Literature DB >> 24457091

Degrasyn-like symmetrical compounds: possible therapeutic agents for multiple myeloma (MM-I).

Zhenghong Peng1, David S Maxwell1, Duoli Sun1, Basvoju A Bhanu Prasad1, Paul T Schuber1, Ashutosh Pal2, Yunming Ying2, Dongmei Han2, Liwei Gao2, Shimei Wang2, Alexander Levitzki3, Vaibhav Kapuria4, Moshe Talpaz4, Matthew Young5, Hollis D Showalter6, Nicholas J Donato4, William G Bornmann7.   

Abstract

A series of degrasyn-like symmetrical compounds have been designed, synthesized, and screened against B cell malignancy (multiple myeloma, mantle cell lymphoma) cell lines. The lead compounds T5165804 and CP2005 showed higher nanomolar potency against these tumor cells in comparison to degrasyn and inhibited Usp9x activity in vitro and in intact cells. These observations suggest that this new class of compounds holds promise as cancer therapeutic agents.
Copyright © 2014. Published by Elsevier Ltd.

Entities:  

Keywords:  Degrasyn; Inhibitors; Jak2/Stat3; Multiple myeloma; Small molecules; Synthesis

Mesh：

Substances：

Year:  2014        PMID： 24457091      PMCID： PMC4158738          DOI： 10.1016/j.bmc.2013.12.048

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  19 in total

1.  Mcl1 becomes ubiquitin-ous: new opportunities to antagonize a pro-survival protein.

Authors:  Michael D Hogarty
Journal:  Cell Res       Date:  2010-04       Impact factor: 25.617

2.  Tyrphostin-like compounds with ubiquitin modulatory activity as possible therapeutic agents for multiple myeloma.

Authors:  Zhenghong Peng; Ashutosh Pal; Dongmei Han; Shimei Wang; David Maxwell; Alexander Levitzki; Moshe Talpaz; Nicholas J Donato; William Bornmann
Journal:  Bioorg Med Chem       Date:  2011-10-07       Impact factor: 3.641

3.  Deubiquitinase USP9X stabilizes MCL1 and promotes tumour cell survival.

Authors:  Martin Schwickart; Xiaodong Huang; Jennie R Lill; Jinfeng Liu; Ronald Ferrando; Dorothy M French; Heather Maecker; Karen O'Rourke; Fernando Bazan; Jeffrey Eastham-Anderson; Peng Yue; David Dornan; David C S Huang; Vishva M Dixit
Journal:  Nature       Date:  2009-12-20       Impact factor: 49.962

4.  Activity profiling of deubiquitinating enzymes in cervical carcinoma biopsies and cell lines.

Authors:  Ulrika Rolén; Vera Kobzeva; Natalja Gasparjan; Huib Ovaa; Gösta Winberg; Fjodor Kisseljov; Maria G Masucci
Journal:  Mol Carcinog       Date:  2006-04       Impact factor: 4.784

Review 5.  Deubiquitinases in cancer: new functions and therapeutic options.

Authors:  J M Fraile; V Quesada; D Rodríguez; J M P Freije; C López-Otín
Journal:  Oncogene       Date:  2011-09-26       Impact factor: 9.867

6.  Deubiquitinase USP9x confers radioresistance through stabilization of Mcl-1.

Authors:  Donatella Trivigno; Frank Essmann; Stephan M Huber; Justine Rudner
Journal:  Neoplasia       Date:  2012-10       Impact factor: 5.715

7.  Tyrenes: synthesis of new antiproliferative compounds with an extended conjugation.

Authors:  Peter Demin; Olga Rounova; Thomas Grunberger; Lorand Cimpean; Nigel Sharfe; Chaim M Roifman
Journal:  Bioorg Med Chem       Date:  2004-06-01       Impact factor: 3.641

8.  WP1066, a novel JAK2 inhibitor, suppresses proliferation and induces apoptosis in erythroid human cells carrying the JAK2 V617F mutation.

Authors:  Srdan Verstovsek; Taghi Manshouri; Alfonso Quintás-Cardama; David Harris; Jorge Cortes; Francis J Giles; Hagop Kantarjian; Waldemar Priebe; Zeev Estrov
Journal:  Clin Cancer Res       Date:  2008-02-01       Impact factor: 12.531

Review 9.  Ubiquitin - omics reveals novel networks and associations with human disease.

Authors:  Benedikt M Kessler
Journal:  Curr Opin Chem Biol       Date:  2013-01-19       Impact factor: 8.822

10.  The downregulation of Mcl-1 via USP9X inhibition sensitizes solid tumors to Bcl-xl inhibition.

Authors:  Chander Peddaboina; Daniel Jupiter; Steven Fletcher; Jeremy L Yap; Arun Rai; Richard P Tobin; Weihua Jiang; Philip Rascoe; M Karen Newell Rogers; W Roy Smythe; Xiaobo Cao
Journal:  BMC Cancer       Date:  2012-11-21       Impact factor: 4.430
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  3 in total

1.  Deubiquitinase inhibition by WP1130 leads to ULK1 aggregation and blockade of autophagy.

Authors:  Stefan Drießen; Niklas Berleth; Olena Friesen; Antje S Löffler; Philip Böhler; Nora Hieke; Fabian Stuhldreier; Christoph Peter; Kay O Schink; Sebastian W Schultz; Harald Stenmark; Petter Holland; Anne Simonsen; Sebastian Wesselborg; Björn Stork
Journal:  Autophagy       Date:  2015       Impact factor: 16.016

2.  Anti-infective Activity of 2-Cyano-3-Acrylamide Inhibitors with Improved Drug-Like Properties against Two Intracellular Pathogens.

Authors:  Karla D Passalacqua; Marie-Eve Charbonneau; Nicholas J Donato; Hollis D Showalter; Duxin Sun; Bo Wen; Miao He; Hanshi Sun; Mary X D O'Riordan; Christiane E Wobus
Journal:  Antimicrob Agents Chemother       Date:  2016-06-20       Impact factor: 5.191

3.  USP9X destabilizes pVHL and promotes cell proliferation.

Authors:  Cong Zhang; Zuohan Peng; Minglu Zhu; Penglong Wang; Xiao Du; Xiang Li; Yu Liu; Yan Jin; Michael A McNutt; Yuxin Yin
Journal:  Oncotarget       Date:  2016-09-13
  3 in total

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