Results 191 to 200 of about 15,581 (231)

Developing chemical probes for the BET bromodomains

open access: yes, 2016
Hewings, D   +12 more
openaire   +1 more source

BET bromodomain inhibitors

Current Opinion in Chemical Biology, 2022
Lysine acetylation creates docking sites for epigenetic reader domains of BET bromodomain proteins that have emerged as principal regulators of linage specific gene transcription. The development of potent and highly selective inhibitors, that have been soon widely available, enabled mechanistic studies in a diversity of disease models leading to a ...
Martin P. Schwalm, Stefan Knapp
openaire   +2 more sources

BET bromodomain inhibitors regulate keratinocyte plasticity

Nature Chemical Biology, 2021
Although most acute skin wounds heal rapidly, non-healing skin ulcers represent an increasing and substantial unmet medical need that urgently requires effective therapeutics. Keratinocytes resurface wounds to re-establish the epidermal barrier by transitioning to an activated, migratory state, but this ability is lost in dysfunctional chronic wounds ...
Gabi Schutzius   +50 more
openaire   +2 more sources

BET bromodomain inhibitors in leukemia

Experimental Hematology, 2015
The last few years have seen the identification of bromodomain and extraterminal (BET) proteins as critical mediators of transcription with effects on its direct control and cisregulation. This discovery is important in furthering our understanding of the mechanisms of normal transcriptional control. Subsequent work has shed light on the multiple roles
Faisal, Basheer, Brian J P, Huntly
openaire   +2 more sources

BET bromodomain inhibitors: a patent review

Expert Opinion on Therapeutic Patents, 2013
The bromodomain (BRD) and extra-C terminal domain (BET) protein family consists of four members (BRD2, BRD3, BRD4 and BRDT). These "epigenetic readers" bind to acetyllysine (KAc) residues on the tails of histones H3 and H4, and regulate chromatin structure and gene expression.
Jean-Marc, Garnier   +2 more
openaire   +2 more sources

Targeting BET Bromodomains for Cancer Treatment

Epigenomics, 2015
The bromodomain and extraterminal (BET) subfamily of bromodomain-containing proteins has emerged in the last few years as an exciting, novel target group. BRD4, the best studied BET protein, is implicated in a number of hematological and solid tumors. This is linked to its role in modulating transcription elongation of essential genes involved in cell ...
Marie, Jung   +4 more
openaire   +2 more sources

Bet Bromodomains’ Functions in Bone-Related Pathologies

Epigenomics, 2019
Throughout life, bones are subjected to the so-called 'bone-remodeling' process, which is a balanced mechanism between the apposition and the resorption of bone. This remodeling process depends on the activities of bone-specialized cells, namely the osteoblasts and the osteoclasts.
Jacques, Camille   +7 more
openaire   +3 more sources

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