Unusually High Affinity of the PLK Inhibitors RO3280 and GSK461364 to HSA and Its Possible Pharmacokinetic Implications

The binding processes of two Polo-like kinase inhibitors, RO3280 and GSK461364, to the human serum albumin (HSA) protein as well as the protonation equilibria of both compounds have been studied combining absorbance and fluorescence spectroscopy experiments together with density functional theory ca...

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Detalles Bibliográficos
Autores: Fernández Sainz, Jesús, Pacheco Liñán, Pedro José, Ripoll Llorente, María Consuelo, González Fuentes, Joaquín, Albaladejo Pérez, José, Bravo Pérez, Iván, Garzón-Ruiz, Andrés
Tipo de recurso: artículo
Fecha de publicación:2023
País:España
Institución:Universidad de Castilla-La Mancha
Repositorio:RUIdeRA. Repositorio Institucional de la UCLM
OAI Identifier:oai:ruidera.uclm.es:10578/36857
Acceso en línea:https://hdl.handle.net/10578/36857
Access Level:acceso abierto
Palabra clave:Drug−protein binding
Human serum albumin
Fluorescence spectroscopy
Descripción
Sumario:The binding processes of two Polo-like kinase inhibitors, RO3280 and GSK461364, to the human serum albumin (HSA) protein as well as the protonation equilibria of both compounds have been studied combining absorbance and fluorescence spectroscopy experiments together with density functional theory calculations.