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Chemical Proteomics Initiative (CPI)

Project leader: Ho Jeong KWON
Yonsei University, Korea
kwonhj@yonsei.ac.kr

1. Objectives

Chemical proteomics is an integrated research engine that bridges over a hurdle to identify target proteins of biologically active small molecules with unknown mode of action for functional studies of proteome and drug discovery. To this end, it covers natural/synthetic chemical library construction, phenotypic screen, small molecule hits, target identification and validation, mode of action, further drug discovery against the identified target, and data base (DB) construction. The objectives of Chemical Proteomics Initiative of AOHUPO (CPI-AOHUPO) focus on systematic analysis of target protein identification of bioactive small molecules using mass spectrometry based proteome analysis and the exchange of new data and innovative technologies for better understanding of proteome and drug discovery.

2. Project plan

CPI-AOHUPO will initially work for 5 years as the first phase with 3+2 years at multi-laboratories of AOHUPO as follows.

  1. The first 3 years will focus on chemical library construction, a standard cell, tissue, and phage-displayed human cDNA expressed proteome preparation, a standardized methodology development of target identification with label or label-free small molecules, and target validation and functional study of newly identified target proteins.
  2. The following 2 years will focus on innovative technology development for proteomics based target identification of small molecules, drug discovery against the identified target, and DB construction.

After the first phase, CPI-AOHUPO may continue to another 5 years with similar scopes of the first phase and expand its activities in collaboration with other AOHUPO initiatives.

3. Milestones

  1. Construction and sharing of authentic small molecule library including target known commercial library (ie., Sigma LOPAC library) and target unknown small molecules from multi-laboratories of AOHUPO.
  2. Proteomics based technology development of target identification of label or label-free small molecules.
  3. Target validation and functional study of newly identified target proteins.
  4. Drug discovery against the identified target and DB construction.

4. A coherent link with the Membrane Proteome Project

  1. Sharing small molecule library and membrane proteome fractions to discover new small molecules or membrane proteins.
  2. Functional studies of membrane proteome with small molecules, vice versa.
  3. Sharing data base and informatics tools.
  4. Joint international grant applications and organization of international meetings.

Welcome to join with CPI team! (contact: kwonhj@yonsei.ac.kr)




Chemical proteomics, an integrated research engine for exploring drug-targetphenotype interactions
 
Examining the influence of specificity ligands and ATP-competitive ligands on the overall effectiveness of bivalent kinase inhibitors
Daptomycin, a last-resort antibiotic, binds ribosomal protein S19 in humans
Tetrazine ligation for chemical proteomics
Photo-affinity labeling (PAL) in chemical proteomics: a handy tool to investigate protein-protein interactions (PPIs)
Thermal proteome profiling: unbiased assessment of protein state through heat-induced stability changes