The war on hTG2: warhead optimization in small molecule human tissue transglutaminase inhibitors
Lavleen Mader, Sarah K. I. Watt, Harish Iyer, Linh Nguyen, Harpreet Kaur, Jeffrey W. Keillor
Abstract
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.
Topics & Concepts
WarheadTissue transglutaminaseSmall moleculeChemistryCell biologyIn vitroHep G2BiophysicsBiochemistryEnzymeBiologyEngineeringAerospace engineeringBlood properties and coagulationTransgenic Plants and Applications