Back to Search Start Over

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

Authors :
Pechalrieu D
Assemat F
Halby L
Marcellin M
Yan P
Chaoui K
Sharma S
Chiosis G
Burlet-Schiltz O
Arimondo PB
Lopez M
Source :
ACS chemical biology [ACS Chem Biol] 2020 Apr 17; Vol. 15 (4), pp. 952-961. Date of Electronic Publication: 2020 Apr 06.
Publication Year :
2020

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.

Details

Language :
English
ISSN :
1554-8937
Volume :
15
Issue :
4
Database :
MEDLINE
Journal :
ACS chemical biology
Publication Type :
Academic Journal
Accession number :
32191434
Full Text :
https://doi.org/10.1021/acschembio.9b00965