Related Experiment Video

Updated: Dec 10, 2025

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
05:33

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

Published on: November 9, 2020

10.7K

PROTACs: New method to degrade transcription regulating proteins

Beichen Hu1, Yirong Zhou2, Dejuan Sun1

  • 1Wuya College of Innovation, Key Laboratory of Structure-Based Drug Design & Discovery, Ministry of Education, Shenyang Pharmaceutical University, Shenyang, 110016, China.

European Journal of Medicinal Chemistry
|August 29, 2020
PubMed

Insights

Proteolysis-targeting chimaeras (PROTACs) offer a novel therapeutic strategy for diseases caused by protein overexpression. These molecules efficiently degrade target proteins involved in transcription regulation, outperforming traditional inhibitors.

Area of Science:

  • Molecular Biology
  • Biochemistry
  • Drug Discovery

Background:

  • Transcription is a fundamental biological process involving numerous proteins, whose overexpression can lead to various diseases.
  • Current therapeutic inhibitors for transcription regulation show limited efficacy.
  • There is a need for advanced technologies to improve therapeutic outcomes for transcription-related diseases.

Purpose of the Study:

  • To review the emerging role of Proteolysis-Targeting Chimeras (PROTACs) in regulating transcription.
  • To highlight the advantages of PROTACs over traditional inhibitors for diseases driven by protein overexpression.
  • To summarize current PROTAC applications in disease treatment and biological research.

Main Methods:

  • Literature review of PROTAC technology.
  • Analysis of PROTACs targeting transcription regulators.
  • Discussion of PROTAC mechanisms and applications.

Main Results:

  • PROTACs are bifunctional molecules that induce target protein ubiquitination and proteasomal degradation.
  • PROTACs demonstrate superior efficiency in degrading overexpressed transcription regulators compared to inhibitors.
  • The review summarizes 29 PROTACs targeting transcription regulators, detailing their advantages.

Conclusions:

  • PROTACs represent a promising therapeutic modality for diseases linked to transcription dysregulation.
  • PROTACs offer enhanced efficacy for degrading target proteins, addressing limitations of conventional therapies.
  • PROTACs serve as valuable tools for both disease treatment and fundamental biological research in transcription.
Keywords:
EpigeneticPROTACsProtein degradationTranscription factor

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
Single-molecule Imaging of Gene Regulation In vivo Using Cotranslational Activation by Cleavage CoTrAC11:31

Single-molecule Imaging of Gene Regulation In vivo Using Cotranslational Activation by Cleavage CoTrAC

Published on: March 15, 2013

10.2K

Related Concept Videos

Transcription Attenuation in Prokaryotes02:42

Transcription Attenuation in Prokaryotes

Transcriptional attenuation occurs when RNA transcription is prematurely terminated due to the formation of a terminator mRNA hairpin structure.  Bacteria use these hairpins to regulate the transcription process and control the synthesis of several amino acids including histidine, lysine, threonine, and phenylalanine. Transcription attenuation takes place in the non-coding regions of mRNA.
There are several different mechanisms used to attenuate transcription. In ribosome mediated...
17.7K
Co-activators and Co-repressors02:04

Co-activators and Co-repressors

Gene transcription is regulated by the synergistic action of several proteins that form a complex at a gene regulatory site. This is observed in eukaryotes, where the regulation of gene expression is a complex process. Regulatory proteins in eukaryotes can broadly be classified into two types – regulators that bind directly to specific DNA sequences and co-regulators that associate with regulatory proteins but cannot directly bind to the DNA. These co-regulators are further divided into...
8.2K
RNA Polymerase II Accessory Proteins02:36

RNA Polymerase II Accessory Proteins

Proteins that regulate transcription can do so either via direct contact with RNA Polymerase or through indirect interactions facilitated by adaptors, mediators, histone-modifying proteins, and nucleosome remodelers. Direct interactions to activate transcription is seen in bacteria as well as in some eukaryotic genes. In these cases, upstream activation sequences are adjacent to the promoters, and the activator proteins interact directly with the transcriptional machinery. For example, in...
10.5K
Regulated Protein Degradation02:58

Regulated Protein Degradation

It is vital to regulate the activity of enzymatic as well as non-enzymatic proteins inside the cell. This can be achieved either through creating a balance between their rate of synthesis and degradation or regulating the intrinsic activity of the protein. Both these regulation mechanisms play an essential role in the normal functioning of cells.
Protein degradation plays two important roles in the cells. It helps to protect cells from misfolded or damaged proteins before they lead to a...
8.5K
Regulated Protein Degradation02:58

Regulated Protein Degradation

2.9K
Regulation of Expression at Multiple Steps01:23

Regulation of Expression at Multiple Steps

The gene expression in cells is regulated at different stages: (i) transcription, (ii) RNA processing, (iii) RNA localization, and (iv) translation. Transcriptional regulation is mediated by regulatory proteins such as transcription factors, activators, or repressors—these control gene expression by initiating or inhibiting the transcription of genes. Once a precursor or pre-mRNA is produced, it undergoes post-transcriptional modification, including 5' capping, splicing, and the...
1.2K