NMR applications to find and progress TREX1 binders

Autor: Leonhard Geist, Paola Martinelli, Shereena Mohideen-Ali, Patrick Werni, Gerhard Fischer, Julian E. Fuchs, Klaus Rumpel, Moriz Mayer
Jazyk: angličtina
Rok vydání: 2022
Předmět:
Zdroj: Journal of Magnetic Resonance Open, Vol 12, Iss , Pp 100075- (2022)
Druh dokumentu: article
ISSN: 2666-4410
DOI: 10.1016/j.jmro.2022.100075
Popis: Inhibition of the exonuclease activity of Three-prime Repair EXonuclease 1 (TREX1) has emerged as a potential novel immunotherapeutic strategy. Herein we describe our screening approach to find initial low-affinity fragment hits for TREX1 from our 19F library and the use of both ligand- and target-based NMR methods for hit confirmation and validation. In a further step to support the early hit expansion stage we describe our setup of a 19F competition assay for KI determination of analogs.
Databáze: Directory of Open Access Journals
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