Bianca M. Liederer

TL;DR: In this review, the most important enzymes involved in the bioconversion of ester-based prodrugs will be discussed in terms of their biology and biochemistry.

TL;DR: GDC-0068 is a highly selective, orally bioavailable Akt kinase inhibitor that shows pharmacodynamic inhibition of Akt signaling and robust antitumor activity in human cancer cells in vitro and in vivo.

TL;DR: Biological studies with one 6,7-dihydro-5H-cyclopenta[d]pyrimidine compound, 28 (GDC-0068), demonstrate good oral exposure resulting in dose-dependent pharmacodynamic effects on downstream biomarkers and a robust antitumor response in xenograft models in which the phosphatidylinositol 3-kinase-Akt-mammalian target of rapamycin pathway is activated.

TL;DR: Using structure-based design, this work sought to increase potency at the GluN2A subtype, while improving selectivity against related α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors (AMPARs) using a combination of electrophysiology and protein crystallography.

TL;DR: Inhibition of RIP1 reduced collagen antibody-induced arthritis, and prevented skin inflammation caused by mutation of Sharpin, or colitis caused by deletion of Nemo from intestinal epithelial cells, but its relevance to tumor progression and metastases is questioned.