Wodtke, Robert, Pietsch, Markus and Loeser, Reik (2020). Solution-phase synthesis of the fluorogenic TGase 2 acyl donor Z-Glu(HMC)-Gly-OH and its use for inhibitor and amine substrate characterisation. Anal. Biochem., 595. SAN DIEGO: ACADEMIC PRESS INC ELSEVIER SCIENCE. ISSN 1096-0309
Full text not available from this repository.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 alpha- and gamma-dipeptides. The 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.
| Item Type: | Journal Article | ||||||||||||||||
| Creators: |
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| URN: | urn:nbn:de:hbz:38-337093 | ||||||||||||||||
| DOI: | 10.1016/j.ab.2020.113612 | ||||||||||||||||
| Journal or Publication Title: | Anal. Biochem. | ||||||||||||||||
| Volume: | 595 | ||||||||||||||||
| Date: | 2020 | ||||||||||||||||
| Publisher: | ACADEMIC PRESS INC ELSEVIER SCIENCE | ||||||||||||||||
| Place of Publication: | SAN DIEGO | ||||||||||||||||
| ISSN: | 1096-0309 | ||||||||||||||||
| Language: | English | ||||||||||||||||
| Faculty: | Unspecified | ||||||||||||||||
| Divisions: | Unspecified | ||||||||||||||||
| Subjects: | no entry | ||||||||||||||||
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| URI: | http://kups.ub.uni-koeln.de/id/eprint/33709 |
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