Prime, Michael E. published the artcileDiscovery and Structure-Activity Relationship of Potent and Selective Covalent Inhibitors of Transglutaminase 2 for Huntington’s Disease, Recommanded Product: Benzyl (piperidin-4-ylmethyl)carbamate, the main research area is transglutaminase inhibitor preparation; Huntington disease human structure activity.
Tissue transglutaminase 2 (TG2) is a multifunctional protein primarily known for its calcium-dependent enzymic protein crosslinking activity via iso-peptide bond formation between glutamine and lysine residues. TG2 overexpression and activity have been found to be associated with Huntington’s disease (HD); specifically, TG2 is up-regulated in the brains of HD patients and in animal models of the disease. Interestingly, genetic deletion of TG2 in two different HD mouse models, R6/1 and R6/2, results in improved phenotypes including a reduction in neuronal death and prolonged survival. Starting with phenyl-acrylamide screening hit I, the SAR of this series leading to potent and selective TG2 inhibitors is described. The suitability of the compounds as in vitro tools to elucidate the biol. of TG2 was demonstrated through mode of inhibition studies, characterization of drug like properties, and inhibition profiles in a cell lysate assay.
Journal of Medicinal Chemistry published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 132431-09-5 belongs to class piperidines, name is Benzyl (piperidin-4-ylmethyl)carbamate, and the molecular formula is C14H20N2O2, Recommanded Product: Benzyl (piperidin-4-ylmethyl)carbamate.
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem