Discovery of a PCAF Bromodomain Chemical Probe

The p300/CBP‐associated factor (PCAF) and related GCN5 bromodomain‐containing lysine acetyl transferases are members of subfamily I of the bromodomain phylogenetic tree. Iterative cycles of rational inhibitor design and biophysical characterization led to the discovery of the triazolopthalazine‐base...

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Published inAngewandte Chemie International Edition Vol. 56; no. 3; pp. 827 - 831
Main Authors Moustakim, Moses, Clark, Peter G. K., Trulli, Laura, Fuentes de Arriba, Angel L., Ehebauer, Matthias T., Chaikuad, Apirat, Murphy, Emma J., Mendez‐Johnson, Jacqui, Daniels, Danette, Hou, Chun‐Feng D., Lin, Yu‐Hui, Walker, John R., Hui, Raymond, Yang, Hongbing, Dorrell, Lucy, Rogers, Catherine M., Monteiro, Octovia P., Fedorov, Oleg, Huber, Kilian V. M., Knapp, Stefan, Heer, Jag, Dixon, Darren J., Brennan, Paul E.
Format Journal Article
LanguageEnglish
Published WEINHEIM Wiley 16.01.2017
Wiley Subscription Services, Inc
John Wiley and Sons Inc
EditionInternational ed. in English
Subjects
Azo Compounds - chemical synthesis
Azo Compounds - chemistry
Azo Compounds - pharmacology
Biocompatibility
bromodomains
chemical probes
Chemistry
Chemistry, Multidisciplinary
Communication
Communications
Crystal structure
Cycle ratio
Cytotoxicity
Dose-Response Relationship, Drug
Drug Discovery
epigenetics
Histone H3
Histones
Homology
Hydralazine - chemical synthesis
Hydralazine - chemistry
Hydralazine - pharmacology
Leukocytes (mononuclear)
Lysine
medicinal chemistry
Microsomes
Molecular Probes - chemical synthesis
Molecular Probes - chemistry
Molecular Probes - pharmacology
Molecular Structure
p300-CBP Transcription Factors - antagonists & inhibitors
Peripheral blood mononuclear cells
Permeability
Phylogeny
Physical Sciences
Plasmodium falciparum
Rodents
Science & Technology
Selectivity
Structure-Activity Relationship
structure-based design
Toxicity
DESIGN
P300
TAT
IDENTIFICATION
TARGETING BROMODOMAINS
epigenetics
structure-based design
FAMILY
bromodomains
BRD9
chemical probes
INHIBITORS
BINDING
medicinal chemistry
ACETYLTRANSFERASE
Online AccessGet full text

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Abstract The p300/CBP‐associated factor (PCAF) and related GCN5 bromodomain‐containing lysine acetyl transferases are members of subfamily I of the bromodomain phylogenetic tree. Iterative cycles of rational inhibitor design and biophysical characterization led to the discovery of the triazolopthalazine‐based L‐45 (dubbed L‐Moses) as the first potent, selective, and cell‐active PCAF bromodomain (Brd) inhibitor. Synthesis from readily available (1R,2S)‐(−)‐norephedrine furnished L‐45 in enantiopure form. L‐45 was shown to disrupt PCAF‐Brd histone H3.3 interaction in cells using a nanoBRET assay, and a co‐crystal structure of L‐45 with the homologous Brd PfGCN5 from Plasmodium falciparum rationalizes the high selectivity for PCAF and GCN5 bromodomains. Compound L‐45 shows no observable cytotoxicity in peripheral blood mononuclear cells (PBMC), good cell‐permeability, and metabolic stability in human and mouse liver microsomes, supporting its potential for in vivo use. Let my PCAF go: The first potent, selective, and cell‐active inhibitor of PCAF bromodomains (Brd) is reported. L‐Moses was shown to disrupt the PCAF‐Brd/histone H3.3 interaction in cells using a nanoBRET assay, and a co‐crystal structure of L‐Moses with the homologous Brd PfGCN5 helps explain the high selectivity for PCAF and GCN5 bromodomains.
AbstractList The p300/CBP‐associated factor (PCAF) and related GCN5 bromodomain‐containing lysine acetyl transferases are members of subfamily I of the bromodomain phylogenetic tree. Iterative cycles of rational inhibitor design and biophysical characterization led to the discovery of the triazolopthalazine‐based L‐45 (dubbed L‐Moses ) as the first potent, selective, and cell‐active PCAF bromodomain (Brd) inhibitor. Synthesis from readily available (1R,2S)‐(−)‐norephedrine furnished L‐45 in enantiopure form. L‐45 was shown to disrupt PCAF‐Brd histone H3.3 interaction in cells using a nanoBRET assay, and a co‐crystal structure of L‐45 with the homologous Brd PfGCN5 from Plasmodium falciparum rationalizes the high selectivity for PCAF and GCN5 bromodomains. Compound L‐45 shows no observable cytotoxicity in peripheral blood mononuclear cells (PBMC), good cell‐permeability, and metabolic stability in human and mouse liver microsomes, supporting its potential for in vivo use.
