A principal challenge in the discovery of proteolysis targeting chimeras (PROTACs) as oral
medications is their bioavailability. To facilitate drug design, it is therefore essential to …

Proteolysis-targeting chimeras (PROTACs) describe compounds that bind to and induce
degradation of a target by simultaneously binding to a ubiquitin ligase. More generally …

New chemical modalities in drug discovery include molecules belonging to the bRo5
chemical space. Because of their complex and flexible structure, bRo5 compounds often …

Molecular chameleonicity may enable compounds to compensate for the unfavorable ADME
properties typically associated with complex molecules, such as PROTACs. Here we present …

Directly targeted KRAS inhibitors are now facing resistance problems, which might be
partially solved by the combination of SOS1 inhibitors with KRAS inhibitors. However, this …

Developing orally bioavailable drugs demands an understanding of absorption in early drug
development. Traditional methods and physicochemical properties optimize absorption for …

Nonalcoholic fatty liver disease (NAFLD) is featured with excessive hepatic lipid
accumulation and its global prevalence is soaring. Nonalcoholic steatohepatitis (NASH), the …

Abstract Proteolysis-targeting chimeras (PROTACs), as heterobifunctional molecules, have
garnered significant attention for their ability to target previously undruggable proteins. Due …

The ability to predict the rate of permeation of new compounds across biological membranes
is of high importance for their success as drugs, as it determines their efficacy …