Selective cellular probes for mammalian thioredoxin reductase TrxR1: rational design of RX1, a modular 1,2-thiaselenane redox probe.
cellular probe
chemical design
dichalcogenide
disulfide
fluorogenic probe
high-throughput screening
redox biology
selenenyl sulfide
thioredoxin
thioredoxin reductase
Journal
Chem
ISSN: 2451-9294
Titre abrégé: Chem
Pays: United States
ID NLM: 101688902
Informations de publication
Date de publication:
12 May 2022
12 May 2022
Historique:
entrez:
8
8
2022
pubmed:
9
8
2022
medline:
9
8
2022
Statut:
ppublish
Résumé
Quantifying the activity of key cellular redox players is crucial for understanding physiological homeostasis, and for targeting their perturbed states in pathologies including cancer and inflammatory diseases. However, cellularly-selective probes for oxidoreductase turnover are sorely lacking. We rationally developed the first probes that selectively target the mammalian selenoprotein thioredoxin reductase (TrxR), using a cyclic selenenylsulfide oriented to harness TrxR's unique selenolthiol chemistry while resisting the cellular monothiol background. Lead probe
Identifiants
pubmed: 35936029
doi: 10.1016/j.chempr.2022.03.010
pmc: PMC9351623
mid: NIHMS1800334
doi:
Types de publication
Journal Article
Langues
eng
Pagination
1493-1517Subventions
Organisme : Intramural NIH HHS
ID : ZIA TR000418
Pays : United States
Déclaration de conflit d'intérêts
DECLARATION OF INTERESTS L.Z., J.G.F., and O.T.-S. are inventors on patent application EP21167187.0 covering compound structures reported in this paper. The authors declare no competing financial interests.
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