Related Experiment Video

Updated: May 25, 2025

Utilizing Functional Genomics Screening to Identify Potentially Novel Drug Targets in Cancer Cell Spheroid Cultures
07:48

Utilizing Functional Genomics Screening to Identify Potentially Novel Drug Targets in Cancer Cell Spheroid Cultures

Published on: December 26, 2016

11.3K

Cellular Epigenetic Targets and Epidrugs in Breast Cancer Therapy: Mechanisms, Challenges, and Future Perspectives

Ibrahim S Alalhareth1, Saleh M Alyami1, Ali H Alshareef2

  • 1College of Pharmacy, Najran University, Najran 66256, Saudi Arabia.

Pharmaceuticals (Basel, Switzerland)
|February 26, 2025
PubMed

Insights

Epigenetic modifications play a crucial role in breast cancer development and drug resistance. Reprogramming the epigenome with epidrugs offers a promising therapeutic strategy, especially in combination with immune checkpoint inhibitors.

Area of Science:

  • Oncology
  • Epigenetics
  • Molecular Biology

Background:

  • Breast cancer is a heterogeneous malignancy influenced by diverse molecular characteristics.
  • Epigenetic modifications, including DNA methylation and histone alterations, are increasingly recognized in breast cancer pathogenesis, impacting drug resistance and progression.
  • These modifications offer potential as diagnostic/prognostic markers and therapeutic targets.

Purpose of the Study:

  • To review the role of aberrant epigenetic regulation in breast cancer initiation and progression.
  • To examine existing and emerging epidrugs for breast cancer treatment.
  • To explore combination therapies involving epidrugs.

Main Methods:

  • Literature review focusing on epigenetic modifications in breast cancer.
  • Analysis of studies on DNA methylation and histone modifications (acetylation, methylation, demethylation).
  • Examination of epidrugs targeting these modifications and their clinical applications.

Main Results:

  • Epigenetic reprogramming is a viable strategy to overcome drug resistance in breast cancer.
  • Epidrugs targeting DNA methylation and histone modifications show therapeutic potential.
  • Combination therapies, particularly epidrugs with immune checkpoint inhibitors, are highly promising.

Conclusions:

  • Aberrant epigenetic regulation is central to breast cancer progression and drug resistance.
  • Epidrugs represent a novel therapeutic avenue for breast cancer, with combination therapies showing significant promise.
  • Further research is needed to overcome obstacles in the clinical application of epidrugs.
Keywords:
Breast cancerDNA methylationepidrugsepigeneticshistone acetyl-transferase and histone deacetylase inhibitorshistone methyltransferase and demethyltransferase inhibitorshistone modification

More Related Videos

Author Spotlight: Exploring Salidroside's Molecular Mechanisms in Breast Cancer Treatment11:13

Author Spotlight: Exploring Salidroside's Molecular Mechanisms in Breast Cancer Treatment

Published on: June 9, 2023

1.5K
Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers10:28

Repressing Gene Transcription by Redirecting Cellular Machinery with Chemical Epigenetic Modifiers

Published on: September 20, 2018

6.4K

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...
7.4K
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...
6.4K
Inhibition of Cdk Activity02:34

Inhibition of Cdk Activity

The orderly progression of the cell cycle depends on the activation of Cdk protein by binding to its cyclin partner. However, the cell cycle must be restricted when undergoing abnormal changes. Most cancers correlate to the deregulated cell cycle, and since Cdks are a central component of the cell cycle, Cdk inhibitors are extensively studied to develop anticancer agents. For instance, cyclin D associates with several Cdks, such as Cdk 4/6, to form an active complex. The cyclin D-Cdk4/6 complex...
4.6K
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
6.0K
Epigenetic Regulation01:37

Epigenetic Regulation

Epigenetic changes alter the physical structure of the DNA without changing the genetic sequence and often regulate whether genes are turned on or off. This regulation ensures that each cell produces only proteins necessary for its function. For example, proteins that promote bone growth are not produced in muscle cells. Epigenetic mechanisms play an essential role in healthy development. Conversely, precisely regulated epigenetic mechanisms are disrupted in diseases like cancer.
X-chromosome...
3.0K
Combination Therapies and Personalized Medicine02:50

Combination Therapies and Personalized Medicine

Combining two or more treatment methods increases the life span of cancer patients while reducing damage to vital organs or tissue from the overuse of a single treatment. Combination therapy also targets different cancer-inducing pathways, thus reducing the chances of developing resistance to treatment.
The combination of the drug acetazolamide and sulforaphane is a good example of combination therapy to treat cancer. The cells in the interior of a large tumor often die due to the hypoxic and...
4.8K