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

Dany Pechalrieu, Fanny Assemat, Ludovic Halby, Marlene Marcellin, Pengrong Yan, Karima Chaoui, Sahil Sharma, Gabriela Chiosis, Odile Burlet-Schiltz, Paola B Arimondo, Marie Lopez

ACS chemical biology 2020 Apr 17

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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.

Citation

Dany Pechalrieu, Fanny Assemat, Ludovic Halby, Marlene Marcellin, Pengrong Yan, Karima Chaoui, Sahil Sharma, Gabriela Chiosis, Odile Burlet-Schiltz, Paola B Arimondo, Marie Lopez. Bisubstrate-Type Chemical Probes Identify GRP94 as a Potential Target of Cytosine-Containing Adenosine Analogs. ACS chemical biology. 2020 Apr 17;15(4):952-961