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 …

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 …

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 …

Emerging EZH2 inhibitors and their application in lymphoma

JK Lue, JE Amengual - Current hematologic malignancy reports, 2018 - Springer
Abstract Purpose of Review Enhancer of Zeste Homolog 2 (EZH2) is histone
methyltransferase and catalyzes the methylation of histone 3 lysine 27, a mark of …

Comprehensive Target Engagement by the EZH2 Inhibitor Tulmimetostat Allows for Targeting of ARID1A Mutant Cancers

PJ Keller, EJ Adams, R Wu, A Côté, S Arora… - Cancer …, 2024 - aacrjournals.org
Recurrent somatic mutations in the BRG1/BRM-associated factor (BAF) chromatin
remodeling complex subunit ARID1A occur frequently in advanced urothelial, endometrial …

Precision targeting with EZH2 and HDAC inhibitors in epigenetically dysregulated lymphomas

JK Lue, SA Prabhu, Y Liu, Y Gonzalez, A Verma… - Clinical Cancer …, 2019 - AACR
Purpose: Both gain-of-function enhancer of zeste homolog 2 (EZH2) mutations and
inactivating histone acetyltransferases mutations, such as CREBBP and EP300, have been …

Role of epigenetic regulation in plasticity of tumor immune microenvironment

Y Yang, Y Wang - Frontiers in Immunology, 2021 - frontiersin.org
The tumor immune microenvironment (TIME), an immunosuppressive niche, plays a pivotal
role in contributing to the development, progression, and immune escape of various types of …

Targeting PRC2 for the treatment of cancer: an updated patent review (2016-2020)

M Dockerill, C Gregson… - Expert Opinion on …, 2021 - Taylor & Francis
Introduction PRC2 is a histone methyltransferase complex associated with several cancer
types. Tazemetostat was recently approved as the first inhibitor targeting the catalytic subunit …

Chemical biology and pharmacology of histone lysine methylation inhibitors

SH Barghout, RAC Machado… - Biochimica et Biophysica …, 2022 - Elsevier
Histone lysine methylation is a post-translational modification that plays a key role in the
epigenetic regulation of a broad spectrum of biological processes. Moreover, the …

Follicular lymphoma: recent and emerging therapies, treatment strategies, and remaining unmet needs

MJ Matasar, S Luminari, PM Barr, SK Barta… - The …, 2019 - academic.oup.com
Follicular lymphoma (FL) is a heterogeneous disease with varying prognosis owing to
differences in clinical, laboratory, and disease parameters. Although generally considered …