Metabolism of PROTACs An understanding of the metabolism of PROTACs is a growing need since their metabolism can't be readily predicted from the individual ligands that constitute the chimera. A...
Metabolic pathways and disposition of Tropifexor in humans Looking at the structure of tropifexor, a farnesoid X receptor (FXR) agonist for the treatment of nonalcoholic steatohepatitis (NASH), immediately raises thoughts...
Metabolism and disposition of ozanimod in humans Check out the implications of the complex metabolism of ozanimod discussed in a paper from Sekhar Surapaneni and other scientists at BMS. There...
Successful and Unsuccessful Prediction of Human Hepatic Clearance for Lead Optimization Here's a great paper published by Jasleen Sodhi and Leslie Benet discussing the difficulties surrounding the prediction of in vivo clearance,...
Structure-Based Design of Potent and Orally Active Isoindolinone Inhibitors of MDM2-p53 Protein–Protein InteractionMulti-faceted paper from the team at Astex Pharmaceuticals (UK) and Cancer Research UK Newcastle Drug Discovery Unit describing the rational...
Issues resulting from late-occurring and persistent human metabolites Issues in metabolite identification in dossiers submitted to the regulatory authorities are still encountered, including deficiencies in characterisation of metabolites at the...
