Bisubstrate-type chemical probes identify GRP94 as a potential target of cytosine-containing adenosine analogs Journal Article
| Authors: | Pechalrieu, D.; Assemat, F.; Halby, L.; Marcellin, M.; Yan, P.; Chaoui, K.; Sharma, S.; Chiosis, G.; Burlet-Schiltz, O.; Arimondo, P. B.; Lopez, M. |
| Article Title: | 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. |
| Journal Title: | ACS Chemical Biology |
| Volume: | 15 |
| Issue: | 4 |
| ISSN: | 1554-8929 |
| Publisher: | American Chemical Society |
| Date Published: | 2020-04-07 |
| Start Page: | 952 |
| End Page: | 961 |
| Language: | English |
| DOI: | 10.1021/acschembio.9b00965 |
| PUBMED: | 32191434 |
| PROVIDER: | scopus |
| PMCID: | PMC7336334 |
| DOI/URL: | |
| Notes: | Article -- Source: Scopus |
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