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Lysine acetylation goes global: from epigenetics to metabolism and therapeutics
Post-translational acetylation of lysine residues has emerged as a key regulatory
mechanism in all eukaryotic organisms. Originally discovered in 1963 as a unique …
mechanism in all eukaryotic organisms. Originally discovered in 1963 as a unique …
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 …
Jaguar: A high‐performance quantum chemistry software program with strengths in life and materials sciences
Jaguar is an ab initio quantum chemical program that specializes in fast electronic structure
predictions for molecular systems of medium and large size. Jaguar focuses on …
predictions for molecular systems of medium and large size. Jaguar focuses on …
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 …
Epigenetic protein families: a new frontier for drug discovery
Epigenetic regulation of gene expression is a dynamic and reversible process that
establishes normal cellular phenotypes but also contributes to human diseases. At the …
establishes normal cellular phenotypes but also contributes to human diseases. At the …
Modulators of protein–protein interactions
Since Hedin's characterization of trypsin and antitrypsin in 1906,(1) arguably the first
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …
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 …
RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain
S Picaud, C Wells, I Felletar, D Brotherton… - Proceedings of the …, 2013 - pnas.org
Bromodomains have emerged as attractive candidates for the development of inhibitors
targeting gene transcription. Inhibitors of the bromo and extraterminal (BET) family recently …
targeting gene transcription. Inhibitors of the bromo and extraterminal (BET) family recently …
Fragment-based approaches in drug discovery and chemical biology
Fragment-based approaches to finding novel small molecules that bind to proteins are now
firmly established in drug discovery and chemical biology. Initially developed primarily in a …
firmly established in drug discovery and chemical biology. Initially developed primarily in a …