Oak Brook, IL - The April edition of SLAS Discovery is a special issue on advances in protein degradation curated by guest editors M. Paola Castaldi, Ph.D., and Stewart L. Fisher, Ph.D.
Targeted protein degradation has generated interest within the drug discovery arena due to the inhibition of one particular function of a protein not often delivering the successful results that comes from whole-protein depletion. The pharmacology of PROTACs present challenges, however, namely for the development of orally bioavailable drugs. In the article "Target Validation Using PROTACs: Applying the Four Pillars Framework" authors Rados?aw P. Nowak, Ph.D., and Lyn H. Jones, Ph.D., describe the application of a translational pharmacology framework (the four pillars) to expedite PROTAC development by informing pharmacokinetic-pharmacodynamic (PKPD) understanding and helping clarify structure-activity relationships. Nowak and Jones hope that the four pillars will serve as a useful guideline to those developing targeted protein degraders and help establish PROTAC molecules as target validation chemical probes.
The April issue of SLAS Discovery includes three articles of original research.
These include:
- Exploring the Biology of Degraders -- Simultaneous Detection of Protein Target Engagement and Functional Readout for In-Depth Characterization of Targeted Protein Degraders
- A Method for Determining the Kinetics of Small Molecule Induced Ubiquitination
- CDK Family PROTAC Degradation Profiling Reveals Differential Family Member Responses and Cell-Cycle Dependent Degradation of CDK
Other articles include:
- Target Validation Using PROTACs: Applying the Four Pillars Framework
- E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones
- Delivering Best Practice PROTACs Projects -- Lessons from AZ Experience.
- High-Throughput Assay Technologies for Accelerating the Discovery and Optimization of Targeted Protein Degradation Therapeutics
- The Vital Role of Proteomics in Characterizing Novel Protein Degraders
- Non PROTAC Small Molecule Degraders -- An Exciting Novel Modality?
- Development of a Novel SNAP-Epitope Tag/Near Infrared Imaging Assay to Quantify G Protein-Coupled Receptor Degradation in Human Cells
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Access to April's SLAS Discovery issue is available at https:/
For more information about SLAS and its journals, visit http://www.
SLAS (Society for Laboratory Automation and Screening) is an international professional society of academic, industry and government life sciences researchers and the developers and providers of laboratory automation technology. The SLAS mission is to bring together researchers in academia, industry and government to advance life sciences discovery and technology via education, knowledge exchange and global community building.
SLAS Discovery: Advancing the Science of Drug Discovery, 2019 Impact Factor 2.195. Editor-in-Chief Robert M. Campbell, Ph.D., Twentyeight-Seven Therapeutics, Boston, MA (USA).
SLAS Technology: Translating Life Sciences Innovation, 2019 Impact Factor 2.174. Editor-in-Chief Edward Kai-Hua Chow, Ph.D., National University of Singapore (Singapore).
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