Back to results
US 2014/0234887 A1Published application
Fluorogenic peptidase substrate
AssigneeCentre National De La Recherche Scientfique
InventorsJens Hasserodt, Oliver Thorn-Seshold
Life of this patent
Estimating the term…
Abstract
The invention relates to novel peptidase substrates of formula (I): wherein R0, R1, R2, R3, R4, R5 and n are as defined in claim 1, and a method for detecting the presence of a catalytically active peptidase, by means of one of these substrates.
Claims14
Peptidase substrate of formula (I):
- wherein:
- R0 is a peptidyl or amino acid group bound to the NH group via its carboxy-terminal end,
- n is 0 or 1,
- R1 is a hydrogen atom or a side chain of an amino acid,
- R5 is a phenoxy derivative, the corresponding phenol derivative of which belongs to the ESIPT class of fluorophores,
- R2, R3 and R4 are defined as follows:
- R2 is a (C1-C4)alkyl group or a hydrogen atom, R3 is a (C1-C4)alkyl group, and R4 is a (C1-C4)alkyl group;
- or else
- R2 is a (C1-C4)alkyl group or a hydrogen atom and R3 and R4 are bound together and form with the carbon and nitrogen atoms to which they are bound an aliphatic heterocycle, this heterocycle may be substituted with a group, of the ammonium, carboxylate or sulfonate type allowing an increase in water-solubility of the substrate;
- or else
- R4 is a (C1-C4)alkyl group and R2 and R3 are bound together and form with the carbon atom to which they are bound an aliphatic carbocyl, as a mixture of optical isomers or diastereoisomers in any proportions, or as a form enriched with an optical isomer or with a diastereoisomer.
8 more elements
Dependencies are inferred from the claim text.