Metabolic reprogramming and epigenetic modifications on the path to cancer

L Sun, H Zhang, P Gao - Protein & cell, 2022 - academic.oup.com
Metabolic rewiring and epigenetic remodeling, which are closely linked and reciprocally
regulate each other, are among the well-known cancer hallmarks. Recent evidence …

DNA methyltransferase inhibitors and the development of epigenetic cancer therapies

F Lyko, R Brown - Journal of the National Cancer Institute, 2005 - academic.oup.com
Epimutations, such as the hypermethylation and epigenetic silencing of tumor suppressor
genes, play a role in the etiology of human cancers. In contrast to DNA mutations, which are …

[图书][B] Medicinal chemistry of anticancer drugs

C Avendaño, JC Menéndez - 2015 - books.google.com
Medicinal Chemistry of Anticancer Drugs, Second Edition, provides an updated treatment
from the point of view of medicinal chemistry and drug design, focusing on the mechanism of …

Epigenetic reactivation of tumor suppressor genes by a novel small-molecule inhibitor of human DNA methyltransferases

B Brueckner, R Garcia Boy, P Siedlecki, T Musch… - Cancer research, 2005 - AACR
DNA methylation regulates gene expression in normal and malignant cells. The possibility to
reactivate epigenetically silenced genes has generated considerable interest in the …

DNA methylation inhibitors in cancer: recent and future approaches

C Gros, J Fahy, L Halby, I Dufau, A Erdmann… - Biochimie, 2012 - Elsevier
This review presents the different human DNA methyltransferases (DNMTs), their biological
roles, their mechanisms of action and their role in cancer. The description of assays for …

Utility of homology models in the drug discovery process

A Hillisch, LF Pineda, R Hilgenfeld - Drug discovery today, 2004 - Elsevier
Advances in bioinformatics and protein modeling algorithms, in addition to the enormous
increase in experimental protein structure information, have aided in the generation of …

Genistein inhibits DNA methylation and increases expression of tumor suppressor genes in human breast cancer cells

Q Xie, Q Bai, LY Zou, QY Zhang, Y Zhou… - Genes …, 2014 - Wiley Online Library
It has been previously demonstrated that genistein exhibits anticancer activity against breast
cancer. However, the precise mechanisms underlying the anticancer effect of genistein, in …

Integrating virtual screening and combinatorial chemistry for accelerated drug discovery

F López-Vallejo, T Caulfield… - … Chemistry & High …, 2011 - ingentaconnect.com
Virtual screening is increasingly being used in drug discovery programs with a growing
number of successful applications. Experimental methodologies developed to speed up the …

Synthesis and Biochemical Evaluation of Δ2-Isoxazoline Derivatives as DNA Methyltransferase 1 Inhibitors

S Castellano, D Kuck, M Viviano, J Yoo… - Journal of medicinal …, 2011 - ACS Publications
A series of Δ2-isoxazoline constrained analogues of procaine/procainamide (7a–k and 8a–
k) were prepared and their inhibitory activity against DNA methyltransferase 1 (DNMT1) was …

Nanaomycin A selectively inhibits DNMT3B and reactivates silenced tumor suppressor genes in human cancer cells

D Kuck, T Caulfield, F Lyko, JL Medina-Franco - Molecular cancer …, 2010 - AACR
Enzymes involved in the epigenetic regulation of the genome represent promising starting
points for therapeutic intervention by small molecules, and DNA methyltransferases (DNMT) …