Related Experiment Video

Updated: Mar 25, 2026

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

8.4K

BET inhibitors in cancer therapeutics: a patent review

Anirban Ghoshal1, D Yugandhar1,2, Ajay Kumar Srivastava1,2

  • 1a Medicinal Chemistry and Pharmacology Division , CSIR - Indian Institute of Chemical Technology , Hyderabad , India.

Expert Opinion on Therapeutic Patents
|March 1, 2016
PubMed
Abstract

Insights

Bromodomain and Extra Terminal (BET) protein inhibition is a promising strategy for novel cancer therapeutics. Research in 2015 focused on BET inhibitors, with seven small molecules currently in clinical trials for cancer drug development.

Area of Science:

  • Oncology
  • Medicinal Chemistry
  • Drug Discovery

Background:

  • Bromodomain and Extra Terminal (BET) protein inhibition is an emerging strategy for advanced cancer therapeutics.
  • Over thirty patents were published in 2015 concerning cancer chemotherapeutics targeting BET proteins.
  • Seven small molecule BET inhibitors are currently undergoing clinical trials for anti-cancer drug development.

Purpose of the Study:

  • To review important patents from 2015 on the development of BET inhibitors as potential cancer therapeutics.
  • To analyze the structural chemical space, therapeutic applications, chemical classes, and structural modifications of these inhibitors.
  • To provide an overview of BET inhibitors currently in clinical trials.

Main Methods:

  • Patent analysis focusing on BET inhibitors published in 2015.
  • Review of structural chemical space related to BET inhibitors.
  • Compilation of data on therapeutic applications, chemical classes, and clinical trial status.

Main Results:

  • Significant patent activity in 2015 highlights the growing interest in BET inhibitors for cancer.
  • A diverse range of chemical classes and structural modifications are being explored.
  • Several BET inhibitors have advanced to clinical trials, indicating therapeutic potential.

Conclusions:

  • BET proteins represent a promising target class for developing novel anti-cancer agents.
  • Further molecular studies are needed to elucidate affected biological pathways and ensure selectivity among BET proteins.
  • In-silico molecular modeling can aid in designing selective BET inhibitors for anti-cancer drug discovery.
Keywords:
BETBromodomainBromodomain and Extra Terminal Proteinsanti-cancer

More Related Videos

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia10:49

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia

Published on: September 18, 2013

18.7K
Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays07:42

Assessment of Resistance to Tyrosine Kinase Inhibitors by an Interrogation of Signal Transduction Pathways by Antibody Arrays

Published on: September 19, 2018

8.4K

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...
9.1K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

1.7K
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...
6.2K
Inhibition of CDK Activity02:34

Inhibition of CDK Activity

5.6K
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...
6.3K
Tumor Immunotherapy01:27

Tumor Immunotherapy

Immunotherapy is a treatment that boosts or manipulates the immune system to fight diseases, including cancer. For instance, by stimulating an immune response through vaccinations against viruses that cause cancers, like hepatitis B virus and human papillomavirus, these diseases can be prevented. Nonetheless, some cancer cells can avoid the immune system due to their rapid mutation and division. The immune response to many cancers involves three phases: elimination, equilibrium, and escape.
2.2K