Emerging DNA methylation inhibitors for cancer therapy: challenges and prospects

A Gonzalez-Fierro… - Expert Review of …, 2019 - Taylor & Francis
Introduction: There is evidence of the association of DNA methylation alterations with cancer
development and progression. Areas covered: This review will briefly discuss the basis of …

DNA methyltransferase inhibitors in cancer: a chemical and therapeutic patent overview and selected clinical studies

J Fahy, A Jeltsch, PB Arimondo - Expert opinion on therapeutic …, 2012 - Taylor & Francis
Introduction: DNA methylation is an epigenetic modification that modulates gene expression
without altering the DNA base sequence. It plays a crucial role in cancer by silencing tumor …

[HTML][HTML] Demethylating agents in the treatment of cancer

PM Howell Jr, Z Liu, HT Khong - Pharmaceuticals, 2010 - mdpi.com
Gene silencing resulting from aberrant DNA methylation can lead to tumorigenesis.
Therefore, drugs that inhibit or interfere with DNA methylation have been used to reactivate …

Targeting DNA methylation

JPJ Issa, HM Kantarjian - Clinical Cancer Research, 2009 - AACR
Two nucleoside inhibitors of DNA methylation, azacitidine and decitabine, are now standard
of care for the treatment of the myelodysplastic syndrome, a deadly form of leukemia. These …

Therapeutics and DNA methylation inhibitors

SC Navada - Medical Epigenetics, 2021 - Elsevier
Dysregulation of cellular epigenetic machinery is linked to the pathogenesis of a number of
malignancies and has been studied extensively in myelodysplastic syndromes and acute …

Inhibitors of DNA methylation: beyond myelodysplastic syndromes

P Fenaux - Nature clinical practice Oncology, 2005 - nature.com
DNA methyltransferase (DNMT) inhibitors, azacitidine (Vidaza®, Pharmion, Boulder, CO,
USA) and decitabine (Dacogen™; SuperGen Inc, Dublin, CA, USA, and MGI Pharma Inc …

[HTML][HTML] Targeting DNA methylation in leukemia, myelodysplastic syndrome, and lymphoma: a potential diagnostic, prognostic, and therapeutic tool

L Kalinkova, A Sevcikova, V Stevurkova… - International Journal of …, 2022 - mdpi.com
DNA methylation represents a crucial mechanism of epigenetic regulation in hematologic
malignancies. The methylation process is controlled by specific DNA methyl transferases …

Role of DNA methylation in the pathogenesis and treatment of myelodysplastic syndromes

H Khan, C Vale, T Bhagat, A Verma - Seminars in hematology, 2013 - Elsevier
The myelodysplastic syndromes (MDS) are a group of hematologic disorders characterized
by ineffective hematopoiesis and increased risk of transformation to acute myeloid leukemia …

DNA hypermethylation as a chemotherapy target

J Ren, BN Singh, Q Huang, Z Li, Y Gao, P Mishra… - Cellular signalling, 2011 - Elsevier
Epigenetics refers to partially reversible, somatically inheritable, but DNA sequence-
independent traits that modulate gene expression, chromatin structure, and cell functions …

[HTML][HTML] DNMT inhibitors increase methylation in the cancer genome

AK Giri, T Aittokallio - Frontiers in pharmacology, 2019 - frontiersin.org
DNA methyltransferase inhibitors (DNMTi) decitabine and azacytidine are approved
therapies for myelodysplastic syndrome and acute myeloid leukemia, and their …