Targeted protein degradation (TPD) strategies have revolutionized how scientists tackle
challenging protein targets deemed undruggable with traditional small molecule inhibitors …

Protein–protein interactions (PPIs) govern all biological processes. Some small molecules
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …

The phosphoinositide 3-kinase (PI3K)/protein kinase B (AKT)/mammalian target of
rapamycin (mTOR) pathway is one of the most important intracellular pathways involved in …

Anticancer-targeted therapies inhibit various kinases implicated in cancer and have been
used in clinical settings for decades. However, many cancer-related targets are proteins …

Abstract Cyclin-dependent kinase 12 (CDK12) plays a crucial role in DNA-damage
response gene transcription and has recently been validated as a promising target in cancer …

Herein, we describe a systematic SAR‐and SPR‐investigation of the peptidomimetic
hydroxy‐proline based VHL‐ligand VH032, from which most to‐date published VHL …

Despite significant efficacy, one of the major limitations of small-molecule Bruton's tyrosine
kinase (BTK) agents is the presence of clinically acquired resistance, which remains a major …

Inducing protein degradation by proteolysis targeting chimeras has gained tremendous
momentum as a promising novel therapeutic strategy. Here, we report the design, synthesis …

Drug resistance is one of the biggest challenges in cancer treatment and limits the potential
to cure patients. In many tumors, sustained activation of the protein NRF2 makes tumor cells …

Targeted protein degradation (TPD) has emerged as a promising approach for drug
development, particularly for undruggable targets. TPD technology has also been …