The p300/CBP‐associated factor (PCAF) and related GCN5 bromodomain‐containing lysine acetyl transferases are members of subfamily I of the bromodomain phylogenetic tree. Iterative cycles of rational inhibitor design and biophysical characterization led to the discovery of the triazolopthalazine‐based L‐45 (dubbed L‐Moses) as the first potent, selective, and cell‐active PCAF bromodomain (Brd) inhibitor. Synthesis from readily available (1R,2S)‐(−)‐norephedrine furnished L‐45 in enantiopure form. L‐45 was shown to disrupt PCAF‐Brd histone H3.3 interaction in cells using a nanoBRET assay, and a co‐crystal structure of L‐45 with the homologous Brd PfGCN5 from Plasmodium falciparum rationalizes the high selectivity for PCAF and GCN5 bromodomains. Compound L‐45 shows no observable cytotoxicity in peripheral blood mononuclear cells (PBMC), good cell‐permeability, and metabolic stability in human and mouse liver microsomes, supporting its potential for in vivo use. Let my PCAF go: The first potent, selective, and cell‐active inhibitor of PCAF bromodomains (Brd) is reported. L‐Moses was shown to disrupt the PCAF‐Brd/histone H3.3 interaction in cells using a nanoBRET assay, and a co‐crystal structure of L‐Moses with the homologous Brd PfGCN5 helps explain the high selectivity for PCAF and GCN5 bromodomains.
The p300/CBP-associated factor (PCAF) and related GCN5 bromodomain-containing lysine acetyl transferases are members of subfamily I of the bromodomain phylogenetic tree. Iterative cycles of rational inhibitor design and biophysical characterization led to the discovery of the triazolopthalazine-based L-45 (dubbed L-Moses) as the first potent, selective, and cell-active PCAF bromodomain (Brd) inhibitor. Synthesis from readily available (1R,2S)-(-)-norephedrine furnished L-45 in enantiopure form. L-45 was shown to disrupt PCAF-Brd histone H3.3 interaction in cells using a nanoBRET assay, and a co-crystal structure of L-45 with the homologous Brd PfGCN5 from Plasmodium falciparum rationalizes the high selectivity for PCAF and GCN5 bromodomains. Compound L-45 shows no observable cytotoxicity in peripheral blood mononuclear cells (PBMC), good cell-permeability, and metabolic stability in human and mouse liver microsomes, supporting its potential for in vivo use.
The p300/CBP-associated factor (PCAF) and related GCN5 bromodomain-containing lysine acetyl transferases are members of subfamilyI of the bromodomain phylogenetic tree. Iterative cycles of rational inhibitor design and biophysical characterization led to the discovery of the triazolopthalazine-based L-45 (dubbed L-Moses) as the first potent, selective, and cell-active PCAF bromodomain (Brd) inhibitor. Synthesis from readily available (1R,2S)-(-)-norephedrine furnished L-45 in enantiopure form. L-45 was shown to disrupt PCAF-Brd histone H3.3 interaction in cells using a nanoBRET assay, and a co-crystal structure of L-45 with the homologous Brd PfGCN5 from Plasmodium falciparum rationalizes the high selectivity for PCAF and GCN5 bromodomains. Compound L-45 shows no observable cytotoxicity in peripheral blood mononuclear cells (PBMC), good cell-permeability, and metabolic stability in human and mouse liver microsomes, supporting its potential for invivo use.
The p300/CBP‐associated factor (PCAF) and related GCN5 bromodomain‐containing lysine acetyl transferases are members of subfamily I of the bromodomain phylogenetic tree. Iterative cycles of rational inhibitor design and biophysical characterization led to the discovery of the triazolopthalazine‐based L‐45 (dubbed L‐Moses) as the first potent, selective, and cell‐active PCAF bromodomain (Brd) inhibitor. Synthesis from readily available (1R,2S)‐(−)‐norephedrine furnished L‐45 in enantiopure form. L‐45 was shown to disrupt PCAF‐Brd histone H3.3 interaction in cells using a nanoBRET assay, and a co‐crystal structure of L‐45 with the homologous Brd PfGCN5 from Plasmodium falciparum rationalizes the high selectivity for PCAF and GCN5 bromodomains. Compound L‐45 shows no observable cytotoxicity in peripheral blood mononuclear cells (PBMC), good cell‐permeability, and metabolic stability in human and mouse liver microsomes, supporting its potential for in vivo use.
Author Knapp, Stefan
Rogers, Catherine M.
Fuentes de Arriba, Angel L.
Lin, Yu‐Hui
Hou, Chun‐Feng D.
Brennan, Paul E.
Yang, Hongbing
Clark, Peter G. K.
