Rational combinations of targeted cancer therapies: background, advances and challenges
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 …
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
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 …
[HTML][HTML] Lineage tracing reveals the phylodynamics, plasticity, and paths of tumor evolution
Tumor evolution is driven by the progressive acquisition of genetic and epigenetic
alterations that enable uncontrolled growth and expansion to neighboring and distal tissues …
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
Epigenetics is dynamic and heritable modifications to the genome that occur independently
of DNA sequence. It requires interactions cohesively with various enzymes and other …
of DNA sequence. It requires interactions cohesively with various enzymes and other …
The roles of DNA, RNA and histone methylation in ageing and cancer
Chromatin is a macromolecular complex predominantly comprising DNA, histone proteins
and RNA. The methylation of chromatin components is highly conserved as it helps …
and RNA. The methylation of chromatin components is highly conserved as it helps …
[HTML][HTML] Leukemic stem cells and therapy resistance in acute myeloid leukemia
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 …
relapse after achieving remission. The latter arises from a few therapy-resistant cells within …
Eukaryotic core promoters and the functional basis of transcription initiation
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 …
transcription start sites of protein-coding and non-coding genes that support the assembly of …
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 …
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 …
proteins enable chromatin binding to facilitate transcription. Drugs that inhibit both …
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 …
found in proteins with varied functions, were highly tractable small-molecule targets. This is …