Rational combinations of targeted cancer therapies: background, advances and challenges

H Jin, L Wang, R Bernards - Nature Reviews Drug Discovery, 2023 - nature.com
Over the past two decades, elucidation of the genetic defects that underlie cancer has
resulted in a plethora of novel targeted cancer drugs. Although these agents can initially be …

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 …

[HTML][HTML] Lineage tracing reveals the phylodynamics, plasticity, and paths of tumor evolution

D Yang, MG Jones, S Naranjo, WM Rideout, KHJ Min… - Cell, 2022 - cell.com
Tumor evolution is driven by the progressive acquisition of genetic and epigenetic
alterations that enable uncontrolled growth and expansion to neighboring and distal tissues …

Epigenetic regulation in human cancer: the potential role of epi-drug in cancer therapy

Y Lu, YT Chan, HY Tan, S Li, N Wang, Y Feng - Molecular cancer, 2020 - Springer
Epigenetics is dynamic and heritable modifications to the genome that occur independently
of DNA sequence. It requires interactions cohesively with various enzymes and other …

The roles of DNA, RNA and histone methylation in ageing and cancer

EM Michalak, ML Burr, AJ Bannister… - Nature reviews Molecular …, 2019 - nature.com
Chromatin is a macromolecular complex predominantly comprising DNA, histone proteins
and RNA. The methylation of chromatin components is highly conserved as it helps …

Eukaryotic core promoters and the functional basis of transcription initiation

V Haberle, A Stark - Nature reviews Molecular cell biology, 2018 - nature.com
Abstract RNA polymerase II (Pol II) core promoters are specialized DNA sequences at
transcription start sites of protein-coding and non-coding genes that support the assembly of …

[HTML][HTML] Leukemic stem cells and therapy resistance in acute myeloid leukemia

P Stelmach, A Trumpp - Haematologica, 2023 - ncbi.nlm.nih.gov
A major obstacle in the treatment of acute myeloid leukemia (AML) is refractory disease or
relapse after achieving remission. The latter arises from a few therapy-resistant cells within …

Bromodomains: a new target class for drug development

AG Cochran, AR Conery, RJ Sims III - Nature Reviews Drug Discovery, 2019 - nature.com
Less than a decade ago, it was shown that bromodomains, acetyl lysine 'reader'modules
found in proteins with varied functions, were highly tractable small-molecule targets. This is …

High-throughput single-cell ChIP-seq identifies heterogeneity of chromatin states in breast cancer

K Grosselin, A Durand, J Marsolier, A Poitou… - Nature …, 2019 - nature.com
Modulation of chromatin structure via histone modification is a major epigenetic mechanism
and regulator of gene expression. However, the contribution of chromatin features to tumor …

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation

O Gilan, I Rioja, K Knezevic, MJ Bell, MM Yeung… - Science, 2020 - science.org
The two tandem bromodomains of the BET (bromodomain and extraterminal domain)
proteins enable chromatin binding to facilitate transcription. Drugs that inhibit both …