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The recent progress of isoxazole in medicinal chemistry
Isoxazole compounds exhibit a wide spectrum of targets and broad biological activities.
Develo** compounds with heterocycle rings has been one of the trends. The integration of …
Develo** compounds with heterocycle rings has been one of the trends. The integration of …
Targeting bromodomains: epigenetic readers of lysine acetylation
Lysine acetylation is a key mechanism that regulates chromatin structure; aberrant
acetylation levels have been linked to the development of several diseases. Acetyl-lysine …
acetylation levels have been linked to the development of several diseases. Acetyl-lysine …
Bromodomain biology and drug discovery
N Zaware, MM Zhou - Nature structural & molecular biology, 2019 - nature.com
The bromodomain (BrD) is a conserved structural module found in chromatin-and
transcription-associated proteins that acts as the primary reader for acetylated lysine …
transcription-associated proteins that acts as the primary reader for acetylated lysine …
Protein lysine acetylation by p300/CBP
Since their discovery in the 1980s and 1990s, the human protein lysine acetyltransferase
encoded by the paralogous p300 and CBP genes has received much interest. p300/CBP …
encoded by the paralogous p300 and CBP genes has received much interest. p300/CBP …
[HTML][HTML] Histone recognition and large-scale structural analysis of the human bromodomain family
P Filippakopoulos, S Picaud, M Mangos, T Keates… - Cell, 2012 - cell.com
Bromodomains (BRDs) are protein interaction modules that specifically recognize ε-N-lysine
acetylation motifs, a key event in the reading process of epigenetic marks. The 61 BRDs in …
acetylation motifs, a key event in the reading process of epigenetic marks. The 61 BRDs in …
BET domain co-regulators in obesity, inflammation and cancer
The bromodomain is a highly conserved motif of 110 amino acids that is bundled into four
anti-parallel α-helices and found in proteins that interact with chromatin, such as …
anti-parallel α-helices and found in proteins that interact with chromatin, such as …
Drug discovery targeting bromodomain-containing protein 4
BRD4, the most extensively studied member of the BET family, is an epigenetic regulator
that localizes to DNA via binding to acetylated histones and controls the expression of …
that localizes to DNA via binding to acetylated histones and controls the expression of …
Recent developments in the synthesis and reactivity of isoxazoles: metal catalysis and beyond
F Hu, M Szostak - Advanced Synthesis & Catalysis, 2015 - Wiley Online Library
Isoxazoles are important five‐membered aromatic heterocycles in organic chemistry.
Recently, many exciting advances in the synthesis and functionalization of isoxazoles have …
Recently, many exciting advances in the synthesis and functionalization of isoxazoles have …
BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses
Histone acetylation regulates activation and repression of multiple inflammatory genes
known to play critical roles in chronic inflammatory diseases. However, proteins responsible …
known to play critical roles in chronic inflammatory diseases. However, proteins responsible …
[HTML][HTML] The bromodomain interaction module
ε-N-acetylation of lysine residues (Kac) is one of the most abundant post-translation
modifications (PTMs) in the human proteome. In the nucleus, acetylation of histones has …
modifications (PTMs) in the human proteome. In the nucleus, acetylation of histones has …