Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …

Over the past 3 years, the first bivalent protein degraders intentionally designed for targeted
protein degradation (TPD) have advanced to clinical trials, with an initial focus on …

Here, we discuss the principles of allosteric activating mutations, propagation downstream of
the signals that they prompt, and allosteric drugs, with examples from the Ras signaling …

Targeted protein degradation has emerged from the chemical biology toolbox as one of the
most exciting areas for novel therapeutic development across the pharmaceutical industry …

Challenging disease targets necessitate new approaches for therapeutic intervention.
Rewiring protein-biomolecule interactions with proximity-inducing agents extends …

The field of targeted protein degradation is growing exponentially. Yet, there is an unmet
need for pharmacokinetic/pharmacodynamic models that provide mechanistic insights, while …

Abstract The Ser/Thr protein kinase Wee1 plays a regulatory role at the G 2/M checkpoint by
phosphorylating CDK1 when DNA is damaged to allow time for DNA to repair, disruption of …

Chemically induced proximity between certain endogenous enzymes and a protein of
interest (POI) inside cells may cause post-translational modifications to the POI with …

Proteolysis targeting chimera (PROTAC) is a novel drug modality that facilitates the
degradation of a target protein by inducing proximity with an E3 ligase. In this work, we …

Targeted protein degradation (TPD) has emerged as a powerful approach in drug discovery
for removing (rather than inhibiting) proteins implicated in diseases. A key step in this …