Publications by authors named "Matthew S Addie"
A novel series of DGAT-1 inhibitors was discovered from an oxadiazole amide high throughput screening (HTS) hit. Optimisation of potency and ligand lipophilicity efficiency (LLE) resulted in a carboxylic acid containing clinical candidate 53 (AZD3988), which demonstrated excellent DGAT-1 potency (0.6 nM), good pharmacokinetics and pre-clinical in vivo efficacy that could be rationalised through a PK/PD relationship.
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- - Two new series of thienopyrrole inhibitors have been developed to target human liver glycogen phosphorylase a (GPa) to help lower glucose production from rat liver cells.
- - These inhibitors work by interacting with a specific site (the dimer interface) in the enzyme's structure, as revealed by X-ray crystallography studies.
- - The research highlights the potential of these compounds in managing glucose levels in the body, which could have implications for diabetes treatment.