Lysine acetylation goes global: from epigenetics to metabolism and therapeutics

I Ali, RJ Conrad, E Verdin, M Ott - Chemical reviews, 2018‏ - ACS Publications
Post-translational acetylation of lysine residues has emerged as a key regulatory
mechanism in all eukaryotic organisms. Originally discovered in 1963 as a unique …

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 …

Jaguar: A high‐performance quantum chemistry software program with strengths in life and materials sciences

AD Bochevarov, E Harder, TF Hughes… - … Journal of Quantum …, 2013‏ - Wiley Online Library
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 …

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 …

Epigenetic protein families: a new frontier for drug discovery

CH Arrowsmith, C Bountra, PV Fish, K Lee… - Nature reviews Drug …, 2012‏ - nature.com
Epigenetic regulation of gene expression is a dynamic and reversible process that
establishes normal cellular phenotypes but also contributes to human diseases. At the …

Modulators of protein–protein interactions

LG Milroy, TN Grossmann, S Hennig… - Chemical …, 2014‏ - ACS Publications
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 …

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 …

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 …

Fragment-based approaches in drug discovery and chemical biology

DE Scott, AG Coyne, SA Hudson, C Abell - Biochemistry, 2012‏ - ACS Publications
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 …