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GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain
[Image: see text] The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engagement assay was recently de...
| Autores principales: | , , , , , , , , , , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
American Chemical
Society
2016
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| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4904261/ https://www.ncbi.nlm.nih.gov/pubmed/27326325 http://dx.doi.org/10.1021/acsmedchemlett.6b00092 |
| _version_ | 1782437117769547776 |
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| author | Bamborough, Paul Barnett, Heather A. Becher, Isabelle Bird, Mark J. Chung, Chun-wa Craggs, Peter D. Demont, Emmanuel H. Diallo, Hawa Fallon, David J. Gordon, Laurie J. Grandi, Paola Hobbs, Clare I. Hooper-Greenhill, Edward Jones, Emma J. Law, Robert P. Le Gall, Armelle Lugo, David Michon, Anne-Marie Mitchell, Darren J. Prinjha, Rab K. Sheppard, Robert J. Watson, Allan J. B. Watson, Robert J. |
| author_facet | Bamborough, Paul Barnett, Heather A. Becher, Isabelle Bird, Mark J. Chung, Chun-wa Craggs, Peter D. Demont, Emmanuel H. Diallo, Hawa Fallon, David J. Gordon, Laurie J. Grandi, Paola Hobbs, Clare I. Hooper-Greenhill, Edward Jones, Emma J. Law, Robert P. Le Gall, Armelle Lugo, David Michon, Anne-Marie Mitchell, Darren J. Prinjha, Rab K. Sheppard, Robert J. Watson, Allan J. B. Watson, Robert J. |
| author_sort | Bamborough, Paul |
| collection | PubMed |
| description | [Image: see text] The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engagement assay was recently described. Herein, we report the optimization of this series leading to the identification of a superior BRPF1 inhibitor suitable for in vivo studies. |
| format | Online Article Text |
| id | pubmed-4904261 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2016 |
| publisher | American Chemical
Society |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-49042612017-06-09 GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain Bamborough, Paul Barnett, Heather A. Becher, Isabelle Bird, Mark J. Chung, Chun-wa Craggs, Peter D. Demont, Emmanuel H. Diallo, Hawa Fallon, David J. Gordon, Laurie J. Grandi, Paola Hobbs, Clare I. Hooper-Greenhill, Edward Jones, Emma J. Law, Robert P. Le Gall, Armelle Lugo, David Michon, Anne-Marie Mitchell, Darren J. Prinjha, Rab K. Sheppard, Robert J. Watson, Allan J. B. Watson, Robert J. ACS Med Chem Lett [Image: see text] The BRPF (Bromodomain and PHD Finger-containing) protein family are important scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a cellular target engagement assay was recently described. Herein, we report the optimization of this series leading to the identification of a superior BRPF1 inhibitor suitable for in vivo studies. American Chemical Society 2016-05-09 /pmc/articles/PMC4904261/ /pubmed/27326325 http://dx.doi.org/10.1021/acsmedchemlett.6b00092 Text en Copyright © 2016 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes. |
| spellingShingle | Bamborough, Paul Barnett, Heather A. Becher, Isabelle Bird, Mark J. Chung, Chun-wa Craggs, Peter D. Demont, Emmanuel H. Diallo, Hawa Fallon, David J. Gordon, Laurie J. Grandi, Paola Hobbs, Clare I. Hooper-Greenhill, Edward Jones, Emma J. Law, Robert P. Le Gall, Armelle Lugo, David Michon, Anne-Marie Mitchell, Darren J. Prinjha, Rab K. Sheppard, Robert J. Watson, Allan J. B. Watson, Robert J. GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain |
| title | GSK6853, a Chemical Probe for Inhibition of the BRPF1
Bromodomain |
| title_full | GSK6853, a Chemical Probe for Inhibition of the BRPF1
Bromodomain |
| title_fullStr | GSK6853, a Chemical Probe for Inhibition of the BRPF1
Bromodomain |
| title_full_unstemmed | GSK6853, a Chemical Probe for Inhibition of the BRPF1
Bromodomain |
| title_short | GSK6853, a Chemical Probe for Inhibition of the BRPF1
Bromodomain |
| title_sort | gsk6853, a chemical probe for inhibition of the brpf1
bromodomain |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4904261/ https://www.ncbi.nlm.nih.gov/pubmed/27326325 http://dx.doi.org/10.1021/acsmedchemlett.6b00092 |
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