Round, round we go–strategies for enzymatic cofactor regeneration

S Mordhorst, JN Andexer - Natural product reports, 2020 - pubs.rsc.org
Covering: up to the beginning of 2020 Enzymes depending on cofactors are essential in
many biosynthetic pathways of natural products. They are often involved in key steps …

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 …

The functional diversity of protein lysine methylation

S Lanouette, V Mongeon, D Figeys… - Molecular systems …, 2014 - embopress.org
Large‐scale characterization of post‐translational modifications (PTM s), such as
phosphorylation, acetylation and ubiquitination, has highlighted their importance in the …

Protein methyltransferases as a target class for drug discovery

RA Copeland, ME Solomon, VM Richon - Nature reviews Drug …, 2009 - nature.com
The protein methyltransferases (PMTs)—which methylate protein lysine and arginine
residues and have crucial roles in gene transcription—are emerging as an important group …

Chemical mechanisms of histone lysine and arginine modifications

BC Smith, JM Denu - Biochimica et Biophysica Acta (BBA)-Gene Regulatory …, 2009 - Elsevier
Histone lysine and arginine residues are subject to a wide array of post-translational
modifications including methylation, citrullination, acetylation, ubiquitination, and …

EZH2: biology, disease, and structure-based drug discovery

J Tan, Y Yan, X Wang, Y Jiang, HE Xu - Acta Pharmacologica Sinica, 2014 - nature.com
EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2), which is a
highly conserved histone methyltransferase that methylates lysine 27 of histone 3 …

Enzymatic and structural insights for substrate specificity of a family of jumonji histone lysine demethylases

JR Horton, AK Upadhyay, HH Qi, X Zhang… - Nature structural & …, 2010 - nature.com
Combinatorial readout of multiple covalent histone modifications is poorly understood. We
provide insights into how an activating histone mark, in combination with linked repressive …

Carbon-oxygen hydrogen bonding in biological structure and function

S Horowitz, RC Trievel - Journal of Biological Chemistry, 2012 - ASBMB
Carbon-oxygen (CH··· O) hydrogen bonding represents an unusual category of molecular
interactions first documented in biological structures over 4 decades ago. Although CH··· O …

Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294

Y Chang, X Zhang, JR Horton, AK Upadhyay… - Nature structural & …, 2009 - nature.com
Histone lysine methylation is an important epigenetic mark that regulates gene expression
and chromatin organization. G9a and G9a-like protein (GLP) are euchromatin-associated …

Lysine methylation of the NF-κB subunit RelA by SETD6 couples activity of the histone methyltransferase GLP at chromatin to tonic repression of NF-κB signaling

D Levy, AJ Kuo, Y Chang, U Schaefer, C Kitson… - Nature …, 2011 - nature.com
Signaling via the methylation of lysine residues in proteins has been linked to diverse
biological and disease processes, yet the catalytic activity and substrate specificity of many …