Anders Karlén

TL;DR: The effective permeability (Peff) in the human jejunum (in vivo) of 22 structurally diverse compounds was correlated with both experimentally determined lipophilicity values and calculated molecular descriptors, and models that correlate passive intestinal permeability to physicochemical descriptors were derived.

TL;DR: The innovative potential of the preclinical pipeline compared with the clinical pipeline is encouraging but fragile and much more work, focus and funding are needed for the novel approaches to result in effective antibacterial therapies to sustainably combat antibacterial resistance.

TL;DR: In this paper, the authors present a strategic blueprint to substantially improve our ability to discover and develop new antibiotics, and propose both short-term and long-term solutions to overcome the most urgent limitations in the various sectors of research and funding.

TL;DR: The interaction between HIV-1 protease and 58 structurally diverse transition-state analogue inhibitors has been analyzed by a surface plasmon resonance based biosensor and shows that different classes of inhibitors fall into distinct clusters in maps.

TL;DR: Two cyclic, C2-symmetric HIV-1 protease inhibitors, one sulfamide and one urea derivative, both comprising phenyl ether groups in the P1/P1' positions, were cocrystallized with HIV- 1 protease, and the crystal structures were determined to 2.0 A resolution.