Emmanuel H Demont
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Explore the profile of Emmanuel H Demont including associated specialties, affiliations and a list of published articles.
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36
Citations
570
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Recent Articles
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Hirst D, Bamborough P, Al-Mahdi N, Angell D, Barnett H, Baxter A, et al.
J Med Chem
. 2024 Jun;
67(12):10464-10489.
PMID: 38866424
The bromodomain and extra terminal (BET) family of bromodomain-containing proteins are important epigenetic regulators that elicit their effect through binding histone tail -acetyl lysine (KAc) post-translational modifications. Recognition of such...
3.
Bradley E, Fusani L, Chung C, Craggs P, Demont E, Humphreys P, et al.
J Med Chem
. 2023 Nov;
66(23):15728-15749.
PMID: 37967462
Small-molecule-mediated disruption of the protein-protein interactions between acetylated histone tails and the tandem bromodomains of the bromodomain and extra-terminal (BET) family of proteins is an important mechanism of action for...
4.
Bamborough P, Chung C, Goodwin N, Mitchell D, Neipp C, Phillipou A, et al.
ACS Med Chem Lett
. 2023 Sep;
14(9):1231-1236.
PMID: 37736196
The 1,3-dihydro-2-benzo[]azepin-2-ones are potent and ligand-efficient pan-BET bromodomain inhibitors. Here we describe the extension of this template to exploit a bivalent mode of action, binding simultaneously to both bromodomains. Initially...
5.
Clegg M, Theodoulou N, Bamborough P, Chung C, Craggs P, Demont E, et al.
ACS Med Chem Lett
. 2021 Aug;
12(8):1308-1317.
PMID: 34413961
Bromodomain containing proteins and the acetyl-lysine binding bromodomains contained therein are increasingly attractive targets for the development of novel epigenetic therapeutics. To help validate this target class and unravel the...
6.
Jones K, Beaumont D, Bernard S, Bit R, Campbell S, Chung C, et al.
J Med Chem
. 2021 Aug;
64(16):12200-12227.
PMID: 34387088
The functions of the bromodomain and extra terminal (BET) family of proteins have been implicated in a wide range of diseases, particularly in the oncology and immuno-inflammatory areas, and several...
7.
Lucas S, Atkinson S, Chung C, Davis R, Gordon L, Grandi P, et al.
J Med Chem
. 2021 Jul;
64(15):10711-10741.
PMID: 34260229
Herein, a series of 2,3-dihydrobenzofurans have been developed as highly potent bromo and extra-terminal domain (BET) inhibitors with 1000-fold selectivity for the second bromodomain (BD2) over the first bromodomain (BD1)....
8.
Seal J, Atkinson S, Bamborough P, Bassil A, Chung C, Foley J, et al.
J Med Chem
. 2021 Jul;
64(15):10772-10805.
PMID: 34255512
The profound efficacy of pan-BET inhibitors is well documented, but these epigenetic agents have shown pharmacology-driven toxicity in oncology clinical trials. The opportunity to identify inhibitors with an improved safety...
9.
Rianjongdee F, Atkinson S, Chung C, Grandi P, Gray J, Kaushansky L, et al.
J Med Chem
. 2021 Jul;
64(15):10806-10833.
PMID: 34251219
Second-generation bromodomain and extra terminal (BET) inhibitors, which selectively target one of the two bromodomains in the BET proteins, have begun to emerge in the literature. These inhibitors aim to...
10.
Harrison L, Atkinson S, Bassil A, Chung C, Grandi P, Gray J, et al.
J Med Chem
. 2021 Jul;
64(15):10742-10771.
PMID: 34232650
Domain-specific BET bromodomain ligands represent an attractive target for drug discovery with the potential to unlock the therapeutic benefits of antagonizing these proteins without eliciting the toxicological aspects seen with...