Literature DB >> 36255627

Synthesis and Characterization of Reversible Covalent HDAC4 Inhibitors.

Anton Frühauf1, Benjamin Wolff1, Markus Schweipert1, Franz-Josef Meyer-Almes2.   

Abstract

Cyanoacrylates define a class of inhibitors which are capable to form a transient covalent bond with a cysteine flanking the binding site, thereby increasing the residence time and prolonging the inhibitory effect on the target protein under nonequilibrium conditions. Herein, we describe the synthetic access to cyanoacrylate-based HDAC4 inhibitors and the procedures for the characterization of the transient nature of the covalent bond between cyanoacrylates and thiols or cysteines in HDAC4.
© 2023. The Author(s), under exclusive license to Springer Science+Business Media, LLC, part of Springer Nature.

Entities:  

Keywords:  HDAC4; Histone deacetylase inhibitor; Residence time; Reversibility assays; Reversible covalent inhibitors

Mesh：

Substances：

Year:  2023        PMID： 36255627     DOI： 10.1007/978-1-0716-2788-4_14

Source DB:  PubMed          Journal:  Methods Mol Biol        ISSN： 1064-3745


  18 in total

1.  Potent, Selective, and CNS-Penetrant Tetrasubstituted Cyclopropane Class IIa Histone Deacetylase (HDAC) Inhibitors.

Authors:  Christopher A Luckhurst; Perla Breccia; Andrew J Stott; Omar Aziz; Helen L Birch; Roland W Bürli; Samantha J Hughes; Rebecca E Jarvis; Marieke Lamers; Philip M Leonard; Kim L Matthews; George McAllister; Scott Pollack; Elizabeth Saville-Stones; Grant Wishart; Dawn Yates; Celia Dominguez
Journal:  ACS Med Chem Lett       Date:  2015-12-10       Impact factor: 4.345

2.  Design, synthesis, and biological evaluation of potent and selective class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease.

Authors:  Roland W Bürli; Christopher A Luckhurst; Omar Aziz; Kim L Matthews; Dawn Yates; Kathy A Lyons; Maria Beconi; George McAllister; Perla Breccia; Andrew J Stott; Stephen D Penrose; Michael Wall; Marieke Lamers; Philip Leonard; Ilka Müller; Christine M Richardson; Rebecca Jarvis; Liz Stones; Samantha Hughes; Grant Wishart; Alan F Haughan; Catherine O'Connell; Tania Mead; Hannah McNeil; Julie Vann; John Mangette; Michel Maillard; Vahri Beaumont; Ignacio Munoz-Sanjuan; Celia Dominguez
Journal:  J Med Chem       Date:  2013-12-05       Impact factor: 7.446

Review 3.  Selective class IIa HDAC inhibitors: myth or reality.

Authors:  Eros Di Giorgio; Enrico Gagliostro; Claudio Brancolini
Journal:  Cell Mol Life Sci       Date:  2014-09-05       Impact factor: 9.261

4.  Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group.

Authors:  Mercedes Lobera; Kevin P Madauss; Denise T Pohlhaus; Quentin G Wright; Mark Trocha; Darby R Schmidt; Erkan Baloglu; Ryan P Trump; Martha S Head; Glenn A Hofmann; Monique Murray-Thompson; Benjamin Schwartz; Subhas Chakravorty; Zining Wu; Palwinder K Mander; Laurens Kruidenier; Robert A Reid; William Burkhart; Brandon J Turunen; James X Rong; Craig Wagner; Mary B Moyer; Carrow Wells; Xuan Hong; John T Moore; Jon D Williams; Dulce Soler; Shomir Ghosh; Michael A Nolan
Journal:  Nat Chem Biol       Date:  2013-03-24       Impact factor: 15.040

5.  Identification of novel, selective, and stable inhibitors of class II histone deacetylases. Validation studies of the inhibition of the enzymatic activity of HDAC4 by small molecules as a novel approach for cancer therapy.

Authors:  Jesus M Ontoria; Sergio Altamura; Annalise Di Marco; Federica Ferrigno; Ralph Laufer; Ester Muraglia; Maria Cecilia Palumbi; Michael Rowley; Rita Scarpelli; Carsten Schultz-Fademrecht; Sergio Serafini; Christian Steinkühler; Philip Jones
Journal:  J Med Chem       Date:  2009-11-12       Impact factor: 7.446

6.  Class IIa HDACs repressive activities on MEF2-depedent transcription are associated with poor prognosis of ER⁺ breast tumors.

Authors:  Andrea Clocchiatti; Eros Di Giorgio; Sabrina Ingrao; Franz-Josef Meyer-Almes; Claudio Tripodo; Claudio Brancolini
Journal:  FASEB J       Date:  2012-11-16       Impact factor: 5.191

7.  Evaluation of 5-(Trifluoromethyl)-1,2,4-oxadiazole-Based Class IIa HDAC Inhibitors for Huntington's Disease.

Authors:  Andrew J Stott; Michel C Maillard; Vahri Beaumont; David Allcock; Omar Aziz; Alexander H Borchers; Wesley Blackaby; Perla Breccia; Gillian Creighton-Gutteridge; Alan F Haughan; Rebecca E Jarvis; Christopher A Luckhurst; Kim L Matthews; George McAllister; Scott Pollack; Elizabeth Saville-Stones; Amanda J Van de Poël; Huw D Vater; Julie Vann; Rachel Williams; Dawn Yates; Ignacio Muñoz-Sanjuán; Celia Dominguez
Journal:  ACS Med Chem Lett       Date:  2021-02-11       Impact factor: 4.345

Review 8.  Class IIa HDACs: from important roles in differentiation to possible implications in tumourigenesis.

Authors:  Andrea Clocchiatti; Cristina Florean; Claudio Brancolini
Journal:  J Cell Mol Med       Date:  2011-09       Impact factor: 5.310

Review 9.  HDAC4 as a potential therapeutic target in neurodegenerative diseases: a summary of recent achievements.

Authors:  Michal Mielcarek; Daniel Zielonka; Alisia Carnemolla; Jerzy T Marcinkowski; Fabien Guidez
Journal:  Front Cell Neurosci       Date:  2015-02-24       Impact factor: 5.505

10.  HDAC4 reduction: a novel therapeutic strategy to target cytoplasmic huntingtin and ameliorate neurodegeneration.

Authors:  Michal Mielcarek; Christian Landles; Andreas Weiss; Amyaouch Bradaia; Tamara Seredenina; Linda Inuabasi; Georgina F Osborne; Kristian Wadel; Chrystelle Touller; Rachel Butler; Janette Robertson; Sophie A Franklin; Donna L Smith; Larry Park; Paul A Marks; Erich E Wanker; Eric N Olson; Ruth Luthi-Carter; Herman van der Putten; Vahri Beaumont; Gillian P Bates
Journal:  PLoS Biol       Date:  2013-11-26       Impact factor: 8.029
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