Evaluation of linker length effects on a BET bromodomain probe-Reference-Cited by-同舟云学术

Evaluation of linker length effects on a BET bromodomain probe

Published:2019 Issue:68 Volume:55 Page:10128-10131
ISSN:1359-7345
Container-title:Chemical Communications
language:en
Short-container-title:Chem. Commun.

Author:

Traquete Rui¹²³⁴⁵,Henderson Elizabeth⁶⁷⁸⁹¹⁰,Picaud Sarah⁶⁷⁸⁹¹⁰,Cal Pedro M. S. D.¹²³⁴⁵,Sieglitz Florian¹²³⁴⁵,Rodrigues Tiago¹²³⁴⁵^ORCID,Oliveira Rudi¹¹¹²⁵^ORCID,Filippakopoulos Panagis⁶⁷⁸⁹¹⁰,Bernardes Gonçalo J. L.¹²³⁴⁵^ORCID

Affiliation:

1. Instituto de Medicina Molecular João Lobo Antunes

2. Faculdade de Medicina

3. Universidade de Lisboa

4. Lisboa

5. Portugal

6. Structural Genomics Consortium

7. Nuffield Department of Clinical Medicine

8. Oxford University

9. ORCRB

10. Roosevelt Drive

11. Hovione Farmaciência SA

12. Loures

Abstract

A systematic study of the biological effects of introducing linkers of different chemical nature and length into BET bromodomain benzodiazepine ligands.

Funder

Deutsche Forschungsgemeinschaft

Royal Society

Medical Research Council

Fundação para a Ciência e a Tecnologia

Publisher

Royal Society of Chemistry (RSC)

Subject

Materials Chemistry,Metals and Alloys,Surfaces, Coatings and Films,General Chemistry,Ceramics and Composites,Electronic, Optical and Magnetic Materials,Catalysis

Link

http://pubs.rsc.org/en/content/articlepdf/2019/CC/C9CC05054J

Reference18 articles.

1. Histone core modifications regulating nucleosome structure and dynamics

2. Targeting the cancer epigenome for therapy

3. Targeting bromodomains: epigenetic readers of lysine acetylation

4. The Making of I-BET762, a BET Bromodomain Inhibitor Now in Clinical Development

5. Suppression of inflammation by a synthetic histone mimic

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