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Bioorthogonal Tethering Enhances Drug Fragment Affinity for G Protein-Coupled Receptors in Live Cells

[Image: see text] G protein-coupled receptors (GPCRs) modulate diverse cellular signaling pathways and are important drug targets. Despite the availability of high-resolution structures, the discovery of allosteric modulators remains challenging due to the dynamic nature of GPCRs in native membranes...

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Detalles Bibliográficos
Autores principales: Mattheisen, Jordan M., Limberakis, Chris, Ruggeri, Roger B., Dowling, Matthew S., am Ende, Christopher W., Ceraudo, Emilie, Huber, Thomas, McClendon, Christopher L., Sakmar, Thomas P.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2023
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10214443/
https://www.ncbi.nlm.nih.gov/pubmed/37116188
http://dx.doi.org/10.1021/jacs.3c00972