An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains
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.
- Standort
-
Deutsche Nationalbibliothek Frankfurt am Main
- Umfang
-
Online-Ressource
- Sprache
-
Englisch
- Erschienen in
-
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)
- Urheber
-
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
- Rechteinformation
-
Open Access; Der Zugriff auf das Objekt ist unbeschränkt möglich.
- Letzte Aktualisierung
-
15.08.2025, 07:26 MESZ
Datenpartner
Dieses Objekt wird bereitgestellt von:
Deutsche Nationalbibliothek. Bei Fragen zum Objekt wenden Sie sich bitte an den Datenpartner.
Deutsche Nationalbibliothek. Bei Fragen zum Objekt wenden Sie sich bitte an den Datenpartner.
Beteiligte
- 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.
Ähnliche Objekte (12)
An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains
Identification of amino acid residues essential for the catalytic activity of Drosophila P. element transposase
Identification of amino acid residues essential for the catalytic activity of Drosophila P element transposase
Processing strategy for catalytic residues containing vanadium
Protein structure based prediction of catalytic residues
Combining specificity determining and conserved residues improves functional site prediction
ResBoost: characterizing and predicting catalytic residues in enzymes
Thiazole–amino acids: influence of thiazole ring on conformational properties of amino acid residues
CSmetaPred: a consensus method for prediction of catalytic residues
Automatic prediction of catalytic residues by modeling residue structural neighborhood
Conserved amino acid markers from past influenza pandemic strains
Activity-based protein profiling
An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains
Identification of amino acid residues essential for the catalytic activity of Drosophila P. element transposase
Identification of amino acid residues essential for the catalytic activity of Drosophila P element transposase
Processing strategy for catalytic residues containing vanadium
Protein structure based prediction of catalytic residues
Combining specificity determining and conserved residues improves functional site prediction
ResBoost: characterizing and predicting catalytic residues in enzymes
Thiazole–amino acids: influence of thiazole ring on conformational properties of amino acid residues
CSmetaPred: a consensus method for prediction of catalytic residues
Automatic prediction of catalytic residues by modeling residue structural neighborhood
Conserved amino acid markers from past influenza pandemic strains
Activity-based protein profiling
An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains
Identification of amino acid residues essential for the catalytic activity of Drosophila P. element transposase
Identification of amino acid residues essential for the catalytic activity of Drosophila P element transposase
Processing strategy for catalytic residues containing vanadium
Protein structure based prediction of catalytic residues
Combining specificity determining and conserved residues improves functional site prediction
ResBoost: characterizing and predicting catalytic residues in enzymes
Thiazole–amino acids: influence of thiazole ring on conformational properties of amino acid residues
CSmetaPred: a consensus method for prediction of catalytic residues
Automatic prediction of catalytic residues by modeling residue structural neighborhood
Conserved amino acid markers from past influenza pandemic strains