Proteolysis-targeting chimeras (PROTACs) have been an area of intensive research with the
potential to extend drug space not target to traditional molecules. In the last half decade, we …

Targeted protein degraders such as PROTACs and molecular glues are a rapidly emerging
therapeutic modality within industry and academia. Degraders possess unique mechanisms …

Abstract Machine learning (ML) systems can model quantitative structure-property
relationships (QSPR) using existing experimental data and make property predictions for …

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

The discovery of cell permeable and orally bioavailable von Hippel-Lindau (VHL)
proteolysis targeting chimeras (PROTACs) is challenging as their structures locates them at …

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 …

PROTACs are an emerging therapeutic approach towards targeted protein degradation.
This article examines the leading examples of this modality that are in clinical development …

Despite significant advances over recent years, the treatment of T cell acute lymphoblastic
leukemia (T-ALL) remains challenging. We have recently shown that a subset of T-ALL …

Abstract Background and Purpose Bifunctional small molecule degraders, which link the
target protein with E3 ubiquitin ligase, could lead to the efficient degradation of the target …

Enzyme-mediated pharmacokinetic drug-drug interactions can be caused by altered activity
of drug metabolizing enzymes in the presence of a perpetrator drug, mostly via inhibition or …