AI Article Synopsis
- Thieno[2,3-d]pyrimidin-4-one acylhydrazide derivatives are identified as moderate inhibitors of tissue transglutaminase (TGase 2) using a fluorescence assay for measuring enzyme activity.
- The study highlights that the presence of an acylhydrazide thioether side-chain and a thiophene ring is essential for the inhibitory effect.
- This research contributes to the understanding of TGase 2 inhibition, which could have implications in therapeutic development.
Article Abstract
Thieno[2,3-d]pyrimidin-4-one acylhydrazide derivatives were discovered as moderately potent inhibitors of TGase 2 (tissue transglutaminase) utilizing a fluorescence-based assay that measured TGase 2 catalyzed incorporation of the dansylated Lys derivative alpha-N-Boc-Lys-CH(2)-CH(2)-dansyl into the protein substrate N,N-dimethylated-casein. A SAR study revealed that the acylhydrazide thioether side-chain and the thiophene ring were critical to inhibitory activity.
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| http://dx.doi.org/10.1016/j.bmcl.2005.02.005 | DOI Listing |
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