Recent Highlights in Targeted Protein Degradation
In Wednesday’s Flash Talk webinar, we covered recent highlights in targeted protein degradation, with lots of great questions from the audience. The webinar and recording are available below to everyone thanks to our sponsor, Revvity Signals, and the slides are available for download to Premium members at the bottom. The talk covered: Some of the…
Small Molecules Evolve
Small molecule drugs make up most of the drugs we take conveniently as pills, including painkillers like ibuprofen (Advil), antibiotics like penicillin and amoxicillin, or cholesterol-lowering drugs like atorvastatin (Lipitor). The biotechnology revolution allowed scientists to create drugs through genetic engineering and related biological processes, creating a new category of drugs known as “biologics.” These…
Macrocyclization via Ring-Closing Metathesis in Drug Discovery & Process Chemistry
Macrocyclic molecules, containing 12 or more atoms in a ring system, are increasingly prevalent in drug discovery, with over 67 macrocyclic drugs approved so far and several notable examples of clinical success highlighted on Drug Hunter recently, including MK-0616, repotrectinib, and pacritinib. By imparting conformational restraint and reducing entropy of binding, macrocyclization can enable more…
Not Your Grandparents’ Drugs: How Approved Drugs Have Evolved Since the 70’s
We recently explored how the lipophilicity (logP) of drugs has changed over time and found that, on average, drugs have become more lipophilic through the decades, primarily attributable to the industry’s move away from natural products. Despite this shift, it is clear from a broad qualitative comparison of structures from past decades to today that…
AI for All? How Pharma Partnerships Improve Software Solutions
Artificial Intelligence (AI) is revolutionizing data processing, with applications to drug discovery ranging from automating cellular imaging to modeling protein folding. Although numerous startups are developing methods to apply AI-driven drug discovery to develop proprietary assets, a remaining challenge is making these powerful tools usable by drug discovery companies without deep in-house AI/ML expertise. Many…
The Molecular Glue Degrader Landscape in 2022
Since the 2014 discoveries that thalidomide-like compounds “glue” together the cereblon (CRBN) unit of the ubiquitin E3 ligase complex and certain immune cell transcription factors, molecular glue degraders have been caught up in the targeted protein degradation zeitgeist that catapulted PROTACs, their bulkier bivalent counterparts, to the forefront of drug hunters’ attention. Interest in molecular…