Epigenetics of colorectal cancer: biomarker and therapeutic potential

G Jung, E Hernández-Illán, L Moreira… - Nature reviews …, 2020 - nature.com
Colorectal cancer (CRC), a leading cause of cancer-related death worldwide, evolves as a
result of the stepwise accumulation of a series of genetic and epigenetic alterations in the …

Recent developments in epigenetic cancer therapeutics: clinical advancement and emerging trends

K Nepali, JP Liou - Journal of Biomedical Science, 2021 - Springer
Epigenetic drug discovery field has evidenced significant advancement in the recent times.
A plethora of small molecule inhibitors have progressed to clinical stage investigations and …

Co-delivery of IOX1 and doxorubicin for antibody-independent cancer chemo-immunotherapy

J Liu, Z Zhao, N Qiu, Q Zhou, G Wang, H Jiang… - Nature …, 2021 - nature.com
Abstract Anti-programmed cell death-1 (PD-1)/programmed cell death-ligand 1 (PD-L1)
antibodies are currently used in the clinic to interupt the PD-1/PD-L1 immune checkpoint …

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 …

An overview of molecular hybrids in drug discovery

G Bérubé - Expert opinion on drug discovery, 2016 - Taylor & Francis
Introduction: The hybridization of biologically active molecules is a powerful tool for drug
discovery used to target a variety of diseases. It offers the prospect of better drugs for the …

8-Hydroxyquinolines in medicinal chemistry: A structural perspective

V Oliveri, G Vecchio - European journal of medicinal chemistry, 2016 - Elsevier
Hydroxyquinolines are heterocyclic compounds characterized by a moderate metal-binding
affinity. The interest in 8-hydroxyquinolines has grown exponentially in the last two decades …

LSD1 inhibitors for cancer treatment: Focus on multi-target agents and compounds in clinical trials

B Noce, E Di Bello, R Fioravanti, A Mai - Frontiers in pharmacology, 2023 - frontiersin.org
Histone lysine-specific demethylase 1 (LSD1/KDM1A) was first identified in 2004 as an
epigenetic enzyme able to demethylate specific lysine residues of histone H3, namely …

8-Hydroxyquinoline: A privileged structure with a broad-ranging pharmacological potential

H Xu, W Chen, P Zhan, X Liu - MedChemComm, 2015 - pubs.rsc.org
Privileged structures can bind to a diverse range of targets with high affinities, thus
benefiting the discovery of novel bioactive agents. 8-Hydroxyquinoline derivatives represent …

A systematic review of histone lysine‐specific demethylase 1 and its inhibitors

YC Zheng, J Ma, Z Wang, J Li, B Jiang… - Medicinal research …, 2015 - Wiley Online Library
Histone lysine‐specific demethylase 1 (LSD1) is the first discovered and reported histone
demethylase by Dr. Shi Yang's group in 2004. It is classified as a member of amine oxidase …

Recent progress in histone demethylase inhibitors

TE McAllister, KS England, RJ Hopkinson… - Journal of medicinal …, 2016 - ACS Publications
There is increasing interest in targeting histone N-methyl-lysine demethylases (KDMs) with
small molecules both for the generation of probes for target exploration and for therapeutic …