Literature DB >> 15261294

Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.

Vasudha Sharma1, Jetze J Tepe.   

Abstract

The marine sponge metabolite hymenialdisine is a potent inhibitor of a variety of kinases including MEK-1, GSK-3 beta, and CK1. In addition, hymenialdisine and debromohymenialdisine exhibit inhibition of the G(2) cell cycle checkpoint at micromolar concentrations. We report herein the potent inhibition of cell cycle kinase Chk2 by the indolic-hymenialdisine indoloazepine 1 (IC(50)=8 nM).

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Year:  2004        PMID： 15261294     DOI： 10.1016/j.bmcl.2004.05.079

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


  15 in total

1.  Trans-activation of the DNA-damage signalling protein kinase Chk2 by T-loop exchange.

Authors:  Antony W Oliver; Angela Paul; Katherine J Boxall; S Elaine Barrie; G Wynne Aherne; Michelle D Garrett; Sibylle Mittnacht; Laurence H Pearl
Journal:  EMBO J       Date:  2006-06-22       Impact factor: 11.598

2.  Crystal structure of checkpoint kinase 2 in complex with NSC 109555, a potent and selective inhibitor.

Authors:  George T Lountos; Joseph E Tropea; Di Zhang; Andrew G Jobson; Yves Pommier; Robert H Shoemaker; David S Waugh
Journal:  Protein Sci       Date:  2009-01       Impact factor: 6.725

Review 3.  Structure-based design, discovery and development of checkpoint kinase inhibitors as potential anticancer therapies.

Authors:  Thomas P Matthews; Alan M Jones; Ian Collins
Journal:  Expert Opin Drug Discov       Date:  2013-04-18       Impact factor: 6.098

4.  Cellular inhibition of checkpoint kinase 2 (Chk2) and potentiation of camptothecins and radiation by the novel Chk2 inhibitor PV1019 [7-nitro-1H-indole-2-carboxylic acid {4-[1-(guanidinohydrazone)-ethyl]-phenyl}-amide].

Authors:  Andrew G Jobson; George T Lountos; Philip L Lorenzi; Jenny Llamas; John Connelly; David Cerna; Joseph E Tropea; Akikazu Onda; Gabriele Zoppoli; Sudhir Kondapaka; Guangtao Zhang; Natasha J Caplen; John H Cardellina; Stephen S Yoo; Anne Monks; Christopher Self; David S Waugh; Robert H Shoemaker; Yves Pommier
Journal:  J Pharmacol Exp Ther       Date:  2009-09-09       Impact factor: 4.030

Review 5.  ATM, ATR, CHK1, CHK2 and WEE1 inhibitors in cancer and cancer stem cells.

Authors:  Cyril Ronco; Anthony R Martin; Luc Demange; Rachid Benhida
Journal:  Medchemcomm       Date:  2016-11-30       Impact factor: 3.597

6.  Methyl 3-(1H-indole-3-carboxamido)propionate hemihydrate.

Authors:  Gang Huang; Xing Yan Xu; Xiang Chao Zeng; Le Zheng; Kai Ping Li
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-05-26

7.  Methyl 2-(1H-indole-3-carboxamido)-acetate.

Authors:  Fang Hu; Le Zheng; Xiang Chao Zeng; Kai Ping Li
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-02-26

8.  Methyl 3-[(1-butyl-1H-indol-3-yl)carbonyl-amino]propionate.

Authors:  Gang Huang; Xing Yan Xu; Xiang Chao Zeng; Gui Hong Tang; Dong Dong Li
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2009-08-08

9.  ATM and Chk2 kinase target the p53 cofactor Strap.

Authors:  Cassandra J Adams; Anne L Graham; Martin Jansson; Amanda S Coutts; Mariola Edelmann; Linda Smith; Benedikt Kessler; Nicholas B La Thangue
Journal:  EMBO Rep       Date:  2008-10-03       Impact factor: 8.807

10.  Fragment-based screening maps inhibitor interactions in the ATP-binding site of checkpoint kinase 2.

Authors:  M Cris Silva-Santisteban; Isaac M Westwood; Kathy Boxall; Nathan Brown; Sam Peacock; Craig McAndrew; Elaine Barrie; Meirion Richards; Amin Mirza; Antony W Oliver; Rosemary Burke; Swen Hoelder; Keith Jones; G Wynne Aherne; Julian Blagg; Ian Collins; Michelle D Garrett; Rob L M van Montfort
Journal:  PLoS One       Date:  2013-06-12       Impact factor: 3.240
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