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Related Concept Videos

Protein Networks02:26

Protein Networks

An organism can have thousands of different proteins, and these proteins must cooperate to ensure the health of an organism. Proteins bind to other proteins and form complexes to carry out their functions. Many proteins interact with multiple other proteins creating a complex network of protein interactions.
These interactions can be represented through maps depicting protein-protein interaction networks, represented as nodes and edges. Nodes are circles that are representative of a protein,...
Proteomics01:33

Proteomics

A proteome is the entire set of proteins that a cell type produces. We can study proteomes using the knowledge of genomes because genes code for mRNAs, and the mRNAs encode proteins. Although mRNA analysis is a step in the right direction, not all mRNAs are translated into proteins.
Proteomics is the study of proteomes' function. It involves the large-scale systematic study of the proteome to denote the protein complement expressed by a genome. Scientist Mark Wilkins coined the term proteomics...
Protein-protein Interfaces02:04

Protein-protein Interfaces

Many proteins form complexes to carry out their functions, making protein-protein interactions (PPIs) essential for an organism's survival. Most PPIs are stabilized by numerous weak noncovalent chemical forces. The physical shape of the interfaces determines the way two proteins interact. Many globular proteins have closely-matching shapes on their surfaces, which form a large number of weak bonds. Additionally, many PPIs occur between two helices or between a surface cleft and a polypeptide...

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Related Experiment Video

Updated: May 20, 2026

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
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Published on: December 1, 2020

Chemistry-based functional proteomics for drug target deconvolution.

Kui Wang1, Tao Yang, Qian Wu

  • 1The State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, 610041, PR China.

Expert Review of Proteomics
|July 20, 2012
PubMed
Summary

Drug target deconvolution identifies protein targets for small molecules, aiding drug discovery. Chemistry-based functional proteomics offers a powerful approach to deconvolute these targets, revealing new therapeutic possibilities and explaining drug side effects.

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Deep Proteome Profiling by Isobaric Labeling, Extensive Liquid Chromatography, Mass Spectrometry, and Software-assisted Quantification

Published on: November 15, 2017

Area of Science:

  • Biochemistry
  • Proteomics
  • Drug Discovery

Background:

  • Drug target deconvolution is crucial for understanding drug action and identifying new therapeutic targets.
  • Genomics and proteomics provide vast data but current deconvolution methods face challenges.
  • Chemistry-based functional proteomics offers a direct approach to identify small molecule targets.

Purpose of the Study:

  • To review chemistry-based functional proteomics strategies for drug target deconvolution.
  • To highlight the application of these methods in identifying and characterizing small molecule targets.
  • To discuss the role of these approaches in drug discovery and development.

Main Methods:

  • Activity-based protein profiling (ABPP) for target identification.
  • Compound-centric chemical proteomics for target characterization.
  • Integration of chemical proteomics with biological assays.

Main Results:

  • Identified numerous previously unknown enzymes as potential drug targets.
  • Rationalized side effects and toxicity of existing and novel drug candidates.
  • Enabled precise characterization of small molecule-protein interactions.

Conclusions:

  • Chemistry-based functional proteomics is a key strategy for effective drug target deconvolution.
  • These methods advance the identification of novel drug targets and the understanding of drug mechanisms.
  • This approach is vital for improving drug safety and efficacy in pharmaceutical research.