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Solution-Phase Synthesis of the Fluorogenic TGase 2 Acyl Donor Z-Glu(HMC)-Gly-OH and its Use for Inhibitor and Amine Substrate Characterisation
- Source :
- Analytical Biochemistry 595(2020), 113612
- Publication Year :
- 2020
-
Abstract
- A reliable solution-phase synthesis of the water-soluble dipeptidic fluorogenic transglutaminase substrate Z-Glu(HMC)-Gly-OH is presented. The route started from Z-Glu-OH, which was converted into the corresponding cyclic anhydride. This building block was transformed into the regioisomeric - and -dipeptides. Key step was the esterification of Z-Glu-Gly-OtBu with 4-methylumbelliferone. The final substrate compound was obtained in an acceptable yield and excellent purity without the need of purification by RP-HPLC. The advantage of this acyl donor substrate for the kinetic characterisation of inhibitors and amine-type acyl acceptor substrates is demonstrated by evaluating commercially available or literature-known irreversible inhibitors and the biogenic amines serotonin, histamine and dopamine, respectively.
Details
- Database :
- OAIster
- Journal :
- Analytical Biochemistry 595(2020), 113612
- Notes :
- application/pdf, English
- Publication Type :
- Electronic Resource
- Accession number :
- edsoai.on1415625348
- Document Type :
- Electronic Resource