Transglutaminase inhibitors and methods of use thereof
Transglutaminase inhibitors and methods of use thereof are provided.
1. A pharmaceutical formulation comprising:
an effective dose of a tTGase inhibitor of the formula:
wherein R 1 is quinolin-3-ylmethyl ester and R 2 is a substituted or unsubstituted heterocyclyl or heterocyclylalkyl group;
R 3 is Br; n is 0; and X is NH.
2. The formulation according to claim 1 , wherein said tTGase inhibitor is a substantially enantiopure compound.
3. The formulation of claim 1 , wherein R 2 is selected from pyrrolidine, (5-hydroxy-1H-indol-3-yl)-ethyl, and (5-methoxy-1H-indol-3-yl)-ethyl.
4. The formulation of claim 1 , wherein the tTGase inhibitor is
5. The formulation of claim 1 , wherein the tTGase inhibitor has the structure
wherein R is selected from (S-),(R-)-5-hydroxy-indole and (S-),(R-)-5-methoxy-indole.