Targeting metalloenzymes for therapeutic intervention

AY Chen, RN Adamek, BL Dick, CV Credille… - Chemical …, 2018 - ACS Publications
Metalloenzymes are central to a wide range of essential biological activities, including
nucleic acid modification, protein degradation, and many others. The role of metalloenzymes …

Dynamic combinatorial/covalent chemistry: a tool to read, generate and modulate the bioactivity of compounds and compound mixtures

A Herrmann - Chemical Society Reviews, 2014 - pubs.rsc.org
Reversible covalent bond formation under thermodynamic control adds reactivity to self-
assembled supramolecular systems, and is therefore an ideal tool to assess complexity of …

A small molecule modulates Jumonji histone demethylase activity and selectively inhibits cancer growth

L Wang, J Chang, D Varghese, M Dellinger… - Nature …, 2013 - nature.com
The pharmacological inhibition of general transcriptional regulators has the potential to
block growth through targeting multiple tumorigenic signalling pathways simultaneously …

Inhibition of 2-oxoglutarate dependent oxygenases

NR Rose, MA McDonough, ONF King… - Chemical Society …, 2011 - pubs.rsc.org
2-Oxoglutarate (2OG) dependent oxygenases are ubiquitous iron enzymes that couple
substrate oxidation to the conversion of 2OG to succinate and carbon dioxide. In humans …

Dynamic combinatorial chemistry: a tool to facilitate the identification of inhibitors for protein targets

M Mondal, AKH Hirsch - Chemical Society Reviews, 2015 - pubs.rsc.org
Dynamic combinatorial chemistry (DCC) has emerged as a powerful strategy to identify
ligands for biological targets given that it enables the target to direct the synthesis and …

Histone lysine methylation and demethylation pathways in cancer

RA Varier, HTM Timmers - Biochimica et Biophysica Acta (BBA)-Reviews …, 2011 - Elsevier
The genetic changes leading to the development of human cancer are accompanied by
alterations in the structure and modification status of chromatin, which represent powerful …

Overview of recent strategic advances in medicinal chemistry

G Wu, T Zhao, D Kang, J Zhang, Y Song… - Journal of medicinal …, 2019 - ACS Publications
Introducing novel strategies, concepts, and technologies that speed up drug discovery and
the drug development cycle is of great importance both in the highly competitive …

Structural studies on human 2-oxoglutarate dependent oxygenases

MA McDonough, C Loenarz, R Chowdhury… - Current opinion in …, 2010 - Elsevier
2-Oxoglutarate and ferrous iron-dependent oxygenases have emerged as an important
family of human enzymes that catalyse hydroxylations and related demethylation reactions …

Advances in histone demethylase KDM4 as cancer therapeutic targets

DH Lee, GW Kim, YH Jeon, J Yoo, SW Lee… - The FASEB …, 2020 - Wiley Online Library
Abstract The KDM4 subfamily H3K9 histone demethylases are epigenetic regulators that
control chromatin structure and gene expression by demethylating histone H3K9, H3K36 …

Structural analysis of human KDM5B guides histone demethylase inhibitor development

C Johansson, S Velupillai, A Tumber… - Nature chemical …, 2016 - nature.com
Members of the KDM5 (also known as JARID1) family are 2-oxoglutarate-and Fe2+-
dependent oxygenases that act as histone H3K4 demethylases, thereby regulating cell …