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Entree


A novel BRET-based assay to investigate binding and residence time of unmodified ligands to the human lysosomal ion channel TRPML1 in intact cells

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Autor(es):
Cunha, Micael R. ; Catta-Preta, Carolina M. C. ; Takarada, Jessica E. ; Moreira, Gabriela A. ; Massirer, Katlin B. ; Counago, Rafael M.
Número total de Autores: 6
Tipo de documento: Artigo Científico
Fonte: Journal of Biological Chemistry; v. 299, n. 6, p. 12-pg., 2023-06-01.
Resumo

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. (AU)

Processo FAPESP: 14/50897-0 - INCT 2014: Centro de Química Medicinal de Acesso Aberto
Beneficiário:Katlin Brauer Massirer
Modalidade de apoio: Auxílio à Pesquisa - Temático
Processo FAPESP: 21/04853-4 - Estudo do potencial terapêutico de novos moduladores do canal de cálcio lisossomal hTRPML1
Beneficiário:Micael Rodrigues Cunha
Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado