Related Experiment Video

Updated: Dec 19, 2025

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog
08:37

Fluorescence-based Monitoring of PAD4 Activity via a Pro-fluorescence Substrate Analog

Published on: November 5, 2014

10.2K

Novel strategies targeting bromodomain-containing protein 4 (BRD4) for cancer drug discovery

Dailin Liang1, Yifan Yu1, Zonghui Ma1

  • 1Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing, 210009, China.

European Journal of Medicinal Chemistry
|June 6, 2020
PubMed

Insights

Novel strategies are needed to develop selective BRD4 inhibitors, as current drugs cause side effects. This review summarizes new approaches targeting BRD4 for improved cancer and disease treatment.

Area of Science:

  • Epigenetics
  • Molecular Biology
  • Medicinal Chemistry

Background:

  • BRD4, a BET protein, is crucial in diseases like cancer and inflammation.
  • Current BRD4 inhibitors lack selectivity, leading to toxic side effects.
  • There's an urgent need for improved BRD4 inhibitor strategies.

Purpose of the Study:

  • To summarize recent advancements in novel strategies targeting BRD4.
  • To highlight opportunities for developing selective and efficacious BRD4 inhibitors.

Main Methods:

  • Review of recent scientific literature on BRD4 inhibitor development.
  • Analysis of novel strategies for targeting BRD4.
  • Discussion of therapeutic potential and challenges.

Main Results:

  • Several novel strategies for BRD4 inhibition have emerged.
  • These strategies aim to enhance selectivity for BRD4 BD1/BD2.
  • Potential for reduced side effects and improved therapeutic outcomes.

Conclusions:

  • New strategies offer promise for selective BRD4 inhibition.
  • Further research can lead to more effective treatments for various diseases.
  • Targeting BRD4 remains a key area in drug discovery.
Keywords:
BRD4Bivalent inhibitorsDual target inhibitorsEpigenetic readersKAcPTOTACs

More Related Videos

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs10:44

Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

Published on: May 15, 2019

13.6K
Sequential Salt Extractions for the Analysis of Bulk Chromatin Binding Properties of Chromatin Modifying Complexes07:41

Sequential Salt Extractions for the Analysis of Bulk Chromatin Binding Properties of Chromatin Modifying Complexes

Published on: October 2, 2017

8.8K

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...
8.5K
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...
5.8K
Treatment Resistant Cancers02:56

Treatment Resistant Cancers

Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...
3.6K
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...
5.0K
Adaptive Mechanisms in Cancer Cells02:53

Adaptive Mechanisms in Cancer Cells

Cancer cells accumulate genetic changes at an abnormally rapid rate due to the defects in the DNA repair mechanisms. From an evolutionary perspective, such genetic instability is advantageous for cancer development. Mutant cell lines accumulate a series of beneficial mutations that contribute to their progression into cancer.
Some of the advantages that cancer cells have on normal cells include - enhanced ability to divide without terminally differentiating, induce new blood vessel formation,...
6.8K
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...
5.4K