Targeting epigenetic regulators to overcome drug resistance in cancers

N Wang, T Ma, B Yu - Signal transduction and targeted therapy, 2023 - nature.com
Drug resistance is mainly responsible for cancer recurrence and poor prognosis. Epigenetic
regulation is a heritable change in gene expressions independent of nucleotide sequence …

LSD1/KDM1A inhibitors in clinical trials: advances and prospects

Y Fang, G Liao, B Yu - Journal of hematology & oncology, 2019 - Springer
Histone demethylase LSD1 plays key roles during carcinogenesis, targeting LSD1 is
becoming an emerging option for the treatment of cancers. Numerous LSD1 inhibitors have …

Targeting epigenetic modifications in cancer therapy: erasing the roadmap to cancer

HP Mohammad, O Barbash, CL Creasy - Nature medicine, 2019 - nature.com
Epigenetic dysregulation is a common feature of most cancers, often occurring directly
through alteration of epigenetic machinery. Over the last several years, a new generation of …

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 …

Docking screens for novel ligands conferring new biology: Miniperspective

JJ Irwin, BK Shoichet - Journal of medicinal chemistry, 2016 - ACS Publications
It is now plausible to dock libraries of 10 million molecules against targets over several days
or weeks. When the molecules screened are commercially available, they may be rapidly …

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 …

Learning from the harvard clean energy project: The use of neural networks to accelerate materials discovery

EO Pyzer‐Knapp, K Li… - Advanced Functional …, 2015 - Wiley Online Library
Here, the employment of multilayer perceptrons, a type of artificial neural network, is
proposed as part of a computational funneling procedure for high‐throughput organic …

A comprehensive survey of prospective structure-based virtual screening for early drug discovery in the past fifteen years

H Zhu, Y Zhang, W Li, N Huang - International Journal of Molecular …, 2022 - mdpi.com
Structure-based virtual screening (SBVS), also known as molecular docking, has been
increasingly applied to discover small-molecule ligands based on the protein structures in …

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 …

Targeting histone lysine methylation in cancer

J McGrath, P Trojer - Pharmacology & therapeutics, 2015 - Elsevier
Within the vast landscape of histone modifications lysine methylation has gained increasing
attention because of its profound regulatory potential. The methylation of lysine residues on …