Pharmacological targeting of the cancer epigenome

NW Mabe, JA Perry, CF Malone, K Stegmaier - Nature Cancer, 2024 - nature.com
Epigenetic dysregulation is increasingly appreciated as a hallmark of cancer, including
disease initiation, maintenance and therapy resistance. As a result, there have been …

Targeting key proteins involved in transcriptional regulation for cancer therapy: Current strategies and future prospective

H Pei, W Guo, Y Peng, H Xiong… - Medicinal Research …, 2022 - Wiley Online Library
The key proteins involved in transcriptional regulation play convergent roles in cellular
homeostasis, and their dysfunction mediates aberrant gene expressions that underline the …

Targeting EZH2 in SMARCB1-deficient sarcomas: advances and opportunities to potentiate the efficacy of EZH2 inhibitors

C Lanzi, N Arrighetti, S Pasquali, G Cassinelli - Biochemical Pharmacology, 2023 - Elsevier
Soft tissue sarcomas (STSs) are rare mesechymal malignancies characterized by distintive
molecular, histological and clinical features. Many STSs are considered as predominatly …

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 …

Chemical inhibitors targeting histone methylation readers

X Huang, Y Chen, Q Xiao, X Shang, Y Liu - Pharmacology & Therapeutics, 2024 - Elsevier
Histone methylation reader domains are protein modules that recognize specific histone
methylation marks, such as methylated or unmethylated lysine or arginine residues on …

Novel agents in relapsed/refractory diffuse large B‐cell lymphoma

G Varma, J Goldstein, RH Advani - Hematological Oncology, 2023 - Wiley Online Library
Patients with relapsed or refractory (R/R) diffuse large B‐cell lymphoma (DLBCL), ineligible
for or relapsing after autologous stem‐cell transplant or chimeric antigen‐receptor T‐cell …

Epigenetic therapies—update on lysine methyltransferase/PRC complex inhibitors

S Kim, N Barkey, O Atasoylu, D Dhanak - Epigenetic Cancer Therapy, 2023 - Elsevier
The approval of tazmetostat as the first EZH2 inhibitor for the treatment of epithelial sarcoma
and follicular lymphoma in 2020 has paved the way for the development of additional …

[PDF][PDF] Chemical biology and pharmacology of histone lysine methylation inhibitors

D Barsyte-Lovejoy - researchgate.net
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 …