New luciferin-based probe substrates for human CYP26A1

Activity of human CYP26A1 towards six proluciferin probe substrates and their ester derivatives was monitored. These included three monofluorobenzyl ether isomers and three five-membered heterocycles. Overall, luciferin substrates with a free acid group gave higher activities than the ester compound...

Descripción completa

Detalles Bibliográficos
Autores principales: Sharma, Shishir, Liu, Jingyao, Zhang, Xue, Sharma, Sangeeta Shrestha, Sorensen, Erik J., Bureik, Matthias
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier 2020
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7695906/
https://www.ncbi.nlm.nih.gov/pubmed/33294638
http://dx.doi.org/10.1016/j.bbrep.2020.100861
Descripción
Sumario:Activity of human CYP26A1 towards six proluciferin probe substrates and their ester derivatives was monitored. These included three monofluorobenzyl ether isomers and three five-membered heterocycles. Overall, luciferin substrates with a free acid group gave higher activities than the ester compounds. Also, luciferin derivatives with six-ring structures were better metabolized than those with five-rings. The best substrates identified in this study are Luciferin 6′ 3-fluorobenzyl ether (Luciferin-3FBE) and its methyl ester (Luciferin-3FBEME). Taken together, we describe eleven new probe substrates for CYP26A1 and demonstrate for the first time that CYP26A1 does not only accept acid substrates but can also metabolize esters.

Ejemplares similares