Achieving clinical success with BET inhibitors as anti-cancer agents

T Shorstova, WD Foulkes, M Witcher - British journal of cancer, 2021 - nature.com
The transcriptional upregulation of oncogenes is a driving force behind the progression of
many tumours. However, until a decade ago, the concept of 'switching off'these oncogenic …

Glioma epigenetics: from subclassification to novel treatment options

O Gusyatiner, ME Hegi - Seminars in cancer biology, 2018 - Elsevier
Gliomas are the most common malignant primary brain tumors, of which glioblastoma is the
most malignant form (WHO grade IV), and notorious for treatment resistance. Over the last …

QKI shuttles internal m7G-modified transcripts into stress granules and modulates mRNA metabolism

Z Zhao, Y Qing, L Dong, L Han, D Wu, Y Li, W Li, J Xue… - Cell, 2023 - cell.com
Summary N 7-methylguanosine (m 7 G) modification, routinely occurring at mRNA 5′ cap
or within tRNAs/rRNAs, also exists internally in messenger RNAs (mRNAs). Although m 7 G …

Epigenetic therapy ties MYC depletion to reversing immune evasion and treating lung cancer

MJ Topper, M Vaz, KB Chiappinelli, CEDS Shields… - Cell, 2017 - cell.com
Combining DNA-demethylating agents (DNA methyltransferase inhibitors [DNMTis]) with
histone deacetylase inhibitors (HDACis) holds promise for enhancing cancer immune …

From signalling pathways to targeted therapies: unravelling glioblastoma's secrets and harnessing two decades of progress

B Dewdney, MR Jenkins, SA Best, S Freytag… - … and Targeted Therapy, 2023 - nature.com
Glioblastoma, a rare, and highly lethal form of brain cancer, poses significant challenges in
terms of therapeutic resistance, and poor survival rates for both adult and paediatric patients …

Modulation of the proteostasis network promotes tumor resistance to oncogenic KRAS inhibitors

X Lv, X Lu, J Cao, Q Luo, Y Ding, F Peng, A Pataer… - Science, 2023 - science.org
Despite substantial advances in targeting mutant KRAS, tumor resistance to KRAS inhibitors
(KRASi) remains a major barrier to progress. Here, we report proteostasis reprogramming as …

Selective small molecule induced degradation of the BET bromodomain protein BRD4

M Zengerle, KH Chan, A Ciulli - ACS chemical biology, 2015 - ACS Publications
The Bromo-and Extra-Terminal (BET) proteins BRD2, BRD3, and BRD4 play important roles
in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET …

[HTML][HTML] Glioblastoma targeted therapy: updated approaches from recent biological insights

M Touat, A Idbaih, M Sanson, KL Ligon - Annals of Oncology, 2017 - Elsevier
Glioblastoma (WHO grade IV astrocytoma) is the most frequent primary brain tumor in adults,
representing a highly heterogeneous group of neoplasms that are among the most …

[HTML][HTML] Enhanced efficacy of combined temozolomide and bromodomain inhibitor therapy for gliomas using targeted nanoparticles

FC Lam, SW Morton, J Wyckoff, TL Vu Han… - Nature …, 2018 - nature.com
Effective treatment for glioblastoma (GBM) is limited by the presence of the blood–brain
barrier (BBB) and rapid resistance to single agent therapies. To address these issues, we …

Targeting bromodomains: epigenetic readers of lysine acetylation

P Filippakopoulos, S Knapp - Nature reviews Drug discovery, 2014 - nature.com
Lysine acetylation is a key mechanism that regulates chromatin structure; aberrant
acetylation levels have been linked to the development of several diseases. Acetyl-lysine …