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A chemical probe for the ATAD2 bromodomain

Research output: Contribution to journalArticlepeer-review

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A chemical probe for the ATAD2 bromodomain. / Bamborough, Paul; Chung, Chun-wa; Demont, Emmanuel H.; Furze, Rebecca C.; Bannister, Andrew J.; Che, Ka Hing; Diallo, Hawa; Douault, Clement; Grandi, Paola; Kouzarides, Tony; Michon, Anne-Marie; Mitchell, Darren J.; Prinjha, Rab K.; Rau, Christina; Robson, Samuel; Sheppard, Robert J.; Upton, Richard; Watson, Robert J.

In: Angewandte Chemie International Edition, Vol. 55, No. 38, 12.09.2016, p. 11382-11386.

Research output: Contribution to journalArticlepeer-review

Harvard

Bamborough, P, Chung, C, Demont, EH, Furze, RC, Bannister, AJ, Che, KH, Diallo, H, Douault, C, Grandi, P, Kouzarides, T, Michon, A-M, Mitchell, DJ, Prinjha, RK, Rau, C, Robson, S, Sheppard, RJ, Upton, R & Watson, RJ 2016, 'A chemical probe for the ATAD2 bromodomain', Angewandte Chemie International Edition, vol. 55, no. 38, pp. 11382-11386. https://doi.org/10.1002/anie.201603928

APA

Bamborough, P., Chung, C., Demont, E. H., Furze, R. C., Bannister, A. J., Che, K. H., Diallo, H., Douault, C., Grandi, P., Kouzarides, T., Michon, A-M., Mitchell, D. J., Prinjha, R. K., Rau, C., Robson, S., Sheppard, R. J., Upton, R., & Watson, R. J. (2016). A chemical probe for the ATAD2 bromodomain. Angewandte Chemie International Edition, 55(38), 11382-11386. https://doi.org/10.1002/anie.201603928

Vancouver

Bamborough P, Chung C, Demont EH, Furze RC, Bannister AJ, Che KH et al. A chemical probe for the ATAD2 bromodomain. Angewandte Chemie International Edition. 2016 Sep 12;55(38):11382-11386. https://doi.org/10.1002/anie.201603928

Author

Bamborough, Paul ; Chung, Chun-wa ; Demont, Emmanuel H. ; Furze, Rebecca C. ; Bannister, Andrew J. ; Che, Ka Hing ; Diallo, Hawa ; Douault, Clement ; Grandi, Paola ; Kouzarides, Tony ; Michon, Anne-Marie ; Mitchell, Darren J. ; Prinjha, Rab K. ; Rau, Christina ; Robson, Samuel ; Sheppard, Robert J. ; Upton, Richard ; Watson, Robert J. / A chemical probe for the ATAD2 bromodomain. In: Angewandte Chemie International Edition. 2016 ; Vol. 55, No. 38. pp. 11382-11386.

Bibtex

@article{0cdb77fb8483427d8a9908a77ecc7cfc,
title = "A chemical probe for the ATAD2 bromodomain",
abstract = "ATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class. Starting from a potent lead, permeability and selectivity were improved through a dual approach: 1) using CF2 as a sulfone bio-isostere to exploit the unique properties of fluorine, and 2) using 1,3-interactions to control the conformation of a piperidine ring. This resulted in the first reported low-nanomolar, selective and cell permeable chemical probe for ATAD2.",
keywords = "RCUK, BBSRC, RG69031",
author = "Paul Bamborough and Chun-wa Chung and Demont, {Emmanuel H.} and Furze, {Rebecca C.} and Bannister, {Andrew J.} and Che, {Ka Hing} and Hawa Diallo and Clement Douault and Paola Grandi and Tony Kouzarides and Anne-Marie Michon and Mitchell, {Darren J.} and Prinjha, {Rab K.} and Christina Rau and Samuel Robson and Sheppard, {Robert J.} and Richard Upton and Watson, {Robert J.}",
year = "2016",
month = sep,
day = "12",
doi = "10.1002/anie.201603928",
language = "English",
volume = "55",
pages = "11382--11386",
journal = "Angewandte Chemie International Edition",
issn = "1433-7851",
publisher = "John Wiley and Sons Ltd",
number = "38",

}

RIS

TY - JOUR

T1 - A chemical probe for the ATAD2 bromodomain

AU - Bamborough, Paul

AU - Chung, Chun-wa

AU - Demont, Emmanuel H.

AU - Furze, Rebecca C.

AU - Bannister, Andrew J.

AU - Che, Ka Hing

AU - Diallo, Hawa

AU - Douault, Clement

AU - Grandi, Paola

AU - Kouzarides, Tony

AU - Michon, Anne-Marie

AU - Mitchell, Darren J.

AU - Prinjha, Rab K.

AU - Rau, Christina

AU - Robson, Samuel

AU - Sheppard, Robert J.

AU - Upton, Richard

AU - Watson, Robert J.

PY - 2016/9/12

Y1 - 2016/9/12

N2 - ATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class. Starting from a potent lead, permeability and selectivity were improved through a dual approach: 1) using CF2 as a sulfone bio-isostere to exploit the unique properties of fluorine, and 2) using 1,3-interactions to control the conformation of a piperidine ring. This resulted in the first reported low-nanomolar, selective and cell permeable chemical probe for ATAD2.

AB - ATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class. Starting from a potent lead, permeability and selectivity were improved through a dual approach: 1) using CF2 as a sulfone bio-isostere to exploit the unique properties of fluorine, and 2) using 1,3-interactions to control the conformation of a piperidine ring. This resulted in the first reported low-nanomolar, selective and cell permeable chemical probe for ATAD2.

KW - RCUK

KW - BBSRC

KW - RG69031

UR - https://www.repository.cam.ac.uk/

U2 - 10.1002/anie.201603928

DO - 10.1002/anie.201603928

M3 - Article

VL - 55

SP - 11382

EP - 11386

JO - Angewandte Chemie International Edition

JF - Angewandte Chemie International Edition

SN - 1433-7851

IS - 38

ER -

ID: 7360731