Endocrine therapy has long been a vital treatment option for estrogen receptor-alpha (ERα)-positive breast cancer. However, the frequent clinical problem of endocrine therapy resistance has left many patients in a difficult situation. This is particularly true whenRead More…
For decades, the primary strategy in drug development has been one of inhibition. We design molecules to block the function of harmful proteins, fitting into their active sites like a key inRead More…
Proteolysis-targeting chimeras function by recruiting ubiquitin ligases to targeted intracellular proteins, which promotes the degradation of pathogenic proteins via the proteasome system. This has made many previously “undruggable” proteins into viable therapeuticRead More…
In the ever-evolving landscape of medical research, protein degraders have emerged as a revolutionary class of therapeutic agents. Targeted protein degradation has rapidly expanded as a promising approach in drug discovery, openingRead More…
When we think about next-gen therapies that eliminate disease-causing proteins, most attention goes to the “targeting” components—the parts that bind to harmful proteins or cellular cleanup crews. But there’s a quiet powerhouseRead More…
Drug discovery is experiencing an unobtrusive revolution. Researchers have advanced past just blocking dangerous proteins and now pursue methods to actively break them down which could enable treatments for previously untreatable diseases. The foundationRead More…
Introduction Targeted Protein Degradation (TPD) has become a revolutionary way to work for the treatment of many diseases, yet they have been very successful in the treatment of diseases that have beenRead More…
Introduction Proteolysis-targeting chimeras are a new class of small molecules that provide alternative ways to discover drugs by leading target proteins to be selectively destroyed. In contrast to conventional inhibitors that only suppressRead More…
Chen, Po-Han, et al. “Modulation of phosphoprotein activity by phosphorylation targeting chimeras (PhosTACs).” ACS chemical biology 16.12 (2021): 2808-2815. In the rapidly evolving field of drug development, targeting protein post-translational modifications (PTMs) has emergedRead More…
Protein targeted degradation chimera is an emerging protein degradation strategy that has been booming in recent years. It was first proposed by Craig Crews et al. in 2001. Its basic principle isRead More…