Related Experiment Video

Updated: Aug 24, 2025

Identification of Transcription Factor Regulators using Medium-Throughput Screening of Arrayed Libraries and a Dual-Luciferase-Based Reporter
11:32

Identification of Transcription Factor Regulators using Medium-Throughput Screening of Arrayed Libraries and a Dual-Luciferase-Based Reporter

Published on: March 27, 2020

7.0K

Targeting Transcription Factors in Cancer: From "Undruggable" to "Druggable"

Zhipeng Tao1, Xu Wu2

  • 1Cutaneous Biology Research Center, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA, USA. ZTAO@mgh.harvard.edu.

Methods in Molecular Biology (Clifton, N.J.)
|October 20, 2022
PubMed

Insights

Transcription factors are key in cancer development. New strategies are emerging to target these "undruggable" proteins, offering potential new cancer therapies.

Area of Science:

  • Oncology
  • Molecular Biology
  • Cancer Genetics

Background:

  • Transcription factor deregulation is a critical hallmark of cancer.
  • Dysfunctional transcription factors drive cancer initiation, progression, and metastasis through various genetic and epigenetic alterations.
  • Transcription factors are traditionally considered

Purpose of the Study:

  • To review recent advancements in understanding transcription factor regulation in cancer.
  • To explore strategies for targeting transcription factors and co-factors in drug development.
  • To focus on key cancer-associated transcription factors: c-Myc, YAP/TAZ, and β-catenin.

Main Methods:

  • Literature review of recent preclinical and clinical studies.
  • Analysis of molecular mechanisms regulating transcription factor activity in cancer.
  • Examination of therapeutic strategies targeting transcription factors and their co-factors.

Main Results:

  • Transcription factor dysfunction is implicated in multiple cancer hallmarks.
  • Despite being considered "undruggable," novel strategies are being developed to target transcription factors.
  • Specific transcription factors like c-Myc, YAP/TAZ, and β-catenin are significant targets due to their roles and interplays in cancer.

Conclusions:

  • Targeting transcription factors represents a promising frontier in cancer therapy.
  • Understanding the complex regulation of transcription factors is crucial for developing effective treatments.
  • Further research into targeting transcription factors like c-Myc, YAP/TAZ, and β-catenin holds significant therapeutic potential.
Keywords:
CancerDruggableTranscription co-factorsTranscription factorUndruggable

More Related Videos

Utilizing Functional Genomics Screening to Identify Potentially Novel Drug Targets in Cancer Cell Spheroid Cultures07:48

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

Published on: December 26, 2016

11.5K
Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down08:59

Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down

Published on: December 11, 2017

7.3K

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...
7.8K
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...
3.4K
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...
7.2K
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
2.7K
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...
5.0K
Drug Discovery: Overview01:26

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...
8.3K