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Achieving clinical success with BET inhibitors as anti-cancer agents
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 …
many tumours. However, until a decade ago, the concept of 'switching off'these oncogenic …
Glioma epigenetics: from subclassification to novel treatment options
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 …
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
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 …
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 …
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
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 …
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
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 …
(KRASi) remains a major barrier to progress. Here, we report proteostasis reprogramming as …
Selective small molecule induced degradation of the BET bromodomain protein BRD4
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 …
in transcriptional regulation, epigenetics, and cancer and are the targets of pan-BET …
[HTML][HTML] Glioblastoma targeted therapy: updated approaches from recent biological insights
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 …
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 …
barrier (BBB) and rapid resistance to single agent therapies. To address these issues, we …
Targeting bromodomains: epigenetic readers of lysine acetylation
Lysine acetylation is a key mechanism that regulates chromatin structure; aberrant
acetylation levels have been linked to the development of several diseases. Acetyl-lysine …
acetylation levels have been linked to the development of several diseases. Acetyl-lysine …