The latest trends in drug discovery

Can gene editing be used as a lifesaving treatment? Could antiviral drugs that target human proteins be more effective than those than target the viruses themselves? The constant evolution of drug discovery is one of the most exciting aspects of modern medicine, and new research is leading to breakthroughs in precision medicine, cancer immunotherapy, neurodegenerative disease detection, and much more. Let's take a closer look at eight key trends happening in drug discovery today.

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Driving E3 ligase discovery through commercial PROTAC momentum

PROteolysis TArgeting Chimeras (PROTACS) are small molecules that drive protein degradation by bringing together the target protein with an E3 ligase. To date, more than 80 PROTAC drugs are in the development pipeline, and over 100 commercial organizations are involved in this field of research. We've seen in the CAS Content CollectionTM, the largest human-curated repository of scientific information, a sharp increase in PROTAC-related publications in less than 10 years, which demonstrates their therapeutic potential. Cancer is the leading disease in PROTAC-related literature, but neurodegenerative, infectious, and autoimmune diseases are represented as well.

Despite the diversity of E3 ubiquitin ligases, however, most designed PROTACs act via one of four E3 ligases: cereblon, VHL, MDM2 and IAP. Efforts are now underway to identify new ligases and utilize others already known beyond the main four. These include DCAF16, DCAF15, DCAF11, KEAP1, and FEM1B.

New insights into the structure and functionality of different ligases could enable targeting of various proteins that were previously inaccessible, and it may lead to fewer off-target effects. Expect to see new PROTAC drug designs entering the preclinical pipeline as researchers continue expanding the E3 ligase toolbox.

Expanding probiotic use beyond gut health for systemic diseases