2. Academic Validation
  3. New luciferin-based probe substrates for human CYP26A1

New luciferin-based probe substrates for human CYP26A1

  • Biochem Biophys Rep. 2020 Nov 23:24:100861. doi: 10.1016/j.bbrep.2020.100861.
Shishir Sharma 1,  Jingyao Liu 1,  Xue Zhang 1,  Sangeeta Shrestha Sharma 1,  Erik J Sorensen 1 2,  Matthias Bureik 1
Affiliations

Affiliations

  • 1 School of Pharmaceutical Science and Technology, Health Sciences Platform, Tianjin University, Tianjin, 300072, China.
  • 2 Department of Chemistry, Princeton University, Princeton, NJ, 08544, USA.
PMID: 33294638 DOI: 10.1016/j.bbrep.2020.100861
Abstract

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.

Keywords

CYP enzymes; Esters; Fission yeast; Luminescent probe; Retinoic acid.

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