Epigenetics-targeted drugs: Current paradigms and future challenges

W Dai, X Qiao, Y Fang, R Guo, P Bai, S Liu… - … and Targeted Therapy, 2024 - nature.com
Epigenetics governs a chromatin state regulatory system through five key mechanisms: DNA
modification, histone modification, RNA modification, chromatin remodeling, and non-coding …

The epigenetic hallmarks of cancer

M Esteller, MA Dawson, C Kadoch, FV Rassool… - Cancer …, 2024 - aacrjournals.org
Cancer is a complex disease in which several molecular and cellular pathways converge to
foster the tumoral phenotype. Notably, in the latest iteration of the cancer hallmarks,“ …

Transcriptional heterogeneity overcomes super-enhancer disrupting drug combinations in multiple myeloma

SJ Welsh, BG Barwick, EW Meermeier, DL Riggs… - Blood cancer …, 2024 - AACR
Multiple myeloma (MM) is a malignancy that is often driven by MYC and that is sustained by
IRF4, which are upregulated by super-enhancers. IKZF1 and IKZF3 bind to super-enhancers …

Targeting Protein–Protein Interactions in Hematologic Malignancies

T Cierpicki, J Grembecka - Annual Review of Pathology …, 2025 - annualreviews.org
Over the last two decades, there have been extensive efforts to develop small-molecule
inhibitors of protein–protein interactions (PPIs) as novel therapeutics for cancer, including …

Integrating text mining with network models for successful target identification: in vitro validation in MASH-induced liver fibrosis

J Venhorst, R Hanemaaijer, R Dulos… - Frontiers in …, 2024 - frontiersin.org
An in silico target discovery pipeline was developed by including a directional and weighted
molecular disease network for metabolic dysfunction-associated steatohepatitis (MASH) …

Group 3 medulloblastoma transcriptional networks collapse under domain specific EP300/CBP inhibition

NAM Shendy, M Bikowitz, LH Sigua, Y Zhang… - Nature …, 2024 - nature.com
Chemical discovery efforts commonly target individual protein domains. Many proteins,
including the EP300/CBP histone acetyltransferases (HATs), contain several targetable …

AR coactivators, CBP/p300, are critical mediators of DNA repair in prostate cancer

S Sardar, CM McNair, L Ravindranath, SN Chand… - Oncogene, 2024 - nature.com
Castration resistant prostate cancer (CRPC) remains an incurable disease stage with
ineffective treatments options. Here, the androgen receptor (AR) coactivators CBP/p300 …

IRF4 requires ARID1A to establish plasma cell identity in multiple myeloma

A Bolomsky, M Ceribelli, S Scheich, K Rinaldi… - Cancer Cell, 2024 - cell.com
Multiple myeloma (MM) is an incurable plasma cell malignancy that exploits transcriptional
networks driven by IRF4. We employ a multi-omics approach to discover IRF4 …

Exploring the landscape of post-translational modification in drug discovery

Y Cao, T Yu, Z Zhu, Y Zhang, S Sun, N Li, C Gu… - Pharmacology & …, 2024 - Elsevier
Post-translational modifications (PTMs) play a crucial role in regulating protein function, and
their dysregulation is frequently associated with various diseases. The emergence of …

Targeting lysine acetylation readers and writers

MM Zhou, PA Cole - Nature Reviews Drug Discovery, 2024 - nature.com
Lysine acetylation is a major post-translational modification in histones and other proteins
that is catalysed by the 'writer'lysine acetyltransferases (KATs) and mediates interactions …