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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 guidel ....

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