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 |
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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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