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Synthesis of Effective Water‐Soluble Fluorescein Dibenzyl Ether Cytochrome P450 Substrates
Author(s) -
Stepler Cameron M,
Gallivan Maxwell A,
Wysocki Laura M
Publication year - 2016
Publication title -
the faseb journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.709
H-Index - 277
eISSN - 1530-6860
pISSN - 0892-6638
DOI - 10.1096/fasebj.30.1_supplement.1092.2
Subject(s) - fluorescein , chemistry , enzyme , cytochrome p450 , water soluble , solubility , fluorescence , ether , cytochrome , biochemistry , combinatorial chemistry , kinetics , organic chemistry , physics , quantum mechanics
Cytochrome P450 is a key family of enzymes in the breakdown of drugs and toxins in the body. We are interested in probing the activity of these enzymes with different organic ethers through a library of fluorescein diether derivatives. These compounds are hydrolytically stable and exhibit very low background fluorescence before unmasking with high contrast, making them ideal targets for sensitive assays. The first‐generation library revealed challenges related to solubility of the fluorogenic compounds in the desired assay. Through the design and synthesis of a variety of substrates, progress was made toward water‐soluble probes that display reasonable kinetics for evaluation and investigation of enzymatic activity. Support or Funding Information This work was supported by the Henry and Nellie Pence Trust.