Xin Teng

TL;DR: Necroptosis is a cellular mechanism of necrotic cell death induced by apoptotic stimuli in the form of death domain receptor engagement by their respective ligands under conditions where apoptotic execution is prevented and necrostatins are established as the first-in-class inhibitors of RIP1 kinase, the key upstream kinase involved in the activation of necroptosis.

TL;DR: 5-(1H-Indol-3-ylmethyl)-2-thiohydantoins and 5-(1h-indol- 3-yl methyl)Hydantoins were found to be potent necroptosis inhibitors (called necrostatins) and several positions of the indole were intolerant of substitution, while small substituents at the 7-position resulted in increased inhibitory activity.

TL;DR: It is shown that Akt kinase activity is critical for necroptosis in L929 cells and plays a key role in TNFα production and the role of AkT kinase in both cell death and inflammatory regulation.

TL;DR: A structure-activity relationship study revealed that small cyclic alkyl groups and 2,6-dihalobenzylamides at the 4- and 5-positions of the [1,2,3]thiadiazole, respectively, were optimal for necroptosis inhibitory activity.

TL;DR: A structure-activity relationship (SAR) study of the [1,2,3]thiadiazole benzylamide series revealed that increased mouse liver microsome stability and increased necroptosis inhibitory activity could be accomplished by replacement of the 4-cyclopropyl-[1, 2,3], 5-cyano-1-methylpyrrole derivatives.