

Review 5.  Protein kinases. 4. Protein kinase CK2: an enzyme with multiple substrates and a puzzling regulation.

Authors:  J E Allende; C C Allende
Journal:  FASEB J       Date:  1995-03       Impact factor: 5.191

Review 6.  Addiction to protein kinase CK2: a common denominator of diverse cancer cells?

Authors:  Maria Ruzzene; Lorenzo A Pinna
Journal:  Biochim Biophys Acta       Date:  2009-08-06

7.  Dephosphorylation and inactivation of Akt/PKB is counteracted by protein kinase CK2 in HEK 293T cells.

Authors:  Giovanni Di Maira; Francesca Brustolon; Lorenzo A Pinna; Maria Ruzzene
Journal:  Cell Mol Life Sci       Date:  2009-08-08       Impact factor: 9.261

8.  Induction of apoptosis by antisense CK2 in human prostate cancer xenograft model.

Authors:  Joel W Slaton; Gretchen M Unger; Daniel T Sloper; Alan T Davis; Khalil Ahmed
Journal:  Mol Cancer Res       Date:  2004-12       Impact factor: 5.852

9.  The alpha catalytic subunit of protein kinase CK2 is required for mouse embryonic development.

Authors:  David Y Lou; Isabel Dominguez; Paul Toselli; Esther Landesman-Bollag; Conor O'Brien; David C Seldin
Journal:  Mol Cell Biol       Date:  2007-10-22       Impact factor: 4.272

Review 10.  Protein kinase CK2 in health and disease: Structural bases of protein kinase CK2 inhibition.

Authors:  R Battistutta
Journal:  Cell Mol Life Sci       Date:  2009-06       Impact factor: 9.261
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  9 in total

1.  Small Molecule Amyloid-β Protein Precursor Processing Modulators Lower Amyloid-β Peptide Levels via cKit Signaling.

Authors:  Ci-Di Chen; Ella Zeldich; Christina Khodr; Kaddy Camara; Tze Yu Tung; Emma C Lauder; Patrick Mullen; Taryn J Polanco; Yen-Yu Liu; Dean Zeldich; Weiming Xia; William E Van Nostrand; Lauren E Brown; John A Porco; Carmela R Abraham
Journal:  J Alzheimers Dis       Date:  2019       Impact factor: 4.472

Review 2.  Targeted regulation of PI3K/Akt/mTOR/NF-κB signaling by indole compounds and their derivatives: mechanistic details and biological implications for cancer therapy.

Authors:  Aamir Ahmad; Bernhard Biersack; Yiwei Li; Dejuan Kong; Bin Bao; Rainer Schobert; Subhash B Padhye; Fazlul H Sarkar
Journal:  Anticancer Agents Med Chem       Date:  2013-09       Impact factor: 2.505

3.  Potent and Selective CK2 Kinase Inhibitors with Effects on Wnt Pathway Signaling in Vivo.

Authors:  James E Dowling; Marat Alimzhanov; Larry Bao; Claudio Chuaqui; Christopher R Denz; Emma Jenkins; Nicholas A Larsen; Paul D Lyne; Timothy Pontz; Qing Ye; Geoff A Holdgate; Lindsay Snow; Nichole O'Connell; Andrew D Ferguson
Journal:  ACS Med Chem Lett       Date:  2016-01-20       Impact factor: 4.345

4.  Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo.

Authors:  James E Dowling; Marat Alimzhanov; Larry Bao; Michael H Block; Claudio Chuaqui; Emma L Cooke; Christopher R Denz; Alex Hird; Shan Huang; Nicholas A Larsen; Bo Peng; Timothy W Pontz; Caroline Rivard-Costa; Jamal Carlos Saeh; Kumar Thakur; Qing Ye; Tao Zhang; Paul D Lyne
Journal:  ACS Med Chem Lett       Date:  2013-07-03       Impact factor: 4.345

5.  A public-private partnership to unlock the untargeted kinome.

Authors:  Stefan Knapp; Paulo Arruda; Julian Blagg; Stephen Burley; David H Drewry; Aled Edwards; Doriano Fabbro; Paul Gillespie; Nathanael S Gray; Bernhard Kuster; Karen E Lackey; Paulo Mazzafera; Nicholas C O Tomkinson; Timothy M Willson; Paul Workman; William J Zuercher
Journal:  Nat Chem Biol       Date:  2013-01       Impact factor: 15.040

6.  Development of a potent and selective chemical probe for the pleiotropic kinase CK2.

Authors:  Carrow I Wells; David H Drewry; Julie E Pickett; Amelie Tjaden; Andreas Krämer; Susanne Müller; Laszlo Gyenis; Daniel Menyhart; David W Litchfield; Stefan Knapp; Alison D Axtman
Journal:  Cell Chem Biol       Date:  2021-01-22       Impact factor: 8.116

7.  Exploring the Pivotal Role of the CK2 Hinge Region Sub-Pocket in Binding with Tricyclic Quinolone Analogues by Computational Analysis.

Authors:  Yue Zhou; Na Zhang; Shan Tang; Xiaoqian Qi; Lijiao Zhao; Rugang Zhong; Yongzhen Peng
Journal:  Molecules       Date:  2017-05-19       Impact factor: 4.411

8.  Host Kinase CSNK2 is a Target for Inhibition of Pathogenic SARS-like β-Coronaviruses.

Authors:  Xuan Yang; Rebekah J Dickmander; Armin Bayati; Sharon A Taft-Benz; Jeffery L Smith; Carrow I Wells; Emily A Madden; Jason W Brown; Erik M Lenarcic; Boyd L Yount; Edcon Chang; Alison D Axtman; Ralph S Baric; Mark T Heise; Peter S McPherson; Nathaniel J Moorman; Timothy M Willson
Journal:  ACS Chem Biol       Date:  2022-06-19       Impact factor: 4.634

Review 9.  Downfalls of Chemical Probes Acting at the Kinase ATP-Site: CK2 as a Case Study.

Authors:  Eleanor L Atkinson; Jessica Iegre; Paul D Brear; Elizabeth A Zhabina; Marko Hyvönen; David R Spring
Journal:  Molecules       Date:  2021-03-31       Impact factor: 4.411
  9 in total

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