The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes-Reference-Cited by-同舟云学术

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The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes

Published:2014 Issue:3 Volume:5 Page:342-351
ISSN:2040-2503
Container-title:MedChemComm
language:en
Short-container-title:Med. Chem. Commun.

Author:

Atkinson Stephen J.¹²³⁴,Soden Peter E.¹²³⁴,Angell Davina C.¹²³⁴,Bantscheff Marcus⁵⁶²⁷⁸,Chung Chun-wa⁹¹⁰²¹¹³,Giblin Kathryn A.¹²³⁴,Smithers Nicholas¹²³⁴,Furze Rebecca C.¹²³⁴,Gordon Laurie¹²¹⁰²¹¹³,Drewes Gerard⁵⁶²⁷⁸,Rioja Inmaculada¹²³⁴,Witherington Jason¹²³⁴,Parr Nigel J.¹²³⁴,Prinjha Rab K.¹²³⁴

Affiliation:

1. Epinova Discovery Performance Unit

2. GlaxoSmithKline R&D

3. Stevenage

4. UK

5. Platform, Technology & Science

6. Cellzome, Molecular Discovery Research

7. Heidelberg

8. Germany

9. Computational & Structural Chemistry

10. Molecular Discovery Research

11. Medicines Research Centre

12. Screening & Compound Profiling

Abstract

DUAL946 (1) inhibits BET and HDAC proteins in chemoproteomic cell lysate experiments and in immune and cancer cells.

Publisher

Royal Society of Chemistry (RSC)

Subject

Pharmaceutical Science,Biochemistry,Drug Discovery,Molecular Medicine,Pharmacology,Organic Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2014/MD/C3MD00285C

Reference52 articles.

1. Suppression of inflammation by a synthetic histone mimic

2. Histone deacetylases and cancer: causes and therapies

3. HDAC inhibitors as anti-inflammatory agents

4. Histone deacetylases as regulators of inflammation and immunity

5. HDAC inhibitors in cancer biology: emerging mechanisms and clinical applications

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1. Identification of potent BRD4‐BD1 inhibitors using classical and steered molecular dynamics based free energy analysis;Journal of Cellular Biochemistry;2024-02-05

2. Development of Potent Dual BET/HDAC Inhibitors via Pharmacophore Merging and Structure-Guided Optimization;ACS Chemical Biology;2024-01-31

3. Dual inhibitors of HDAC and other epigenetic regulators: A novel strategy for cancer treatment;European Journal of Medicinal Chemistry;2024-01

4. Targeting the epigenetic reader “BET” as a therapeutic strategy for cancer;Bioorganic Chemistry;2023-11

5. Difluoromethyl-1,3,4-oxadiazoles Are Selective, Mechanism-Based, and Essentially Irreversible Inhibitors of Histone Deacetylase 6;Journal of Medicinal Chemistry;2023-10-02

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