Epigenetic tools (The Writers, The Readers and The Erasers) and their implications in cancer therapy

S Biswas, CM Rao - European journal of pharmacology, 2018 - Elsevier
Addition of chemical tags on the DNA and modification of histone proteins impart a distinct
feature on chromatin architecture. With the advancement in scientific research, the key …

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 promise and peril of chemical probes

CH Arrowsmith, JE Audia, C Austin, J Baell… - Nature chemical …, 2015 - nature.com
Chemical probes are powerful reagents with increasing impacts on biomedical research.
However, probes of poor quality or that are used incorrectly generate misleading results. To …

2, 5-Diketopiperazines: synthesis, reactions, medicinal chemistry, and bioactive natural products

AD Borthwick - Chemical reviews, 2012 - ACS Publications
2, 5-Diketopiperazines (2, 5-DKPs) are cyclodipeptides obtained by the condensation of two
α-amino acids. They not only abound in nature but are often produced as degradation …

Cancer epigenetics reaches mainstream oncology

M Rodríguez-Paredes, M Esteller - Nature medicine, 2011 - nature.com
Epigenetics is one of the most promising and expanding fields in the current biomedical
research landscape. Since the inception of epigenetics in the 1940s, the discoveries …

Inhibitors of protein methyltransferases and demethylases

HU Kaniskan, ML Martini, J Jin - Chemical reviews, 2018 - ACS Publications
Post-translational modifications of histones by protein methyltransferases (PMTs) and
histone demethylases (KDMs) play an important role in the regulation of gene expression …

Structural simplification of natural products

S Wang, G Dong, C Sheng - Chemical Reviews, 2019 - ACS Publications
Natural products (NPs) are important sources of clinical drugs due to their structural diversity
and biological prevalidation. However, the structural complexity of NPs leads to synthetic …

A brief history of antibiotics and select advances in their synthesis

KC Nicolaou, S Rigol - The Journal of antibiotics, 2018 - nature.com
The advent of modern antibiotics contributed enormously to the dramatic extension of
human lifespan since their discovery by virtue of their lethal and selective action against …

Critical roles of non-histone protein lysine methylation in human tumorigenesis

R Hamamoto, V Saloura, Y Nakamura - Nature Reviews Cancer, 2015 - nature.com
Several protein lysine methyltransferases and demethylases have been identified to have
critical roles in histone modification. A large body of evidence has indicated that their …

The role of macrophages in HIV-1 persistence and pathogenesis

Z Kruize, NA Kootstra - Frontiers in microbiology, 2019 - frontiersin.org
Current antiretroviral therapy (ART) effectively suppresses Human Immunodeficiency Virus
type 1 (HIV-1) in infected individuals. However, even long term ART does not eradicate HIV …