[HTML][HTML] The promise for histone methyltransferase inhibitors for epigenetic therapy in clinical oncology: a narrative review

HS Rugo, I Jacobs, S Sharma, F Scappaticci… - Advances in …, 2020 - Springer
Epigenetic processes are essential for normal development and the maintenance of tissue-
specific gene expression in mammals. Changes in gene expression and malignant cellular …

Use of histone methyltransferase inhibitors in cancer treatment: A systematic review

LL Marzochi, CI Cuzziol… - European journal of …, 2023 - Elsevier
Histone modifications are an epigenetic mechanism, and the dysregulation of these proteins
is known to be associated with the initiation and progression of cancer. In the search for the …

The importance of being me: magic methyls, methyltransferase inhibitors, and the discovery of tazemetostat

KW Kuntz, JE Campbell, H Keilhack… - Journal of medicinal …, 2016 - ACS Publications
Posttranslational methylation of histones plays a critical role in gene regulation.
Misregulation of histone methylation can lead to oncogenic transformation. Enhancer of …

The importance of non-histone protein methylation in cancer therapy

M Rodríguez-Paredes, F Lyko - Nature reviews Molecular cell biology, 2019 - nature.com
Epigenetic regulatory enzymes are generally considered innovative targets for cancer
therapy and several histone methyltransferase inhibitors are currently being evaluated in …

Epigenetic therapy: histone acetylation, DNA methylation and anti-cancer drug discovery

A Ganesan, L Nolan, SJ Crabb… - Current Cancer Drug …, 2009 - ingentaconnect.com
Histone proteins are subject to a diverse range of post-translational modifications which,
along with DNA methylation, play a major role in controlling gene expression, cell division …

Histone methyltransferase inhibitors: novel epigenetic agents for cancer treatment

C Zagni, U Chiacchio… - Current medicinal …, 2013 - ingentaconnect.com
Epigenetics is defined as heritable changes in gene activity and expression that occur
without alteration in DNA sequence. The gene transcription is strictly correlated to chromatin …

[HTML][HTML] Targeting histone methylation for cancer therapy: enzymes, inhibitors, biological activity and perspectives

Y Song, F Wu, J Wu - Journal of hematology & oncology, 2016 - Springer
Post-translational methylation of histone lysine or arginine residues plays important roles in
gene regulation and other physiological processes. Aberrant histone methylation caused by …

Drugging histone methyltransferases in cancer

L Richart, R Margueron - Current Opinion in Chemical Biology, 2020 - Elsevier
Targeting chromatin-modifying enzymes is a promising strategy for cancer treatment. The
antitumor effectivity of compounds inhibiting histone methyltransferases—mainly EZH2—is …

Emerging epigenetic targets and therapies in cancer medicine

R Popovic, JD Licht - Cancer discovery, 2012 - AACR
Abnormalities in the epigenetic regulation of chromatin structure and function can lead to
aberrant gene expression and cancer development. Consequently, epigenetic therapies aim …

Cancer treatment of the future: inhibitors of histone methyltransferases

A Spannhoff, W Sippl, M Jung - The international journal of biochemistry & …, 2009 - Elsevier
Cancer in humans is the result of a multi-step process. This process often involves the
activation of oncogenes and/or the inactivation of tumor suppressor genes. These two steps …