Magda Kosmopoulou

TL;DR: A series of small compounds, bisthiazolidines, which act as inhibitors of all MBL types, restoring the efficacy of currently used antibiotics against resistant bacterial strains producing different MBLs are shown.

TL;DR: Inspired by known interactions of MBLs with β-lactams, four BTZs are designed that behave as in vitro NDM-1 inhibitors with Ki values in the low micromolar range and restore the antibacterial activity of imipenem.

TL;DR: It is proposed that targeting this pocket within the active site from polar to a hydrophobic pocket, similar to what is observed in the structure of Aurora-A bound to a compound that induces DFG-out, may be a productive route in the design of selective kinase inhibitors and described the structural basis for the rational design of these compounds.

TL;DR: The complex structures of GPb in complex with the three analogs revealed that the inhibitors can be accommodated in the catalytic site of T‐state GPb with very little change of the tertiary structure, and provide a rationalization for understanding variations in potency of the inhibitors.

TL;DR: Compound 51 is highly orally bioavailable, and in in vivo efficacy studies it inhibited the growth of SW620 colon carcinoma xenografts following oral administration with no observed toxicities as defined by body weight loss.