Cross-coupling reactions have played a critical role enabling the rapid expansion of
structure–activity relationships (SAR) during the drug discovery phase to identify a clinical …

Proteolysis-targeting chimeras (PROTACs) have received tremendous attention as a new
and exciting class of therapeutic agents that promise to significantly impact drug discovery …

The biological and medicinal impacts of proteolysis-targeting chimeras (PROTACs) and
related chimeric molecules that effect intracellular degradation of target proteins via ubiquitin …

Current methods for the preparation of heterobifunctional pomalidomide-conjugates rely on
methods that are often low yielding and produce intractable byproducts. Herein we describe …

Protein N-terminal methylation catalyzed by N-terminal methyltransferase 1 (NTMT1) is an
emerging methylation present in eukaryotes, playing important regulatory roles in various …

Hypoxia-inducible factor-1α (HIF-1α) constitutes the principal mediator of cellular adaptation
to hypoxia in humans. The HIF-1α protein level and activity are tightly regulated by the …

MyD88 gene mutation has been identified as one of the most prevalent driver mutations in
the activated B-cell-like diffuse large B-cell lymphoma (ABC DLBCL). The published …

PROTACs represent a promising modality that has gained significant attention for the
treatment of cancer, Alzheimer's disease, and so forth. Due to limited structural information of …

Small molecule heterobifunctional degraders (commonly also known as PROTACs) offer
tremendous potential to deliver new therapeutics in areas of unmet medical need. To deliver …

Squalene synthase (SQS) is an essential enzyme in the mevalonate pathway, which
controls cholesterol biosynthesis and homeostasis. Although catalytic inhibitors of SQS have …