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Bisubstrate-Type Chemical Probes Identify GRP94 as a Potential Target of Cytosine-Containing Adenosine Analogs.
- 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.
- Subjects :
- Adenosine radiation effects
Affinity Labels chemical synthesis
Affinity Labels radiation effects
Cell Line, Tumor
Click Chemistry
Cytosine radiation effects
Humans
Membrane Glycoproteins chemistry
Proteome chemistry
Proteomics
Ultraviolet Rays
Adenosine analogs & derivatives
Adenosine pharmacology
Affinity Labels pharmacology
Cytosine analogs & derivatives
Cytosine pharmacology
Membrane Glycoproteins antagonists & inhibitors
Subjects
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