Articles with "yeats domain" as a keyword



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Evaluation of acyllysine isostere interactions with the aromatic pocket of the AF9 YEATS domain

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Published in 2022 at "Protein Science"

DOI: 10.1002/pro.4533

Abstract: Amide−π interactions, in which an amide interacts with an aromatic group, are ubiquitous in biology, yet remain understudied relative to other noncovalent interactions. Recently, we demonstrated that an electrostatically tunable amide−π interaction is key to… read more here.

Keywords: af9 yeats; amide isosteres; yeats domain; interactions aromatic ... See more keywords
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More than π-π-π stacking: Contribution of Amide-π and CH-π interactions to Crotonyllysine Binding by the AF9 YEATS Domain.

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Published in 2020 at "Journal of the American Chemical Society"

DOI: 10.1021/jacs.0c06568

Abstract: Lysine crotonylation (Kcr) is a histone post-translational modification that is implicated in numerous epigenetic pathways and diseases. Recognition of Kcr by YEATS domains has been proposed to occur through intermolecular amide-π and alkene-π interactions, but… read more here.

Keywords: yeats domain; af9; af9 yeats; contribution amide ... See more keywords
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Transcription control by the ENL YEATS domain in acute leukemia

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Published in 2017 at "Nature"

DOI: 10.1038/nature21688

Abstract: Recurrent chromosomal translocations producing a chimaeric MLL oncogene give rise to a highly aggressive acute leukaemia associated with poor clinical outcome. The preferential involvement of chromatin-associated factors as MLL fusion partners belies a dependency on… read more here.

Keywords: transcription control; enl; yeats domain; acute leukaemia ... See more keywords
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Structural insights into the π-π-π stacking mechanism and DNA-binding activity of the YEATS domain

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Published in 2018 at "Nature Communications"

DOI: 10.1038/s41467-018-07072-6

Abstract: The YEATS domain has been identified as a reader of histone acylation and more recently emerged as a promising anti-cancer therapeutic target. Here, we detail the structural mechanisms for π-π-π stacking involving the YEATS domains… read more here.

Keywords: yeats domain; structural insights; af9 yeats; dna binding ... See more keywords
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Discovery of a Selective Inhibitor for the YEATS Domains of ENL/AF9

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Published in 2019 at "SLAS Discovery"

DOI: 10.1177/2472555218809904

Abstract: Eleven-nineteen leukemia (ENL) contains an epigenetic reader domain (YEATS domain) that recognizes lysine acylation on histone 3 and facilitates transcription initiation and elongation through its interactions with the super elongation complex (SEC) and the histone… read more here.

Keywords: selective inhibitor; yeats domain; inhibitor; discovery selective ... See more keywords
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Fragment-Based Discovery of AF9 YEATS Domain Inhibitors

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Published in 2022 at "International Journal of Molecular Sciences"

DOI: 10.3390/ijms23073893

Abstract: YEATS (YAF9, ENL, AF9, TAF14, SAS5) family proteins recognize acylated histones and in turn regulate chromatin structure, gene transcription, and stress signaling. The chromosomal translocations of ENL and mixed lineage leukemia are considered oncogenic drivers… read more here.

Keywords: fragment based; af9 yeats; based discovery; yeats domain ... See more keywords