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

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journal contribution
posted on 2020-04-06, 15:04 authored by Dany Pechalrieu, Fanny Assemat, Ludovic Halby, Marlene Marcellin, Pengrong Yan, Karima Chaoui, Sahil Sharma, Gabriela Chiosis, Odile Burlet-Schiltz, Paola B. Arimondo, Marie Lopez
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.

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