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The Proteasome02:18

The Proteasome

9.9K
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...
9.9K
The Proteasome01:13

The Proteasome

1.5K
Eukaryotic cells can degrade proteins through several pathways. One of the most important among 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. This involves participation of a series of enzymes including— E1 (ubiquitin-activating enzyme), E2 (ubiquitin-conjugating enzyme), and E3...
1.5K
Regulated Protein Degradation02:58

Regulated Protein Degradation

2.9K
2.9K
Regulated Protein Degradation02:58

Regulated Protein Degradation

8.6K
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...
8.6K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

8.5K
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
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

9.8K
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...
9.8K

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Related Experiment Video

Updated: Dec 22, 2025

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

Published on: November 9, 2020

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Monomeric Targeted Protein Degraders.

Emily J Hanan, Jun Liang, Xiaojing Wang

    Journal of Medicinal Chemistry
    |May 1, 2020
    PubMed
    Summary

    Targeted protein degraders offer advantages over inhibition. This perspective highlights smaller, monomeric molecules for targeted protein degradation, contrasting them with larger, engineered degraders.

    Area of Science:

    • Medicinal Chemistry
    • Chemical Biology
    • Drug Discovery

    Background:

    • Targeted protein degraders are an emerging therapeutic strategy.
    • Protein degradation offers advantages over inhibition, including prolonged action and enhanced pharmacology.
    • Recent focus has been on engineered heterodimeric molecules.

    Purpose of the Study:

    • To highlight targeted protein degradation by smaller, monomeric molecules.
    • To compare monomeric and heterodimeric targeted protein degraders.
    • To discuss methods for evaluating protein degradation.

    Main Methods:

    • Literature review of monomeric targeted protein degraders.
    • Analysis of methods for assessing protein degradation.
    • Comparison of physical properties between monomeric and heterodimeric degraders.

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    Main Results:

    • Examples of successful targeted protein degradation using monomeric molecules are presented.
    • Monomeric degraders possess distinct physical properties compared to heterodimeric ones.
    • Established methods for evaluating protein degradation are discussed.

    Conclusions:

    • Monomeric molecules represent a viable strategy for targeted protein degradation.
    • Understanding the properties of monomeric degraders is crucial for drug development.
    • Further research into monomeric targeted protein degraders is warranted.