New luciferin-based probe substrates for human CYP26A1

Autor: Shishir Sharma, Jingyao Liu, Xue Zhang, Sangeeta Shrestha Sharma, Erik J. Sorensen, Matthias Bureik
Jazyk: angličtina
Rok vydání: 2020
Předmět:
Zdroj: Biochemistry and Biophysics Reports, Vol 24, Iss , Pp 100861- (2020)
Druh dokumentu: article
ISSN: 2405-5808
DOI: 10.1016/j.bbrep.2020.100861
Popis: 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.
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