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Epigenetic & Transcriptional Therapy

Epigenetic and transcriptional therapy changes how genes are read rather than the genes themselves.

DNMT and HDAC inhibitors (haematologic malignancies), EZH2 inhibitors, IDH inhibitors, menin inhibitors (revumenib), BET inhibitors, and emerging transcription-factor degraders. Mostly established in blood cancers; solid tumours are catching up.

Epigenetic & Transcriptional Therapy: how this front works · animated schematic, not to scale

Technologies

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Approved
Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET)

Drugs that change how genes are switched on and off without changing the DNA itself.

Concept
Epigenetic editing (durable gene silencing)

Switching a gene off for good without changing the DNA sequence, by writing chemical marks onto it.

Key papers

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reviewCancer Discovery 2022
Hallmarks of Cancer 2022: adding phenotypic plasticity, epigenetic reprogramming, microbiomes and senescent cells

Cancer is now understood to change its identity and behaviour without new mutations, to be shaped by bacteria inside and around it, and to be helped along by ageing cells. This explains why some tumours escape targeted drugs by changing cell type and why gut bacteria affect immunotherapy response.

Connected

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technologies

2
Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET)Epigenetic editing (durable gene silencing)

companies

5
Kura OncologyMorphoSys (Novartis)ServierSyndax PharmaceuticalsTaiho Oncology (Otsuka)

institutions

2
Ruijin Hospital, Shanghai Jiao Tong UniversityUSC Norris Comprehensive Cancer Center

key papers

1
Hallmarks of Cancer 2022: adding phenotypic plasticity, epigenetic reprogramming, microbiomes and senescent cells