Related Experiment Video

Updated: Feb 2, 2026

In Vitro Analysis of E3 Ubiquitin Ligase Function
06:06

In Vitro Analysis of E3 Ubiquitin Ligase Function

Published on: May 14, 2021

6.0K

A patent review of the ubiquitin ligase system: 2015-2018

Xin Li1,2,3, Ekinci Elmira3, Sagar Rohondia3

  • 1a Department of Biotechnology , Guangdong Polytechnic of Science and Trade , Guangzhou , Guangdong , China.

Expert Opinion on Therapeutic Patents
|November 20, 2018
PubMed
Abstract

Insights

Targeting E3 enzymes, key components of the ubiquitin-proteasome system (UPS), offers a promising strategy for novel anticancer drug development. This review highlights recent advances and patents in E3 inhibitors and modulators for cancer therapy.

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Pharmacology

Background:

  • The ubiquitin-proteasome system (UPS) is a validated anticancer drug target.
  • UPS involves ubiquitination by E1, E2, and E3 enzymes and degradation by the 26S proteasome.
  • E3 enzymes are crucial for substrate specificity and represent significant therapeutic opportunities.

Purpose of the Study:

  • To review recent advancements in small molecule inhibitors targeting UPS enzymes (E1, E2, E3).
  • To focus on patents from 2015-2018 concerning E3 inhibitors and modulators.
  • To discuss the potential of E3 enzymes as next-generation anticancer drug targets.

Main Methods:

  • Literature review of recent scientific publications.
  • Analysis of patent literature (2015-2018) on E3 inhibitors and modulators.
  • Synthesis of current knowledge on E3 enzyme function in cancer.

Main Results:

  • Recent progress in developing small molecule inhibitors for E1, E2, and E3 enzymes.
  • Identification of E3 enzymes as promising targets to overcome limitations of current proteasome inhibitors.
  • Exploration of various strategies for E3 modulator development, including rational design and screening.

Conclusions:

  • E3 enzymes are critical regulators in cancer development and offer novel therapeutic targets.
  • Developing E3 inhibitors and modulators presents a viable strategy for next-generation anticancer drugs.
  • Further research into E3-substrate interactions is essential for effective drug discovery.
Keywords:
E3cancer therapydrug discoveryprotein ubiquitination and degradationubiquitin-proteasome system

More Related Videos

Functional Characterization of RING-Type E3 Ubiquitin Ligases In Vitro and In Planta10:27

Functional Characterization of RING-Type E3 Ubiquitin Ligases In Vitro and In Planta

Published on: December 5, 2019

9.4K
Evaluation of Substrate Ubiquitylation by E3 Ubiquitin-ligase in Mammalian Cell Lysates09:47

Evaluation of Substrate Ubiquitylation by E3 Ubiquitin-ligase in Mammalian Cell Lysates

Published on: May 10, 2022

3.1K

Related Concept Videos

Review and Preview01:10

Review and Preview

In statistics, several tools are used to interpret the data. Measures of central tendency represent the characteristics of the data, such as mean, median, and mode. Additionally, measures of variance like standard deviation and range are used to find the spread of data from the mean. Relative standing measures the distance between data locations. Commonly used measures of relative standings are percentile, z score, and quartiles.
Percentiles are a type of fractile that partition data into...
8.4K
Review and Preview01:13

Review and Preview

Data are individual items of information obtained from a population or sample. Data may be classified as qualitative (categorical), quantitative continuous, or quantitative discrete. Because it is not practical to measure the entire population in a study, researchers use samples to represent the population. A random sample is a representative group from the population chosen by using a method that gives each individual in the population an equal chance of being included in the sample. Random...
11.3K
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...
8.9K
The Proteasome02:18

The Proteasome

Eukaryotic cells can degrade proteins through several pathways. One of the most important amongst these is the ubiquitin-proteasome pathway. It helps the cell eliminate the misfolded, damaged, or unwarranted cytoplasmic proteins in a highly specific manner.
In this pathway, the target proteins are first tagged with small proteins called ubiquitin. A series of enzymes carry out the ubiquitination of the target proteins - E1 (ubiquitin-activating enzyme), E2 (ubiquitin-conjugating enzyme), and E3...
10.2K
Protein Complexes with Interchangeable Parts01:57

Protein Complexes with Interchangeable Parts

Groups of proteins may form a complex where each protein in this complex has a different role in the overall execution of the complex’s function. Often some of the proteins in the complex can be replaced by a closely related variant to give a complex that contains many of the same components yet is functionally distinct.
The SCF ubiquitin ligase is a protein complex of five individual proteins. This complex attaches ubiquitin to other target proteins to mark them for degradation. In order...
2.9K
Covalently Linked Protein Regulators02:04

Covalently Linked Protein Regulators

Proteins can undergo many types of post-translational modifications, often in response to changes in their environment. These modifications play an important role in the function and stability of these proteins. Covalently linked molecules include functional groups, such as methyl, acetyl, and phosphate groups, and also small proteins, such as ubiquitin. There are around 200 different types of covalent regulators that have been identified.
These groups modify specific amino acids in a protein....
9.6K