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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.

SUBMITTER: Pechalrieu D

PROVIDER: S-EPMC7336334 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature

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

Pechalrieu Dany D Assemat Fanny F Halby Ludovic L Marcellin Marlene M Yan Pengrong P Chaoui Karima K Sharma Sahil S Chiosis Gabriela G Burlet-Schiltz Odile O Arimondo Paola B PB Lopez Marie M

ACS chemical biology 20200406 4

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 ...[more]

PMID: 32191434

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