New research led by the University of Minnesota Medical School demonstrates that molecules acting as "molecular bumpers" and "molecular glues" can rewire G protein-coupled receptor (GPCR) signaling, turning the cell's busiest receptors into precision tools—opening the door to a new generation of safer, smarter medicines.

Regulator of G protein Signaling 2 (RGS2) negatively modulates signaling downstream of G protein-coupled receptors (GPCRs) by accelerating GTP hydrolysis at Gα subunits of heterotrimeric G proteins. D...

In most drug discovery efforts targeting regulator of G-protein signaling (RGS) proteins, inhibiting their activity is the end-goal. A recent article …

The following column by Senator Todd Young (R-Ind.) and Matthew Pottinger, Former Deputy National Security Advisor of the United States, was published in The Washington Post on March 24, 2025. By Sena...

The development of targeted protein degradation by recruiting a protein of interest to a ubiquitin ligase to facilitate its degradation has become a powerful therapeutic tool. The potential of this approach is limited to proteins that can be readily ubiquitinated and relies on having a ligand with the various E3 ligases. Here, we describe a new methodology for targeted protein degradation that directly recruits a protein of interest to the proteasome for degradation. We generated bifunctional molecules that incorporate a small molecule ligand into a subunit on the 26S proteasome that recruits the protein directly for degradation. ByeTAC degradation requires binding to Rpn-13, a nonessential ubiquitin receptor of the 26S proteasome, and the protein of interest and does not have to rely on the E ligase cascade for ubiquitination. The ByeTAC methodology demonstrates the application of directly recruiting a protein to the proteasome via interactions with Rpn-13 for degradation.

Regulators of G protein signaling (RGS) proteins negatively regulate signaling through G protein-coupled receptors, and reduced RGS protein function i…

Accomplished early-career pharmaceutical scientist recognized as next-generation leader

As researchers representing universities across the country, the last few weeks have been filled with uncertainty. As you are aware, the Trump administration’s National Institutes of Health (NIH) prop...

Regulators of G protein signaling (RGS) proteins finetune signaling via heterotrimeric G proteins to maintain physiologic homeostasis in various organ systems of the human body including the brain, ki...