Literature DB >> 35187421

Comparison of Cellular Target Engagement Methods for the Tubulin Deacetylases Sirt2 and HDAC6: NanoBRET, CETSA, Tubulin Acetylation, and PROTACs.

Anja Vogelmann1, Manfred Jung1, Finn K Hansen2, Matthias Schiedel3.   

Abstract

The tubulin deacetylases Sirt2 and HDAC6 have been associated with the development of various diseases. Herein, we discuss recent approaches that enable cellular target engagement studies for these deacetylases and thus play a critical role in the evaluation of small molecule inhibitors of Sirt2 or HDAC6 as potential therapeutic agents.
© 2022 The Authors. Published by American Chemical Society.

Entities:  

Year:  2022        PMID： 35187421      PMCID： PMC8844959          DOI： 10.1021/acsptsci.2c00004

Source DB:  PubMed          Journal:  ACS Pharmacol Transl Sci        ISSN： 2575-9108


  10 in total

1.  HDAC6 is a microtubule-associated deacetylase.

Authors:  Charlotte Hubbert; Amaris Guardiola; Rong Shao; Yoshiharu Kawaguchi; Akihiro Ito; Andrew Nixon; Minoru Yoshida; Xiao-Fan Wang; Tso-Pang Yao
Journal:  Nature       Date:  2002-05-23       Impact factor: 49.962

2.  The human Sir2 ortholog, SIRT2, is an NAD+-dependent tubulin deacetylase.

Authors:  Brian J North; Brett L Marshall; Margie T Borra; John M Denu; Eric Verdin
Journal:  Mol Cell       Date:  2003-02       Impact factor: 17.970

Review 3.  A Review of Progress in Histone Deacetylase 6 Inhibitors Research: Structural Specificity and Functional Diversity.

Authors:  Xin-Hui Zhang; Hui-Pan Wu; Mussa Yussuf Khamis; Yi-Han Li; Li-Ying Ma; Hong-Min Liu
Journal:  J Med Chem       Date:  2021-02-01       Impact factor: 7.446

4.  Importance of Quantifying Drug-Target Engagement in Cells.

Authors:  Jakub Stefaniak; Kilian V M Huber
Journal:  ACS Med Chem Lett       Date:  2020-03-06       Impact factor: 4.345

5.  Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals).

Authors:  Matthias Schiedel; Daniel Herp; Sören Hammelmann; Sören Swyter; Attila Lehotzky; Dina Robaa; Judit Oláh; Judit Ovádi; Wolfgang Sippl; Manfred Jung
Journal:  J Med Chem       Date:  2017-04-17       Impact factor: 7.446

6.  Development of Selective Histone Deacetylase 6 (HDAC6) Degraders Recruiting Von Hippel-Lindau (VHL) E3 Ubiquitin Ligase.

Authors:  Ka Yang; Hao Wu; Zhongrui Zhang; Eric D Leisten; Xueqing Nie; Binkai Liu; Zhi Wen; Jing Zhang; Michael D Cunningham; Weiping Tang
Journal:  ACS Med Chem Lett       Date:  2020-03-18       Impact factor: 4.345

7.  Design, Synthesis, and Biological Evaluation of Quinazolin-4-one-Based Hydroxamic Acids as Dual PI3K/HDAC Inhibitors.

Authors:  Ashish Thakur; Gregory J Tawa; Mark J Henderson; Carina Danchik; Suiyang Liu; Pranav Shah; Amy Q Wang; Garrett Dunn; Md Kabir; Elias C Padilha; Xin Xu; Anton Simeonov; Surender Kharbanda; Richard Stone; Gurmit Grewal
Journal:  J Med Chem       Date:  2020-04-08       Impact factor: 7.446

8.  The HDAC6/8/10 inhibitor TH34 induces DNA damage-mediated cell death in human high-grade neuroblastoma cell lines.

Authors:  Fiona R Kolbinger; Emily Koeneke; Johannes Ridinger; Tino Heimburg; Michael Müller; Theresa Bayer; Wolfgang Sippl; Manfred Jung; Nikolas Gunkel; Aubry K Miller; Frank Westermann; Olaf Witt; Ina Oehme
Journal:  Arch Toxicol       Date:  2018-06-09       Impact factor: 5.153

9.  Hydroxamic Acids Immobilized on Resins (HAIRs): Synthesis of Dual-Targeting HDAC Inhibitors and HDAC Degraders (PROTACs).

Authors:  Laura Sinatra; Jan J Bandolik; Martin Roatsch; Melf Sönnichsen; Clara T Schoeder; Alexandra Hamacher; Andrea Schöler; Arndt Borkhardt; Jens Meiler; Sanil Bhatia; Matthias U Kassack; Finn K Hansen
Journal:  Angew Chem Int Ed Engl       Date:  2020-10-09       Impact factor: 15.336
  10 in total
  3 in total

1.  Virtual Special Issue: Epigenetics 2022.

Authors:  Courtney C Aldrich; Félix Calderón; Stuart J Conway; Chuan He; Jacob M Hooker; Donna M Huryn; Craig W Lindsley; Dennis C Liotta; Christa E Müller
Journal:  ACS Pharmacol Transl Sci       Date:  2022-09-09

2.  Virtual Special Issue: Epigenetics 2022.

Authors:  Courtney C Aldrich; Félix Calderón; Stuart J Conway; Chuan He; Jacob M Hooker; Donna M Huryn; Craig W Lindsley; Dennis C Liotta; Christa E Müller
Journal:  ACS Med Chem Lett       Date:  2022-10-13       Impact factor: 4.632

3.  Real-Time Cellular Thermal Shift Assay to Monitor Target Engagement.

Authors:  Tino W Sanchez; Michael H Ronzetti; Ashley E Owens; Maria Antony; Ty Voss; Eric Wallgren; Daniel Talley; Krishna Balakrishnan; Sebastian E Leyes Porello; Ganesha Rai; Juan J Marugan; Samuel G Michael; Bolormaa Baljinnyam; Noel Southall; Anton Simeonov; Mark J Henderson
Journal:  ACS Chem Biol       Date:  2022-09-01       Impact factor: 4.634
  3 in total

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