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Pharmacological targeting of the cancer epigenome
Epigenetic dysregulation is increasingly appreciated as a hallmark of cancer, including
disease initiation, maintenance and therapy resistance. As a result, there have been …
disease initiation, maintenance and therapy resistance. As a result, there have been …
Chromatin remodellers as therapeutic targets
HA Malone, CWM Roberts - Nature Reviews Drug Discovery, 2024 - nature.com
Large-scale cancer genome sequencing studies have revealed that chromatin regulators
are frequently mutated in cancer. In particular, more than 20% of cancers harbour mutations …
are frequently mutated in cancer. In particular, more than 20% of cancers harbour mutations …
Targeting DCAF5 suppresses SMARCB1-mutant cancer by stabilizing SWI/SNF
Whereas oncogenes can potentially be inhibited with small molecules, the loss of tumour
suppressors is more common and is problematic because the tumour-suppressor proteins …
suppressors is more common and is problematic because the tumour-suppressor proteins …
NSD2 is a requisite subunit of the AR/FOXA1 neo-enhanceosome in promoting prostate tumorigenesis
Androgen receptor (AR) is a ligand-responsive transcription factor that drives terminal
differentiation of the prostatic luminal epithelia. By contrast, in tumors originating from these …
differentiation of the prostatic luminal epithelia. By contrast, in tumors originating from these …
Chromatin regulation of transcriptional enhancers and cell fate by the Sotos syndrome gene NSD1
Nuclear receptor-binding SET-domain protein 1 (NSD1), a methyltransferase that catalyzes
H3K36me2, is essential for mammalian development and is frequently dysregulated in …
H3K36me2, is essential for mammalian development and is frequently dysregulated in …
Epigenetic therapies targeting histone lysine methylation: complex mechanisms and clinical challenges
S Gold, A Shilatifard - The Journal of Clinical Investigation, 2024 - jci.org
As epigenetic therapies continue to gain ground as potential treatment strategies for cancer
and other diseases, compounds that target histone lysine methylation and the enzyme …
and other diseases, compounds that target histone lysine methylation and the enzyme …
Lineage-specific canonical and non-canonical activity of EZH2 in advanced prostate cancer subtypes
Enhancer of zeste homolog 2 (EZH2) is a histone methyltransferase and emerging
therapeutic target that is overexpressed in most castration-resistant prostate cancers and …
therapeutic target that is overexpressed in most castration-resistant prostate cancers and …
Overcoming clinical resistance to EZH2 inhibition using rational epigenetic combination therapy
Y Kazansky, D Cameron, HS Mueller… - Cancer …, 2024 - aacrjournals.org
Epigenetic dependencies have become evident in many cancers. On the basis of
antagonism between BAF/SWI-SNF and PRC2 in SMARCB1-deficient sarcomas, we …
antagonism between BAF/SWI-SNF and PRC2 in SMARCB1-deficient sarcomas, we …
Targeting EZH2 in SMARCB1-deficient sarcomas: advances and opportunities to potentiate the efficacy of EZH2 inhibitors
Soft tissue sarcomas (STSs) are rare mesechymal malignancies characterized by distintive
molecular, histological and clinical features. Many STSs are considered as predominatly …
molecular, histological and clinical features. Many STSs are considered as predominatly …
Epigenetic reprogramming in pediatric gliomas: from molecular mechanisms to therapeutic implications
Brain tumors in children and adults differ greatly in patient outcomes and responses to
radiotherapy and chemotherapy. Moreover, the prevalence of recurrent mutations in …
radiotherapy and chemotherapy. Moreover, the prevalence of recurrent mutations in …