The recent progress of isoxazole in medicinal chemistry

J Zhu, J Mo, H Lin, Y Chen, H Sun - Bioorganic & Medicinal Chemistry, 2018 - Elsevier
Isoxazole compounds exhibit a wide spectrum of targets and broad biological activities.
Developing compounds with heterocycle rings has been one of the trends. The integration of …

Targeting bromodomains: epigenetic readers of lysine acetylation

P Filippakopoulos, S Knapp - Nature reviews Drug discovery, 2014 - nature.com
Lysine acetylation is a key mechanism that regulates chromatin structure; aberrant
acetylation levels have been linked to the development of several diseases. Acetyl-lysine …

Protein lysine acetylation by p300/CBP

BM Dancy, PA Cole - Chemical reviews, 2015 - ACS Publications
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 …

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 …

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 …

BET domain co-regulators in obesity, inflammation and cancer

AC Belkina, GV Denis - Nature reviews Cancer, 2012 - nature.com
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 …

Drug discovery targeting bromodomain-containing protein 4

Z Liu, P Wang, H Chen, EA Wold, B Tian… - Journal of medicinal …, 2017 - ACS Publications
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 …

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 …

BET protein function is required for inflammation: Brd2 genetic disruption and BET inhibitor JQ1 impair mouse macrophage inflammatory responses

AC Belkina, BS Nikolajczyk, GV Denis - The Journal of Immunology, 2013 - journals.aai.org
Histone acetylation regulates activation and repression of multiple inflammatory genes
known to play critical roles in chronic inflammatory diseases. However, proteins responsible …

[HTML][HTML] The bromodomain interaction module

P Filippakopoulos, S Knapp - FEBS letters, 2012 - Elsevier
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 …