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 degradation refers to the use of small molecules to induce the selective
degradation of proteins. In its most common form, this degradation is achieved through …

Targeted protein degradation (TPD) has emerged as a potentially transformational
therapeutic modality with considerable promise. Molecular glue degraders remodel the …

Targeted protein degradation (TPD) involving chimeric molecules has emerged as one of
the most promising therapeutic modalities in recent years. Among various reported TPD …

Many cereblon (CRBN) ligands have been used to develop proteolysis targeting chimeras
(PROTACs), but all are reversible binders of the E3 ubiquitin ligase. We recently described …

The absence of effective active pockets makes traditional molecularly targeted drug
strategies ineffective against 80% of human disease-related proteins. The PROTAC …

Using dasatinib linked to E3 ligase ligands, we identified a potent and selective dual Csk/c-
Src PROTAC degrader. We then replaced dasatinib, the c-Src-directed ligand, with a …

Anaplastic lymphoma kinase (ALK) gene rearrangements have been identified as potent
oncogenic drivers in several malignancies, including non-small cell lung cancer (NSCLC) …

Proteolysis targeting chimera (PROTAC) technology represents a groundbreaking
development in drug discovery, leveraging the ubiquitin‒proteasome system to specifically …

Fusion oncoproteins are associated with childhood cancers and have proven challenging to
target, aside from those that include kinases. As part of its efforts for targeting childhood …