Related Experiment Video

Updated: Feb 18, 2026

Silencing of BRCA2 to Identify Novel BRCA2-regulated Biological Functions in Cultured Human Cells
09:24

Silencing of BRCA2 to Identify Novel BRCA2-regulated Biological Functions in Cultured Human Cells

Published on: August 12, 2015

9.6K

Targeting bromodomain and extraterminal proteins in breast cancer

Jennifer M Sahni1, Ruth A Keri2

  • 1Department of Pharmacology, Case Western Reserve University, Cleveland, OH 44106, United States.

Pharmacological Research
|November 21, 2017
PubMed

Insights

Bromodomain and Extraterminal (BET) inhibitors show promise in suppressing breast cancer oncogenes. These epigenetic drugs are effective alone and synergize with other anti-cancer agents, warranting further investigation.

Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Breast cancer comprises diverse subtypes driven by unique gene expression profiles.
  • Epigenetic marks control gene expression, and aberrant epigenetic changes occur during carcinogenesis.
  • Epigenetic alterations are reversible, suggesting potential for epigenome-modulating drugs.

Purpose of the Study:

  • To review the impact of Bromodomain and Extraterminal (BET) family epigenetic reader inhibitors in breast cancer.
  • To explore the therapeutic potential of BET inhibitors in various breast cancer subtypes.

Main Methods:

  • Review of studies investigating BET inhibitors, such as JQ1, in breast cancer models.
  • Analysis of data on the efficacy and toxicity of BET inhibitors.
  • Examination of synergistic effects of BET inhibitors with approved anti-cancer drugs.

Main Results:

  • BET inhibitors suppress various oncogenic pathways in multiple breast cancer subtypes.
  • These agents demonstrate minimal toxicity in preclinical models.
  • BET inhibitors exhibit synergistic effects with approved anti-cancer drugs, enhancing treatment response.

Conclusions:

  • BET inhibitors represent a promising therapeutic strategy for breast cancer.
  • Their ability to silence oncogenes and synergize with existing treatments supports further clinical investigation.
  • Epigenetic therapy with BET inhibitors offers a novel approach to combatting breast cancer.
Keywords:
ARV-825 PubChem CID 92044400Anti-cancer drugsBET inhibitorBETd-246 PubChem CID 131698640Breast cancerBromodomain and extraterminal proteinDrug synergyI-BET151 PubChem CID 52912189I-BET762 PubChem CID 46943432JQ1 PubChem CID 46907787MS417 PubChem CID 59190723OTX015 PubChem CID 9936746THZ1 PubChem CID 73602827Transcriptional controlXD14 PubChem CID 52670832dBET1 PubChem CID 91799313

More Related Videos

Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts10:27

Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts

Published on: July 25, 2020

8.0K
High-Throughput Dissociation and Orthotopic Implantation of Breast Cancer Patient-Derived Xenografts06:06

High-Throughput Dissociation and Orthotopic Implantation of Breast Cancer Patient-Derived Xenografts

Published on: December 20, 2024

1.3K

Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
9.0K
Mitogens and the Cell Cycle02:38

Mitogens and the Cell Cycle

Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
8.2K
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
24
Abnormal Proliferation02:23

Abnormal Proliferation

Under normal conditions, most adult cells remain in a non-proliferative state unless stimulated by internal or external factors to replace lost cells. Abnormal cell proliferation is a condition in which the cell's growth exceeds and is uncoordinated with normal cells. In such situations, cell division persists in the same excessive manner even after cessation of the stimuli, leading to persistent tumors. The tumor arises from the damaged cells that replicate to pass the damage to the...
5.3K
mTOR Signaling and Cancer Progression03:03

mTOR Signaling and Cancer Progression

The mammalian target of rapamycin or mTOR protein was discovered in 1994 due to its direct interaction with rapamycin. The protein gets its name from a yeast homolog called TOR. The mTOR protein complex in mammalian cells plays a major role in balancing anabolic processes such as the synthesis of proteins, lipids, and nucleotides and catabolic processes, such as autophagy in response to environmental cues, such as availability of nutrients and growth factors.
The mTOR pathway or the...
4.9K