Laboratory study demonstrates how chemical warhead design affects stability and reactivity in human tissue transglutaminase inhibitors, highlighting key pathways for therapeutic drug development.
stability, which we model by measuring intrinsic reactivity with glutathione, as well as stability in hepatocytes and in whole blood, giving insight into degradation pathways and relative therapeutic potential of different functional groups. This work provides fundamental structural and reactivity information highlighting the importance of strategic warhead design for the development of potent hTG2 inhibitors.
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Mader et al. (2022) studied this question.
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