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© Yang SI, Institut Pasteur
Publication : ACS chemical biology

Bisubstrate-Type Chemical Probes Identify GRP94 as a Potential Target of Cytosine-Containing Adenosine Analogs.

Team: Epigenetic Chemical Biology
Team: UMR3523 – Chemistry for Life Sciences (Chem4Life)
Member: Paola Arimondo
Member: Ludovic Halby
Scientific Fields
Diseases
Organisms
Applications
Technique

Published in ACS chemical biology - 19 Mar 2020

Pechalrieu D, Assemat F, Halby L, Marcellin M, Yan P, Chaoui K, Sharma S, Chiosis G, Burlet-Schiltz O, Arimondo PB, Lopez M,

Link to Pubmed [PMID] – 32191434

Link to DOI – 10.1021/acschembio.9b00965

ACS Chem Biol 2020 04; 15(4): 952-961

We synthesized affinity-based chemical probes of cytosine-adenosine bisubstrate analogs and identified several potential targets by proteomic analysis. The validation of the proteomic analysis identified the chemical probe as a specific inhibitor of glucose-regulated protein 94 (GRP94), a potential drug target for several types of cancers. Therefore, as a result of the use of bisubstrate-type chemical probes and a chemical-biology methodology, this work opens the way to the development of a new family of GRP94 inhibitors that could potentially be of therapeutic interest.