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A novel BRET-based assay to investigate binding and residence time of unmodified ligands to the human lysosomal ion channel TRPML1 in intact cells.
Cunha, Micael R; Catta-Preta, Carolina M C; Takarada, Jéssica E; Moreira, Gabriela A; Massirer, Katlin B; Couñago, Rafael M.
Afiliación
  • Cunha MR; Center of Medicinal Chemistry (CQMED), Center for Molecular Biology and Genetic Engineering (CBMEG), University of Campinas, Campinas, Brazil. Electronic address: micaelrc@unicamp.br.
  • Catta-Preta CMC; Center of Medicinal Chemistry (CQMED), Center for Molecular Biology and Genetic Engineering (CBMEG), University of Campinas, Campinas, Brazil.
  • Takarada JE; Center of Medicinal Chemistry (CQMED), Center for Molecular Biology and Genetic Engineering (CBMEG), University of Campinas, Campinas, Brazil.
  • Moreira GA; Center of Medicinal Chemistry (CQMED), Center for Molecular Biology and Genetic Engineering (CBMEG), University of Campinas, Campinas, Brazil.
  • Massirer KB; Center of Medicinal Chemistry (CQMED), Center for Molecular Biology and Genetic Engineering (CBMEG), University of Campinas, Campinas, Brazil. Electronic address: kmassire@unicamp.br.
  • Couñago RM; Center of Medicinal Chemistry (CQMED), Center for Molecular Biology and Genetic Engineering (CBMEG), University of Campinas, Campinas, Brazil; Structural Genomics Consortium and Division of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina, Chape
J Biol Chem ; 299(6): 104807, 2023 06.
Article en En | MEDLINE | ID: mdl-37172730
Here, we report a bioluminescence resonance energy transfer (BRET) assay as a novel way to investigate the binding of unlabeled ligands to the human transient receptor potential mucolipin 1 (hTRPML1), a lysosomal ion channel involved in several genetic diseases and cancer progression. This novel BRET assay can be used to determine equilibrium and kinetic binding parameters of unlabeled compounds to hTRPML1 using intact human-derived cells, thus complementing the information obtained using functional assays based on ion channel activation. We expect this new BRET assay to expedite the identification and optimization of cell-permeable ligands that interact with hTRPML1 within the physiologically relevant environment of lysosomes.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Canales de Potencial de Receptor Transitorio / Transferencia de Energía por Resonancia de Bioluminiscencia Límite: Humans Idioma: En Revista: J Biol Chem Año: 2023 Tipo del documento: Article Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Canales de Potencial de Receptor Transitorio / Transferencia de Energía por Resonancia de Bioluminiscencia Límite: Humans Idioma: En Revista: J Biol Chem Año: 2023 Tipo del documento: Article Pais de publicación: Estados Unidos