Literature DB >> 26723891

Screening and profiling assays for HDACs and sirtuins.

Konrad T Howitz1.   

Abstract

Epigenetic factors are enzymes or proteins that confer, remove or recognize covalent modifications to chromatin DNA or proteins. They can be divided into three broad groups, commonly referred to as the 'writers', 'erasers' and 'readers'. The HDACs and sirtuins, which remove acetyl groups from the ɛ-amino of protein lysine residues, fall into the 'eraser' category. Due to their important effects on gene expression and involvement in various disease states, these enzymes have been the subjects of many assay development efforts in recent years. Commonly used techniques include mass spectrometry, antibody-based methods and protease-coupled assays with fluorogenic peptide substrates. Recent advances include the development of synthetic substrates for the assay of various newly discovered non-acetyl deacylation activities among the sirtuins.
Copyright © 2015 Elsevier Ltd. All rights reserved.

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Year:  2015        PMID: 26723891     DOI: 10.1016/j.ddtec.2015.10.008

Source DB:  PubMed          Journal:  Drug Discov Today Technol        ISSN: 1740-6749


  4 in total

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Authors:  Elisabetta Di Bello; Beatrice Noce; Rossella Fioravanti; Clemens Zwergel; Sergio Valente; Dante Rotili; Giulia Fianco; Daniela Trisciuoglio; Marina M Mourão; Policarpo Sales; Suzanne Lamotte; Eric Prina; Gerald F Späth; Cécile Häberli; Jennifer Keiser; Antonello Mai
Journal:  ACS Infect Dis       Date:  2022-06-22       Impact factor: 5.578

2.  A Comparative Study of Target Engagement Assays for HDAC1 Inhibitor Profiling.

Authors:  Rosita R Asawa; Alexey Zakharov; Taylor Niehoff; Ata Chitsaz; Ajit Jadhav; Mark J Henderson; Anton Simeonov; Natalia J Martinez
Journal:  SLAS Discov       Date:  2019-10-29       Impact factor: 3.341

3.  Chemo-proteomics exploration of HDAC degradability by small molecule degraders.

Authors:  Yuan Xiong; Katherine A Donovan; Nicholas A Eleuteri; Nadia Kirmani; Hong Yue; Anthony Razov; Noah M Krupnick; Radosław P Nowak; Eric S Fischer
Journal:  Cell Chem Biol       Date:  2021-07-26       Impact factor: 9.039

4.  Reconstitution of Mammalian Enzymatic Deacylation Reactions in Live Bacteria Using Native Acylated Substrates.

Authors:  Emanuel M Avrahami; Shahar Levi; Eyal Zajfman; Clil Regev; Oshrit Ben-David; Eyal Arbely
Journal:  ACS Synth Biol       Date:  2018-09-18       Impact factor: 5.110

  4 in total

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