Moustakim, Moses
Dorrell, Lucy
Murphy, Emma J.
Fedorov, Oleg
Huber, Kilian V. M.
Trulli, Laura
Ehebauer, Matthias T.
Chaikuad, Apirat
Mendez‐Johnson, Jacqui
Hui, Raymond
Daniels, Danette
Walker, John R.
Monteiro, Octovia P.
Heer, Jag
Dixon, Darren J.
AuthorAffiliation 1 Structural Genomics Consortium & Target Discovery Institute University of Oxford NDM Research Building Roosevelt Drive Oxford OX3 7DQ and OX3 7FZ UK
3 Department of Chemistry Simon Fraser University Burnaby V5A 1S6 Canada
5 ARUK Oxford Drug Discovery Institute University of Oxford Oxford OX3 7FZ UK
7 Promega Corporation 2800 Woods Hollow Road Madison WI 153611 USA
9 Nuffield Department of Medicine and Oxford NIHR Biomedical Research Centre University of Oxford Oxford OX3 7FZ UK
10 UCB Pharma Ltd Slough SL1 3WE UK
8 Structural Genomics Consortium MaRS South Tower, Suite 732 101 College Street Toronto Ontario M5G 1LZ Canada
2 Department of Chemistry Chemistry Research Laboratory University of Oxford Mansfield Road Oxford OX1 3TA UK
6 Johann Wolfgang Goethe-University Institute for Pharmaceutical Chemistry and Buchmann Institute for Life Sciences 60438 Frankfurt am Main Germany
4 Dipartimento di Chimica Università degli Studi di Roma “La Sapienza” Piazzale Aldo Moro 5 00185 Roma Italy
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– name: 7 Promega Corporation 2800 Woods Hollow Road Madison WI 153611 USA
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– name: 4 Dipartimento di Chimica Università degli Studi di Roma “La Sapienza” Piazzale Aldo Moro 5 00185 Roma Italy
– name: 3 Department of Chemistry Simon Fraser University Burnaby V5A 1S6 Canada
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  organization: Simon Fraser University
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  organization: University of Oxford
BackLink https://www.ncbi.nlm.nih.gov/pubmed/27966810$$D View this record in MEDLINE/PubMed
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– notice: 2017. This article is published under http://creativecommons.org/licenses/by/4.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.
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Issue 3
Keywords DESIGN
P300
TAT
IDENTIFICATION
TARGETING BROMODOMAINS
epigenetics
structure-based design
FAMILY
bromodomains
BRD9
chemical probes
INHIBITORS
BINDING
medicinal chemistry
ACETYLTRANSFERASE
Language English
License Attribution
http://creativecommons.org/licenses/by/4.0
2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.
This is an open access article under the terms of the Creative Commons Attribution License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited.
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SSID ssj0028806
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Snippet The p300/CBP‐associated factor (PCAF) and related GCN5 bromodomain‐containing lysine acetyl transferases are members of subfamily I of the bromodomain...
The p300/CBP-associated factor (PCAF) and related GCN5 bromodomain-containing lysine acetyl transferases are members of subfamily I of the bromodomain...
The p300/CBP-associated factor (PCAF) and related GCN5 bromodomain-containing lysine acetyl transferases are members of subfamily I of the bromodomain...
The p300/CBP-associated factor (PCAF) and related GCN5 bromodomain-containing lysine acetyl transferases are members of subfamilyI of the bromodomain...
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SubjectTerms Azo Compounds - chemical synthesis
Azo Compounds - chemistry
Azo Compounds - pharmacology
Biocompatibility
bromodomains
chemical probes
Chemistry
Chemistry, Multidisciplinary
Communication
Communications
Crystal structure
Cycle ratio
Cytotoxicity
Dose-Response Relationship, Drug
Drug Discovery
epigenetics
Histone H3
Histones
Homology
Hydralazine - chemical synthesis
Hydralazine - chemistry
Hydralazine - pharmacology
Leukocytes (mononuclear)
Lysine
medicinal chemistry
Microsomes
Molecular Probes - chemical synthesis
Molecular Probes - chemistry
Molecular Probes - pharmacology
Molecular Structure
p300-CBP Transcription Factors - antagonists & inhibitors
Peripheral blood mononuclear cells
Permeability
Phylogeny
Physical Sciences
Plasmodium falciparum
Rodents
Science & Technology
Selectivity
Structure-Activity Relationship
structure-based design
Toxicity
Title Discovery of a PCAF Bromodomain Chemical Probe
URI https://onlinelibrary.wiley.com/doi/abs/10.1002%2Fanie.201610816
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https://www.ncbi.nlm.nih.gov/pubmed/27966810
https://www.proquest.com/docview/1856753188
https://www.proquest.com/docview/2462428869
https://pubmed.ncbi.nlm.nih.gov/PMC5412877
Volume 56
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