Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action | Zendy

Amaury E. FernándezMontalván | Zendy; Markus Berger | Zendy; Benno Kuropka | Zendy; Seong Joo Koo | Zendy; Volker Badock | Zendy; Joerg Weiske | Zendy; Vera Puetter | Zendy; Simon J. Holton | Zendy; Detlef Stöckigt | Zendy; Antonius ter Laak | Zendy; Paolo A. Centrella | Zendy; Matthew Clark | Zendy; Christoph E. Dumelin | Zendy; Eric A. Sigel | Zendy; Holly H. Soutter | Zendy; Dawn M. Troast | Zendy; Ying Zhang | Zendy; John W. Cuozzo | Zendy; Anthony D. Keefe | Zendy; Didier Roche | Zendy; Vincent Rodeschini | Zendy; A. Chaikuad | Zendy; L. Diaz Saez | Zendy; James M. Bennett | Zendy; Oleg Fedorov | Zendy; K. Huber | Zendy; Jan Hübner | Zendy; Hilmar Weinmann | Zendy; Ingo V. Hartung | Zendy; Mátyás Gorjánácz | Zendy

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Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action

Author(s) -

Amaury E. FernándezMontalván,

Markus Berger,

Benno Kuropka,

Seong Joo Koo,

Volker Badock,

Joerg Weiske,

Vera Puetter,

Simon J. Holton,

Detlef Stöckigt,

Antonius ter Laak,

Paolo A. Centrella,

Matthew Clark,

Christoph E. Dumelin,

Eric A. Sigel,

Holly H. Soutter,

Dawn M. Troast,

Ying Zhang,

John W. Cuozzo,

Anthony D. Keefe,

Didier Roche,

Vincent Rodeschini,

A. Chaikuad,

L. Diaz Saez,

James M. Bennett,

Oleg Fedorov,

K. Huber,

Jan Hübner,

Hilmar Weinmann,

Ingo V. Hartung,

Mátyás Gorjánácz

Publication year - 2017

Publication title -

acs chemical biology

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.899

H-Index - 111

eISSN - 1554-8937

pISSN - 1554-8929

DOI - 10.1021/acschembio.7b00708

Subject(s) - bromodomain , gene isoform , histone , epigenetics , acetylation , chromatin , chemical biology , regulator , mode of action , microbiology and biotechnology , biology , dna , computational biology , chemistry , biochemistry , genetics , gene

ATAD2 (ANCCA) is an epigenetic regulator and transcriptional cofactor, whose overexpression has been linked to the progress of various cancer types. Here, we report a DNA-encoded library screen leading to the discovery of BAY-850, a potent and isoform selective inhibitor that specifically induces ATAD2 bromodomain dimerization and prevents interactions with acetylated histones in vitro, as well as with chromatin in cells. These features qualify BAY-850 as a chemical probe to explore ATAD2 biology.

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