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

Abstract : 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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https://hal-pasteur.archives-ouvertes.fr/pasteur-03026521
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Submitted on : Friday, January 1, 2021 - 4:44:55 PM
Last modification on : Wednesday, January 6, 2021 - 3:57:03 PM

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Dany Pechalrieu, Fanny Assemat, Ludovic Halby, Marlene Marcellin, Pengrong Yan, et al.. Bisubstrate-Type Chemical Probes Identify GRP94 as a Potential Target of Cytosine-Containing Adenosine Analogs. ACS Chemical Biology, American Chemical Society, 2020, 15 (4), pp.952-961. ⟨10.1021/acschembio.9b00965⟩. ⟨pasteur-03026521⟩

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