Literature DB >> 23743278

Design, synthesis and evaluation of inhibitor of apoptosis protein (IAP) antagonists that are highly selective for the BIR2 domain of XIAP.

Robert J Ardecky1, Kate Welsh, Darren Finlay, Pooi San Lee, Marcos González-López, Santhi Reddy Ganji, Palaniyandi Ravanan, Peter D Mace, Stefan J Riedl, Kristiina Vuori, John C Reed, Nicholas D P Cosford.   

Abstract

We recently reported the systematic ligand-based rational design and synthesis of monovalent Smac mimetics that bind preferentially to the BIR2 domain of the anti-apoptotic protein XIAP. Expanded structure-activity relationship (SAR) studies around these peptidomimetics led to compounds with significantly improved selectivity (>60-fold) for the BIR2 domain versus the BIR3 domain of XIAP. The potent and highly selective IAP antagonist 8q (ML183) sensitized TRAIL-resistant prostate cancer cells to apoptotic cell death, highlighting the merit of this probe compound as a valuable tool to investigate the biology of XIAP.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID： 23743278      PMCID： PMC3772719          DOI： 10.1016/j.bmcl.2013.04.096

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


  21 in total

Review 1.  The hallmarks of cancer.

Authors:  D Hanahan; R A Weinberg
Journal:  Cell       Date:  2000-01-07       Impact factor: 41.582

2.  Cyclopeptide Smac mimetics as antagonists of IAP proteins.

Authors:  Haiying Sun; Liu Liu; Jianfeng Lu; Su Qiu; Chao-Yie Yang; Han Yi; Shaomeng Wang
Journal:  Bioorg Med Chem Lett       Date:  2010-05-15       Impact factor: 2.823

3.  Characterization of dequalinium as a XIAP antagonist that targets the BIR2 domain.

Authors:  Mar Orzáez; Anna Gortat; Mónica Sancho; Rodrigo J Carbajo; Antonio Pineda-Lucena; Yadira Palacios-Rodríguez; Enrique Pérez-Payá
Journal:  Apoptosis       Date:  2011-05       Impact factor: 4.677

Review 4.  Targeting IAP proteins for therapeutic intervention in cancer.

Authors:  Simone Fulda; Domagoj Vucic
Journal:  Nat Rev Drug Discov       Date:  2012-02-01       Impact factor: 84.694

5.  Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.

Authors:  Marcos González-López; Kate Welsh; Darren Finlay; Robert J Ardecky; Santhi Reddy Ganji; Ying Su; Hongbin Yuan; Peter Teriete; Peter D Mace; Stefan J Riedl; Kristiina Vuori; John C Reed; Nicholas D P Cosford
Journal:  Bioorg Med Chem Lett       Date:  2011-05-24       Impact factor: 2.823

6.  Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity.

Authors:  Haiying Sun; Liu Liu; Jianfeng Lu; Longchuan Bai; Xiaoqin Li; Zaneta Nikolovska-Coleska; Donna McEachern; Chao-Yie Yang; Su Qiu; Han Yi; Duxin Sun; Shaomeng Wang
Journal:  J Med Chem       Date:  2011-04-13       Impact factor: 7.446

7.  Expedient synthesis of highly potent antagonists of inhibitor of apoptosis proteins (IAPs) with unique selectivity for ML-IAP.

Authors:  Mitchell Vamos; Kate Welsh; Darren Finlay; Pooi San Lee; Peter D Mace; Scott J Snipas; Monica L Gonzalez; Santhi Reddy Ganji; Robert J Ardecky; Stefan J Riedl; Guy S Salvesen; Kristiina Vuori; John C Reed; Nicholas D P Cosford
Journal:  ACS Chem Biol       Date:  2013-02-05       Impact factor: 5.100

8.  Development and optimization of a binding assay for the XIAP BIR3 domain using fluorescence polarization.

Authors:  Zaneta Nikolovska-Coleska; Renxiao Wang; Xueliang Fang; Hongguang Pan; York Tomita; Peng Li; Peter P Roller; Krzysztof Krajewski; Naoyuki G Saito; Jeanne A Stuckey; Shaomeng Wang
Journal:  Anal Biochem       Date:  2004-09-15       Impact factor: 3.365

Review 9.  IAP antagonists: promising candidates for cancer therapy.

Authors:  Raimund Mannhold; Simone Fulda; Emanuele Carosati
Journal:  Drug Discov Today       Date:  2010-01-21       Impact factor: 7.851

10.  Small-molecule antagonists of apoptosis suppressor XIAP exhibit broad antitumor activity.

Authors:  Aaron D Schimmer; Kate Welsh; Clemencia Pinilla; Zhiliang Wang; Maryla Krajewska; Marie-Josee Bonneau; Irene M Pedersen; Shinichi Kitada; Fiona L Scott; Beatrice Bailly-Maitre; Gennadi Glinsky; Dominick Scudiero; Edward Sausville; Guy Salvesen; Adel Nefzi; John M Ostresh; Richard A Houghten; John C Reed
Journal:  Cancer Cell       Date:  2004-01       Impact factor: 31.743
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  6 in total

1.  Imaging caspase-3 activation as a marker of apoptosis-targeted treatment response in cancer.

Authors:  Delphine L Chen; Jacquelyn T Engle; Elizabeth A Griffin; J Philip Miller; Wenhua Chu; Dong Zhou; Robert H Mach
Journal:  Mol Imaging Biol       Date:  2015-06       Impact factor: 3.488

Review 2.  X-linked inhibitor of apoptosis protein - a critical death resistance regulator and therapeutic target for personalized cancer therapy.

Authors:  Petra Obexer; Michael J Ausserlechner
Journal:  Front Oncol       Date:  2014-07-28       Impact factor: 6.244

Review 3.  NMR-based approaches for the identification and optimization of inhibitors of protein-protein interactions.

Authors:  Elisa Barile; Maurizio Pellecchia
Journal:  Chem Rev       Date:  2014-04-08       Impact factor: 60.622

4.  Development of XIAP Antagonists Based On De Novo 8,5-Fused Bicyclic Lactams.

Authors:  Zhaojun J Sheng; Yiming M Shi; Ximing Xu; Sébastien Bellynck; Kun Zhang; Zhiyun Y Du; Xuetao Xu; François Maurel; Chang-Zhi Dong
Journal:  ChemistryOpen       Date:  2019-01-15       Impact factor: 2.911

5.  Structure based pharmacophore modeling, virtual screening, molecular docking and ADMET approaches for identification of natural anti-cancer agents targeting XIAP protein.

Authors:  Firoz A Dain Md Opo; Mohammed M Rahman; Foysal Ahammad; Istiak Ahmed; Mohiuddin Ahmed Bhuiyan; Abdullah M Asiri
Journal:  Sci Rep       Date:  2021-02-18       Impact factor: 4.379

6.  Characterization of Potent SMAC Mimetics that Sensitize Cancer Cells to TNF Family-Induced Apoptosis.

Authors:  Kate Welsh; Snezana Milutinovic; Robert J Ardecky; Marcos Gonzalez-Lopez; Santhi Reddy Ganji; Peter Teriete; Darren Finlay; Stefan Riedl; Shu-Ichi Matsuzawa; Clemencia Pinilla; Richard Houghten; Kristiina Vuori; John C Reed; Nicholas D P Cosford
Journal:  PLoS One       Date:  2016-09-12       Impact factor: 3.240
  6 in total

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