AI Article Synopsis
- PROTACs represent a novel strategy for targeting and degrading specific proteins in disease treatment, currently being studied in clinical settings.
- The article focuses on the physical and chemical characteristics of PROTACs, including the challenges medicinal chemists encounter in making these drugs effective when taken orally.
- The authors share their insights and recommendations, aiming to support others in the field of drug discovery exploring this innovative therapeutic approach.
Article Abstract
PROTACs are an emerging therapeutic approach towards targeted protein degradation. This article examines the leading examples of this modality that are in clinical development through the prism of their physicochemical properties. In particular, the optimisation of the various components of PROTACs together with the difficulties faced by medicinal chemists seeking to achieve oral bioavailability in this challenging space are outlined. Guidance, opinion and advice based on the authors' own experiences in this area are offered in the hope this may be useful to others working in this fascinating frontier of drug discovery.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11561549 | PMC |
| http://dx.doi.org/10.1039/d4md00769g | DOI Listing |
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