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Application of FRET- and BRET-based live-cell biosensors in deorphanization and ligand discovery studies on orphan G protein-coupled receptors.
Sajkowska, Joanna J; Tsang, Choi Har; Kozielewicz, Pawel.
Afiliación
  • Sajkowska JJ; Department of Medical Biochemistry and Biophysics, Karolinska Institute, Stockholm, Sweden; Department of Organic and Physical Chemistry, Faculty of Pharmacy, Medical University of Warsaw, Warsaw, Poland; Department of Medical Biochemistry and Microbiology, Uppsala University, Uppsala, Sweden.
  • Tsang CH; Department of Physiology and Pharmacology, Molecular Pharmacology of GPCRs, Karolinska Institute, Stockholm, Sweden.
  • Kozielewicz P; Department of Physiology and Pharmacology, Molecular Pharmacology of GPCRs, Karolinska Institute, Stockholm, Sweden. Electronic address: pawel.kozielewicz@ki.se.
SLAS Discov ; 29(6): 100174, 2024 Sep.
Article en En | MEDLINE | ID: mdl-39084335
ABSTRACT
Bioluminescence- and fluorescence-based resonance energy transfer assays have gained considerable attention in pharmacological research as high-throughput scalable tools applicable to drug discovery. To this end, G protein-coupled receptors represent the biggest target class for marketed drugs, and among them, orphan G protein-coupled receptors have the biggest untapped therapeutic potential. In this review, the cases where biophysical methods, BRET and FRET, were employed for deorphanization and ligand discovery studies on orphan G protein-coupled receptors are listed and discussed.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Técnicas Biosensibles / Transferencia Resonante de Energía de Fluorescencia / Receptores Acoplados a Proteínas G / Descubrimiento de Drogas Límite: Humans Idioma: En Revista: SLAS Discov Año: 2024 Tipo del documento: Article País de afiliación: Suecia Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Técnicas Biosensibles / Transferencia Resonante de Energía de Fluorescencia / Receptores Acoplados a Proteínas G / Descubrimiento de Drogas Límite: Humans Idioma: En Revista: SLAS Discov Año: 2024 Tipo del documento: Article País de afiliación: Suecia Pais de publicación: Estados Unidos