An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains

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Abstract: Bromodomain‐containing proteins are epigenetic modulators involved in a wide range of cellular processes, from recruitment of transcription factors to pathological disruption of gene regulation and cancer development. Since the druggability of these acetyl‐lysine reader domains was established, efforts were made to develop potent and selective inhibitors across the entire family. Here we report the development of a small molecule‐based approach to covalently modify recombinant and endogenous bromodomain‐containing proteins by targeting a conserved lysine and a tyrosine residue in the variable ZA or BC loops. Moreover, the addition of a reporter tag allowed in‐gel visualization and pull‐down of the desired bromodomains.

Location: Deutsche Nationalbibliothek Frankfurt am Main

Extent: Online-Ressource

Language: Englisch

Bibliographic citation: An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains ; volume:131 ; number:4 ; year:2019 ; pages:1019-1024 ; extent:6
Angewandte Chemie ; 131, Heft 4 (2019), 1019-1024 (gesamt 6)

Creator: D'Ascenzio, Melissa
Pugh, Kathryn M.
Konietzny, Rebecca
Berridge, Georgina
Tallant, Cynthia
Hashem, Shaima
Monteiro, Octovia
Thomas, Jason R.
Schirle, Markus
Knapp, Stefan
Marsden, Brian
Fedorov, Oleg
Bountra, Chas
Kessler, Benedikt M.
Brennan, Paul E.

DOI: 10.1002/ange.201807825

URN: urn:nbn:de:101:1-2022070711373419567630

Rights: Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.

Last update: 15.08.2025, 7:26 AM CEST

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D'Ascenzio, Melissa
Pugh, Kathryn M.
Konietzny, Rebecca
Berridge, Georgina
Tallant, Cynthia
Hashem, Shaima
Monteiro, Octovia
Thomas, Jason R.
Schirle, Markus
Knapp, Stefan
Marsden, Brian
Fedorov, Oleg
Bountra, Chas
Kessler, Benedikt M.
Brennan, Paul E.

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An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains

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Other Objects (12)

An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains

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Processing strategy for catalytic residues containing vanadium

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ResBoost: characterizing and predicting catalytic residues in enzymes

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