Kinase sensors
AssigneeMassachusetts Institute of Technology
InventorsBarbara Imperiali, Elvedin Lukovic, Juan Antonio Gonzalez-Vera
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Abstract
The present invention generally relates to compositions and methods for determining kinase activity. In some cases, the compositions comprise a triazole heterocycle. In some embodiments, the compositions comprise a quinoline moiety. In one aspect, the present invention is directed to compositions that undergo chelation-enhanced fluorescence (CHEF). In some cases, the compositions may have fluorescence emission spectra with peak maxima greater than 490 nm. The compositions of the present invention can be used, in certain embodiments, to detect phosphorylated substrates and biological processes such as phosphorylation events.
Claims11
A composition, comprising:
- a compound having a structure as in formula (I):
- wherein R1 and R2 are each independently hydrogen or aryl, or wherein R1 and R2 together with the carbon atoms of the triazole ring to which they are connected form a ring;
- R3 is independently hydrogen, alkyl, aryl, halo, or hydroxyl, amino, thiol, sulfonic acid, sulfonamide, a protein kinase substrate, at least one amino acid, or a substituted derivative thereof, wherein R3 can substitute any open valence of any ring within structure (I);
- m is 1, 2, 3, 4, or 5;
- and
- R4 is hydroxyl, amino, thiol, or a substituted derivative thereof.
A method, comprising:
- determining phosphorylation of a protein kinase substrate using fluorescence of a composition of formula (I):
- wherein R1 and R2 are each independently hydrogen or aryl, or where R1 and R2 together with the carbon atoms which they substitute form a ring;
- R3 is independently hydrogen, alkyl, aryl, halo, or hydroxyl, amino, thiol, sulfonic acid, sulfonamide, a protein kinase substrate, at least one amino acid, or a substituted derivative thereof, wherein R3 can substitute an open valence of any ring within structure (I);
- m is 1, 2, 3, 4, or 5;
- and
- R4 is hydroxyl, amino, thiol, or a substituted derivative thereof.
Dependencies are inferred from the claim text.