PROTACs, PHOTACs and LYTACs: How to Target a Protein for Degradation

Targeting a single protein and making it disappear from the cell is quite the magic trick, and there are various molecular tools available for this task. You can use RNA interference, which prevents a protein from being made, inhibitors that bind the protein, rendering it unavailable for use or even gene editing tools like CRISPR […]

Bringing Cutting Edge Technologies to Academic Researchers Through the Academic Access Program

This post was written by guest blogger Iain Ronald, Director Academic/Government Market Segment at Promega.My back story is similar to most of you reading this blog, high school education, undergraduate degree then onto a postgraduate degree. However, over 25 years ago during my undergraduate study, I was fortunate enough to work in the lab of […]

Directed Targeted Protein Degradation with Pre-Built HiBiT Cell Lines

Recently, selectively targeting proteins for degradation using the cell’s natural ubiquitin proteasome pathway (UPS) has surfaced as an effective strategy to bypass difficult-to-drug proteins related to diseases like cancer. Using sensitive bioluminescence technology, CRISPR-edited cell lines can facilitate studying popular protein degradation targets. NanoLuc® Luciferase (NLuc) has made biology more accessible than ever (1). Further […]

Paving New Ways for Drug Discovery & Development: Targeted Protein Degradation

The Dana-Farber Targeted Protein Degradation Webinar Series discusses new discoveries and modalities in protein degradation. In this webinar, Senior Research Scientist, Dr. Danette Daniels, focuses primarily on proteolysis-targeting chimeras, or PROTACs. A variety of topics are covered including the design, potency, and efficacy of PROTACs in targeted protein degradation. Watch the video below to learn […]

Designing BET(ter) Inhibitors to Guide Therapy for Cancer and Inflammatory Diseases

Transcriptional activation of genes within the nucleus of eukaryotic cells occurs by a variety of mechanisms. Typically, these mechanisms rely on the interaction of regulatory proteins (transcriptional activators or repressors) with specific DNA sequences that control gene expression. Upon DNA binding, regulatory proteins also interact with other proteins that are part of the RNA polymerase […]

Targeted Protein Degradation: A Bright Future for Drug Discovery

Our cells have evolved multiple mechanisms for “taking out the trash”—breaking down and disposing of cellular components that are defective, damaged or no longer required. Within a cell, these processes are balanced by the synthesis of new components, so that DNA, RNA and proteins are constantly undergoing turnover. Proteins are degraded by two major components […]

A Roadmap for PROTAC Development

PROTACs or Proteolysis-Targeting Chimeras are an emerging tool in protein degradation studies, potentially suited to any need involving the removal of a specific protein. These small-molecule chimeras are exciting due to: 1) their target specificity; and 2) their ability to enable target destruction versus target inhibition. Here we discuss a paper that presents a roadmap […]