Literature DB >> 18054239

Phenylalanine-containing hydroxamic acids as selective inhibitors of class IIb histone deacetylases (HDACs).

Stefan Schäfer1, Laura Saunders, Elena Eliseeva, Alfredo Velena, Mira Jung, Andreas Schwienhorst, Anja Strasser, Achim Dickmanns, Ralf Ficner, Sonja Schlimme, Wolfgang Sippl, Eric Verdin, Manfred Jung.   

Abstract

We synthesized biarylalanine-containing hydroxamic acids and tested them on immunoprecipitated HDAC1 and HDAC6 and show a subtype selectivity for HDAC6 that was confirmed in cells by Western blot (tubulin vs histones). We obtained an X-ray structure with a HDAC6-selective inhibitor with the bacterial deacetylase HDAH. Docking studies were carried out using HDAC1 and HDAC6 protein models. Antiproliferative activity was shown on cancer cells for selected compounds.

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Year:  2007        PMID： 18054239     DOI： 10.1016/j.bmc.2007.10.092

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


  15 in total

1.  Dual targeting of histone deacetylase and topoisomerase II with novel bifunctional inhibitors.

Authors:  William Guerrant; Vishal Patil; Joshua C Canzoneri; Adegboyega K Oyelere
Journal:  J Med Chem       Date:  2012-02-13       Impact factor: 7.446

2.  Extending Cross Metathesis To Identify Selective HDAC Inhibitors: Synthesis, Biological Activities, and Modeling.

Authors:  Samuel Bouchet; Camille Linot; Dusan Ruzic; Danica Agbaba; Benoit Fouchaq; Joëlle Roche; Katarina Nikolic; Christophe Blanquart; Philippe Bertrand
Journal:  ACS Med Chem Lett       Date:  2019-05-09       Impact factor: 4.345

Review 3.  Isoform-selective histone deacetylase inhibitors.

Authors:  Anton V Bieliauskas; Mary Kay H Pflum
Journal:  Chem Soc Rev       Date:  2008-05-08       Impact factor: 54.564

4.  Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells.

Authors:  Edwin F de Zoeten; Liqing Wang; Kyle Butler; Ulf H Beier; Tatiana Akimova; Hong Sai; James E Bradner; Ralph Mazitschek; Alan P Kozikowski; Patrick Matthias; Wayne W Hancock
Journal:  Mol Cell Biol       Date:  2011-03-28       Impact factor: 4.272

5.  Design and structure activity relationship of tumor-homing histone deacetylase inhibitors conjugated to folic and pteroic acids.

Authors:  Quaovi H Sodji; James R Kornacki; John F McDonald; Milan Mrksich; Adegboyega K Oyelere
Journal:  Eur J Med Chem       Date:  2015-04-08       Impact factor: 6.514

6.  A proton-shuttle reaction mechanism for histone deacetylase 8 and the catalytic role of metal ions.

Authors:  Ruibo Wu; Shenglong Wang; Nengjie Zhou; Zexing Cao; Yingkai Zhang
Journal:  J Am Chem Soc       Date:  2010-07-14       Impact factor: 15.419

7.  Structural studies of human histone deacetylase 8 and its site-specific variants complexed with substrate and inhibitors.

Authors:  Daniel P Dowling; Stephanie L Gantt; Samuel G Gattis; Carol A Fierke; David W Christianson
Journal:  Biochemistry       Date:  2008-12-23       Impact factor: 3.162

Review 8.  Computational studies on the histone deacetylases and the design of selective histone deacetylase inhibitors.

Authors:  Difei Wang
Journal:  Curr Top Med Chem       Date:  2009       Impact factor: 3.295

Review 9.  Modulation of epigenetic targets for anticancer therapy: clinicopathological relevance, structural data and drug discovery perspectives.

Authors:  Federico Andreoli; Arménio Jorge Moura Barbosa; Marco Daniele Parenti; Alberto Del Rio
Journal:  Curr Pharm Des       Date:  2013       Impact factor: 3.310

Review 10.  HDAC6 as a target for neurodegenerative diseases: what makes it different from the other HDACs?

Authors:  Claudia Simões-Pires; Vincent Zwick; Alessandra Nurisso; Esther Schenker; Pierre-Alain Carrupt; Muriel Cuendet
Journal:  Mol Neurodegener       Date:  2013-01-29       Impact factor: 14.195
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