Fluorogenic ester substrates to assess proteolytic activity.
The synthesis of a new type of fluorogenic ester substrates is described. Prepared from fluorescein in three steps with common commercially available precursors, they all generate bright green fluorescence upon proteolysis. Their particular structure allows the same substrate be used to report enzymatic activity of various proteases from serine and cysteine superfamilies. The substrate cleavage is sensitive to specific protease inhibitors providing a tool for inhibitor screening.
Mugherli
Laurent
L
Laboratoire Biopuces, Département Réponse et Dynamique Cellulaires, Commissariat à l'Energie Atomique, Grenoble, France.
Burchak
Olga N
ON
Chatelain
François
F
Balakirev
Maxim Y
MY
D004952:Esters / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D019793:Fluorescein / Q000737:chemistry*; D007700:Kinetics; D015394:Molecular Structure; D010447:Peptide Hydrolases / Q000378:metabolism*; D013379:Substrate Specificity
D004952:Esters; D010447:Peptide Hydrolases; D019793:Fluorescein